A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
A membrane glycoprotein and differentiation antigen expressed on the surface of T-cells that binds to CD40 ANTIGENS on B-LYMPHOCYTES and induces their proliferation. Mutation of the gene for CD40 ligand is a cause of HYPER-IGM IMMUNODEFICIENCY SYNDROME, TYPE 1.
A transmembrane protein belonging to the tumor necrosis factor superfamily that was originally discovered on cells of the lymphoid-myeloid lineage, including activated T-LYMPHOCYTES and NATURAL KILLER CELLS. It plays an important role in immune homeostasis and cell-mediated toxicity by binding to the FAS RECEPTOR and triggering APOPTOSIS.
The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.
A transmembrane protein belonging to the tumor necrosis factor superfamily that specifically binds RECEPTOR ACTIVATOR OF NUCLEAR FACTOR-KAPPA B and OSTEOPROTEGERIN. It plays an important role in regulating OSTEOCLAST differentiation and activation.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
A membrane-bound tumor necrosis family member found primarily on activated T-LYMPHOCYTES that binds specifically to CD30 ANTIGEN. It may play a role in INFLAMMATION and immune regulation.
Glycoproteins found on the membrane or surface of cells.
A transmembrane-protein belonging to the TNF family of intercellular signaling proteins. It is a widely expressed ligand that activates APOPTOSIS by binding to TNF-RELATED APOPTOSIS-INDUCING LIGAND RECEPTORS. The membrane-bound form of the protein can be cleaved by specific CYSTEINE ENDOPEPTIDASES to form a soluble ligand form.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
A membrane-bound tumor necrosis family member that is expressed on activated antigen-presenting cells such as B-LYMPHOCYTES and MACROPHAGES. It signals T-LYMPHOCYTES by binding the OX40 RECEPTOR.
The level of protein structure in which combinations of secondary protein structures (alpha helices, beta sheets, loop regions, and motifs) pack together to form folded shapes called domains. Disulfide bridges between cysteines in two different parts of the polypeptide chain along with other interactions between the chains play a role in the formation and stabilization of tertiary structure. Small proteins usually consist of only one domain but larger proteins may contain a number of domains connected by segments of polypeptide chain which lack regular secondary structure.
The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).
The rate dynamics in chemical or physical systems.
Established cell cultures that have the potential to propagate indefinitely.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A membrane bound member of the TNF superfamily that is expressed on activated B-LYMPHOCYTES; MACROPHAGES; and DENDRITIC CELLS. The ligand is specific for the 4-1BB RECEPTOR and may play a role in inducing the proliferation of activated peripheral blood T-LYMPHOCYTES.
Cell surface proteins that bind signalling molecules external to the cell with high affinity and convert this extracellular event into one or more intracellular signals that alter the behavior of the target cell (From Alberts, Molecular Biology of the Cell, 2nd ed, pp693-5). Cell surface receptors, unlike enzymes, do not chemically alter their ligands.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
Proteins which are found in membranes including cellular and intracellular membranes. They consist of two types, peripheral and integral proteins. They include most membrane-associated enzymes, antigenic proteins, transport proteins, and drug, hormone, and lectin receptors.
Proteins prepared by recombinant DNA technology.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
A tumor necrosis factor receptor subtype found in a variety of tissues and on activated LYMPHOCYTES. It has specificity for FAS LIGAND and plays a role in regulation of peripheral immune responses and APOPTOSIS. Multiple isoforms of the protein exist due to multiple ALTERNATIVE SPLICING. The activated receptor signals via a conserved death domain that associates with specific TNF RECEPTOR-ASSOCIATED FACTORS in the CYTOPLASM.
CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.
A costimulatory B7 antigen that has specificity for the T-CELL receptor PROGRAMMED CELL DEATH 1 RECEPTOR. It is closely-related to CD274 antigen; however, its expression is restricted to DENDRITIC CELLS and activated MACROPHAGES.
Cell surface molecules on cells of the immune system that specifically bind surface molecules or messenger molecules and trigger changes in the behavior of cells. Although these receptors were first identified in the immune system, many have important functions elsewhere.
The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.
Tumor necrosis factor receptor family members that are widely expressed and play a role in regulation of peripheral immune responses and APOPTOSIS. The receptors are specific for TNF-RELATED APOPTOSIS-INDUCING LIGAND and signal via conserved death domains that associate with specific TNF RECEPTOR-ASSOCIATED FACTORS in the CYTOPLASM.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
Recombinant proteins produced by the GENETIC TRANSLATION of fused genes formed by the combination of NUCLEIC ACID REGULATORY SEQUENCES of one or more genes with the protein coding sequences of one or more genes.
Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are linear polypeptides that are normally synthesized on RIBOSOMES.
Transport proteins that carry specific substances in the blood or across cell membranes.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
Intracellular receptors that can be found in the cytoplasm or in the nucleus. They bind to extracellular signaling molecules that migrate through or are transported across the CELL MEMBRANE. Many members of this class of receptors occur in the cytoplasm and are transported to the CELL NUCLEUS upon ligand-binding where they signal via DNA-binding and transcription regulation. Also included in this category are receptors found on INTRACELLULAR MEMBRANES that act via mechanisms similar to CELL SURFACE RECEPTORS.
Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
Adherence of cells to surfaces or to other cells.
A cell line derived from cultured tumor cells.
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
Differentiation antigens residing on mammalian leukocytes. CD stands for cluster of differentiation, which refers to groups of monoclonal antibodies that show similar reactivity with certain subpopulations of antigens of a particular lineage or differentiation stage. The subpopulations of antigens are also known by the same CD designation.
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.
Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.
Technique using an instrument system for making, processing, and displaying one or more measurements on individual cells obtained from a cell suspension. Cells are usually stained with one or more fluorescent dyes specific to cell components of interest, e.g., DNA, and fluorescence of each cell is measured as it rapidly transverses the excitation beam (laser or mercury arc lamp). Fluorescence provides a quantitative measure of various biochemical and biophysical properties of the cell, as well as a basis for cell sorting. Other measurable optical parameters include light absorption and light scattering, the latter being applicable to the measurement of cell size, shape, density, granularity, and stain uptake.
Regulatory proteins and peptides that are signaling molecules involved in the process of PARACRINE COMMUNICATION. They are generally considered factors that are expressed by one cell and are responded to by receptors on another nearby cell. They are distinguished from HORMONES in that their actions are local rather than distal.
A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
Antibodies produced by a single clone of cells.
A rigorously mathematical analysis of energy relationships (heat, work, temperature, and equilibrium). It describes systems whose states are determined by thermal parameters, such as temperature, in addition to mechanical and electromagnetic parameters. (From Hawley's Condensed Chemical Dictionary, 12th ed)
Peptides composed of between two and twelve amino acids.
Morphologic alteration of small B LYMPHOCYTES or T LYMPHOCYTES in culture into large blast-like cells able to synthesize DNA and RNA and to divide mitotically. It is induced by INTERLEUKINS; MITOGENS such as PHYTOHEMAGGLUTININS, and by specific ANTIGENS. It may also occur in vivo as in GRAFT REJECTION.
Lymphocytes responsible for cell-mediated immunity. Two types have been identified - cytotoxic (T-LYMPHOCYTES, CYTOTOXIC) and helper T-lymphocytes (T-LYMPHOCYTES, HELPER-INDUCER). They are formed when lymphocytes circulate through the THYMUS GLAND and differentiate to thymocytes. When exposed to an antigen, they divide rapidly and produce large numbers of new T cells sensitized to that antigen.
The process by which two molecules of the same chemical composition form a condensation product or polymer.
The characteristic three-dimensional shape of a molecule.
The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.
Linear POLYPEPTIDES that are synthesized on RIBOSOMES and may be further modified, crosslinked, cleaved, or assembled into complex proteins with several subunits. The specific sequence of AMINO ACIDS determines the shape the polypeptide will take, during PROTEIN FOLDING, and the function of the protein.
The level of protein structure in which regular hydrogen-bond interactions within contiguous stretches of polypeptide chain give rise to alpha helices, beta strands (which align to form beta sheets) or other types of coils. This is the first folding level of protein conformation.
Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A family of conserved cell surface receptors that contain EPIDERMAL GROWTH FACTOR repeats in their extracellular domain and ANKYRIN repeats in their cytoplasmic domains. The cytoplasmic domain of notch receptors is released upon ligand binding and translocates to the CELL NUCLEUS where it acts as transcription factor.
Theoretical representations that simulate the behavior or activity of chemical processes or phenomena; includes the use of mathematical equations, computers, and other electronic equipment.
Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.
Progressive restriction of the developmental potential and increasing specialization of function that leads to the formation of specialized cells, tissues, and organs.
CELL LINES derived from the CV-1 cell line by transformation with a replication origin defective mutant of SV40 VIRUS, which codes for wild type large T antigen (ANTIGENS, POLYOMAVIRUS TRANSFORMING). They are used for transfection and cloning. (The CV-1 cell line was derived from the kidney of an adult male African green monkey (CERCOPITHECUS AETHIOPS).)
The color-furnishing portion of hemoglobin. It is found free in tissues and as the prosthetic group in many hemeproteins.
Cell surface receptors that bind TUMOR NECROSIS FACTORS and trigger changes which influence the behavior of cells.
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
A large group of proteins that control APOPTOSIS. This family of proteins includes many ONCOGENE PROTEINS as well as a wide variety of classes of INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS such as CASPASES.
A member of tumor necrosis factor superfamily found on MACROPHAGES; DENDRITIC CELLS and T-LYMPHOCYTES. It occurs as transmembrane protein that can be cleaved to release a secreted form that specifically binds to TRANSMEMBRANE ACTIVATOR AND CAML INTERACTOR PROTEIN; and B CELL MATURATION ANTIGEN.
Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).
A member of the tumor necrosis factor receptor superfamily with specificity for CD40 LIGAND. It is found on mature B-LYMPHOCYTES and some EPITHELIAL CELLS, lymphoid DENDRITIC CELLS. Evidence suggests that CD40-dependent activation of B-cells is important for generation of memory B-cells within the germinal centers. Mutations of the gene for CD40 antigen result in HYPER-IGM IMMUNODEFICIENCY SYNDROME, TYPE 3. Signaling of the receptor occurs through its association with TNF RECEPTOR-ASSOCIATED FACTORS.
An activating NK cell lectin-like receptor subfamily that regulates immune responses to INFECTION and NEOPLASMS. Members of this subfamily generally occur as homodimers.
Cellular uptake of extracellular materials within membrane-limited vacuoles or microvesicles. ENDOSOMES play a central role in endocytosis.
A variation of the PCR technique in which cDNA is made from RNA via reverse transcription. The resultant cDNA is then amplified using standard PCR protocols.
A positive regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.
The modification of the reactivity of ENZYMES by the binding of effectors to sites (ALLOSTERIC SITES) on the enzymes other than the substrate BINDING SITES.
A family of proteins that were originally identified by their ability to cause NECROSIS of NEOPLASMS. Their necrotic effect on cells is mediated through TUMOR NECROSIS FACTOR RECEPTORS which induce APOPTOSIS.
Carbon monoxide (CO). A poisonous colorless, odorless, tasteless gas. It combines with hemoglobin to form carboxyhemoglobin, which has no oxygen carrying capacity. The resultant oxygen deprivation causes headache, dizziness, decreased pulse and respiratory rates, unconsciousness, and death. (From Merck Index, 11th ed)
Serum glycoprotein produced by activated MACROPHAGES and other mammalian MONONUCLEAR LEUKOCYTES. It has necrotizing activity against tumor cell lines and increases ability to reject tumor transplants. Also known as TNF-alpha, it is only 30% homologous to TNF-beta (LYMPHOTOXIN), but they share TNF RECEPTORS.
Specialized cells of the hematopoietic system that have branch-like extensions. They are found throughout the lymphatic system, and in non-lymphoid tissues such as SKIN and the epithelia of the intestinal, respiratory, and reproductive tracts. They trap and process ANTIGENS, and present them to T-CELLS, thereby stimulating CELL-MEDIATED IMMUNITY. They are different from the non-hematopoietic FOLLICULAR DENDRITIC CELLS, which have a similar morphology and immune system function, but with respect to humoral immunity (ANTIBODY PRODUCTION).
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
A family of pattern recognition receptors characterized by an extracellular leucine-rich domain and a cytoplasmic domain that share homology with the INTERLEUKIN 1 RECEPTOR and the DROSOPHILA toll protein. Following pathogen recognition, toll-like receptors recruit and activate a variety of SIGNAL TRANSDUCING ADAPTOR PROTEINS.
Endogenous substances, usually proteins, which are effective in the initiation, stimulation, or termination of the genetic transcription process.
The movement of cells from one location to another. Distinguish from CYTOKINESIS which is the process of dividing the CYTOPLASM of a cell.
Neutral or negatively charged ligands bonded to metal cations or neutral atoms. The number of ligand atoms to which the metal center is directly bonded is the metal cation's coordination number, and this number is always greater than the regular valence or oxidation number of the metal. A coordination complex can be negative, neutral, or positively charged.
Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.
A tumor necrosis factor receptor family member that is specific for RANK LIGAND and plays a role in bone homeostasis by regulating osteoclastogenesis. It is also expressed on DENDRITIC CELLS where it plays a role in regulating dendritic cell survival. Signaling by the activated receptor occurs through its association with TNF RECEPTOR-ASSOCIATED FACTORS.
A class of compounds of the type R-M, where a C atom is joined directly to any other element except H, C, N, O, F, Cl, Br, I, or At. (Grant & Hackh's Chemical Dictionary, 5th ed)
A family of transmembrane glycoproteins (MEMBRANE GLYCOPROTEINS) consisting of noncovalent heterodimers. They interact with a wide variety of ligands including EXTRACELLULAR MATRIX PROTEINS; COMPLEMENT, and other cells, while their intracellular domains interact with the CYTOSKELETON. The integrins consist of at least three identified families: the cytoadhesin receptors(RECEPTORS, CYTOADHESIN), the leukocyte adhesion receptors (RECEPTORS, LEUKOCYTE ADHESION), and the VERY LATE ANTIGEN RECEPTORS. Each family contains a common beta-subunit (INTEGRIN BETA CHAINS) combined with one or more distinct alpha-subunits (INTEGRIN ALPHA CHAINS). These receptors participate in cell-matrix and cell-cell adhesion in many physiologically important processes, including embryological development; HEMOSTASIS; THROMBOSIS; WOUND HEALING; immune and nonimmune defense mechanisms; and oncogenic transformation.
A genus of the family Muridae consisting of eleven species. C. migratorius, the grey or Armenian hamster, and C. griseus, the Chinese hamster, are the two species used in biomedical research.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.
The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.
Bone marrow-derived lymphocytes that possess cytotoxic properties, classically directed against transformed and virus-infected cells. Unlike T CELLS; and B CELLS; NK CELLS are not antigen specific. The cytotoxicity of natural killer cells is determined by the collective signaling of an array of inhibitory and stimulatory CELL SURFACE RECEPTORS. A subset of T-LYMPHOCYTES referred to as NATURAL KILLER T CELLS shares some of the properties of this cell type.
Non-antibody proteins secreted by inflammatory leukocytes and some non-leukocytic cells, that act as intercellular mediators. They differ from classical hormones in that they are produced by a number of tissue or cell types rather than by specialized glands. They generally act locally in a paracrine or autocrine rather than endocrine manner.
Laboratory mice that have been produced from a genetically manipulated EGG or EMBRYO, MAMMALIAN.
A class of cellular receptors that have an intrinsic PROTEIN-TYROSINE KINASE activity.
The arrangement of two or more amino acid or base sequences from an organism or organisms in such a way as to align areas of the sequences sharing common properties. The degree of relatedness or homology between the sequences is predicted computationally or statistically based on weights assigned to the elements aligned between the sequences. This in turn can serve as a potential indicator of the genetic relatedness between the organisms.
A biosensing technique in which biomolecules capable of binding to specific analytes or ligands are first immobilized on one side of a metallic film. Light is then focused on the opposite side of the film to excite the surface plasmons, that is, the oscillations of free electrons propagating along the film's surface. The refractive index of light reflecting off this surface is measured. When the immobilized biomolecules are bound by their ligands, an alteration in surface plasmons on the opposite side of the film is created which is directly proportional to the change in bound, or adsorbed, mass. Binding is measured by changes in the refractive index. The technique is used to study biomolecular interactions, such as antigen-antibody binding.
The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
Short sequences (generally about 10 base pairs) of DNA that are complementary to sequences of messenger RNA and allow reverse transcriptases to start copying the adjacent sequences of mRNA. Primers are used extensively in genetic and molecular biology techniques.
A conjugated protein which is the oxygen-transporting pigment of muscle. It is made up of one globin polypeptide chain and one heme group.
Conjugated protein-carbohydrate compounds including mucins, mucoid, and amyloid glycoproteins.
The naturally occurring or experimentally induced replacement of one or more AMINO ACIDS in a protein with another. If a functionally equivalent amino acid is substituted, the protein may retain wild-type activity. Substitution may also diminish, enhance, or eliminate protein function. Experimentally induced substitution is often used to study enzyme activities and binding site properties.
Elements of limited time intervals, contributing to particular results or situations.
A computer simulation technique that is used to model the interaction between two molecules. Typically the docking simulation measures the interactions of a small molecule or ligand with a part of a larger molecule such as a protein.
All of the processes involved in increasing CELL NUMBER including CELL DIVISION.
Cell surface glycoproteins that bind to chemokines and thus mediate the migration of pro-inflammatory molecules. The receptors are members of the seven-transmembrane G protein-coupled receptor family. Like the CHEMOKINES themselves, the receptors can be divided into at least three structural branches: CR, CCR, and CXCR, according to variations in a shared cysteine motif.
An essential amino acid that is required for the production of HISTAMINE.
THIAZOLES with two keto oxygens. Members are insulin-sensitizing agents which overcome INSULIN RESISTANCE by activation of the peroxisome proliferator activated receptor gamma (PPAR-gamma).
A secreted member of the TNF receptor superfamily that negatively regulates osteoclastogenesis. It is a soluble decoy receptor of RANK LIGAND that inhibits both CELL DIFFERENTIATION and function of OSTEOCLASTS by inhibiting the interaction between RANK LIGAND and RECEPTOR ACTIVATOR OF NUCLEAR FACTOR-KAPPA B.
Cell adhesion molecule and CD antigen that serves as a homing receptor for lymphocytes to lymph node high endothelial venules.
A CELL LINE derived from human T-CELL LEUKEMIA and used to determine the mechanism of differential susceptibility to anti-cancer drugs and radiation.
A cell line generated from human embryonic kidney cells that were transformed with human adenovirus type 5.
Inorganic or organic compounds derived from phosphine (PH3) by the replacement of H atoms. (From Grant & Hackh's Chemical Dictionary, 5th ed)
A negative regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
Group of chemokines with paired cysteines separated by a different amino acid. CXC chemokines are chemoattractants for neutrophils but not monocytes.
Surface ligands, usually glycoproteins, that mediate cell-to-cell adhesion. Their functions include the assembly and interconnection of various vertebrate systems, as well as maintenance of tissue integration, wound healing, morphogenic movements, cellular migrations, and metastasis.
A collection of cloned peptides, or chemically synthesized peptides, frequently consisting of all possible combinations of amino acids making up an n-amino acid peptide.
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
Proteins that contain an iron-porphyrin, or heme, prosthetic group resembling that of hemoglobin. (From Lehninger, Principles of Biochemistry, 1982, p480)
A hematopoietic growth factor and the ligand of the cell surface c-kit protein (PROTO-ONCOGENE PROTEINS C-KIT). It is expressed during embryogenesis and is a growth factor for a number of cell types including the MAST CELLS and the MELANOCYTES in addition to the HEMATOPOIETIC STEM CELLS.
Proteins and peptides that are involved in SIGNAL TRANSDUCTION within the cell. Included here are peptides and proteins that regulate the activity of TRANSCRIPTION FACTORS and cellular processes in response to signals from CELL SURFACE RECEPTORS. Intracellular signaling peptide and proteins may be part of an enzymatic signaling cascade or act through binding to and modifying the action of other signaling factors.
The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
Cell adhesion molecule and CD antigen that mediates the adhesion of neutrophils and monocytes to activated platelets and endothelial cells.
Histochemical localization of immunoreactive substances using labeled antibodies as reagents.
A cell surface receptor involved in regulation of cell growth and differentiation. It is specific for EPIDERMAL GROWTH FACTOR and EGF-related peptides including TRANSFORMING GROWTH FACTOR ALPHA; AMPHIREGULIN; and HEPARIN-BINDING EGF-LIKE GROWTH FACTOR. The binding of ligand to the receptor causes activation of its intrinsic tyrosine kinase activity and rapid internalization of the receptor-ligand complex into the cell.
A computer simulation developed to study the motion of molecules over a period of time.
Commonly observed structural components of proteins formed by simple combinations of adjacent secondary structures. A commonly observed structure may be composed of a CONSERVED SEQUENCE which can be represented by a CONSENSUS SEQUENCE.
A technique applicable to the wide variety of substances which exhibit paramagnetism because of the magnetic moments of unpaired electrons. The spectra are useful for detection and identification, for determination of electron structure, for study of interactions between molecules, and for measurement of nuclear spins and moments. (From McGraw-Hill Encyclopedia of Science and Technology, 7th edition) Electron nuclear double resonance (ENDOR) spectroscopy is a variant of the technique which can give enhanced resolution. Electron spin resonance analysis can now be used in vivo, including imaging applications such as MAGNETIC RESONANCE IMAGING.
Single-stranded complementary DNA synthesized from an RNA template by the action of RNA-dependent DNA polymerase. cDNA (i.e., complementary DNA, not circular DNA, not C-DNA) is used in a variety of molecular cloning experiments as well as serving as a specific hybridization probe.
A class of animal lectins that bind to carbohydrate in a calcium-dependent manner. They share a common carbohydrate-binding domain that is structurally distinct from other classes of lectins.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
A nuclear transcription factor. Heterodimerization with RETINOID X RECEPTOR ALPHA is important in regulation of GLUCOSE metabolism and CELL GROWTH PROCESSES. It is a target of THIAZOLIDINEDIONES for control of DIABETES MELLITUS.
CXCR receptors that are expressed on the surface of a number of cell types, including T-LYMPHOCYTES; NK CELLS; DENDRITIC CELLS; and a subset of B-LYMPHOCYTES. The receptors are activated by CHEMOKINE CXCL9; CHEMOKINE CXCL10; and CHEMOKINE CXCL11.
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.
A subtype of RETINOIC ACID RECEPTORS that are specific for 9-cis-retinoic acid which function as nuclear TRANSCRIPTION FACTORS that regulate multiple signaling pathways.
A thiol-containing non-essential amino acid that is oxidized to form CYSTINE.
NMR spectroscopy on small- to medium-size biological macromolecules. This is often used for structural investigation of proteins and nucleic acids, and often involves more than one isotope.
Measurement of the intensity and quality of fluorescence.
The fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION.
The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.)
Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.
Proteins found in any species of bacterium.
Lymphoid cells concerned with humoral immunity. They are short-lived cells resembling bursa-derived lymphocytes of birds in their production of immunoglobulin upon appropriate stimulation.
A pattern recognition receptor that forms heterodimers with other TOLL-LIKE RECEPTORS. It interacts with multiple ligands including PEPTIDOGLYCAN, bacterial LIPOPROTEINS, lipoarabinomannan, and a variety of PORINS.
A B7 antigen that binds specifically to INDUCIBLE T-CELL CO-STIMULATOR PROTEIN on T-CELLS. It provides a costimulatory signal for T-cell proliferation and cytokine secretion.
Molecules on the surface of T-lymphocytes that recognize and combine with antigens. The receptors are non-covalently associated with a complex of several polypeptides collectively called CD3 antigens (ANTIGENS, CD3). Recognition of foreign antigen and the major histocompatibility complex is accomplished by a single heterodimeric antigen-receptor structure, composed of either alpha-beta (RECEPTORS, ANTIGEN, T-CELL, ALPHA-BETA) or gamma-delta (RECEPTORS, ANTIGEN, T-CELL, GAMMA-DELTA) chains.
A chemical reaction in which an electron is transferred from one molecule to another. The electron-donating molecule is the reducing agent or reductant; the electron-accepting molecule is the oxidizing agent or oxidant. Reducing and oxidizing agents function as conjugate reductant-oxidant pairs or redox pairs (Lehninger, Principles of Biochemistry, 1982, p471).
A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.
Proteins in the nucleus or cytoplasm that specifically bind RETINOIC ACID or RETINOL and trigger changes in the behavior of cells. Retinoic acid receptors, like steroid receptors, are ligand-activated transcription regulators. Several types have been recognized.
Endogenous glycoproteins from which SIALIC ACID has been removed by the action of sialidases. They bind tightly to the ASIALOGLYCOPROTEIN RECEPTOR which is located on hepatocyte plasma membranes. After internalization by adsorptive ENDOCYTOSIS they are delivered to LYSOSOMES for degradation. Therefore receptor-mediated clearance of asialoglycoproteins is an important aspect of the turnover of plasma glycoproteins. They are elevated in serum of patients with HEPATIC CIRRHOSIS or HEPATITIS.
Receptors that are specifically found on the surface of NATURAL KILLER CELLS. They play an important role in regulating the cellular component of INNATE IMMUNITY.
A critical subpopulation of T-lymphocytes involved in the induction of most immunological functions. The HIV virus has selective tropism for the T4 cell which expresses the CD4 phenotypic marker, a receptor for HIV. In fact, the key element in the profound immunosuppression seen in HIV infection is the depletion of this subset of T-lymphocytes.
A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.
Proteins that share the common characteristic of binding to carbohydrates. Some ANTIBODIES and carbohydrate-metabolizing proteins (ENZYMES) also bind to carbohydrates, however they are not considered lectins. PLANT LECTINS are carbohydrate-binding proteins that have been primarily identified by their hemagglutinating activity (HEMAGGLUTININS). However, a variety of lectins occur in animal species where they serve diverse array of functions through specific carbohydrate recognition.
Transmembrane proteins consisting of a lectin-like domain, an epidermal growth factor-like domain, and a variable number of domains that are homologous to complement regulatory proteins. They are important cell adhesion molecules which help LEUKOCYTES attach to VASCULAR ENDOTHELIUM.
The measurement of the quantity of heat involved in various processes, such as chemical reactions, changes of state, and formations of solutions, or in the determination of the heat capacities of substances. The fundamental unit of measurement is the joule or the calorie (4.184 joules). (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
The assembly of the QUATERNARY PROTEIN STRUCTURE of multimeric proteins (MULTIPROTEIN COMPLEXES) from their composite PROTEIN SUBUNITS.
Cell adhesion molecule and CD antigen that mediates neutrophil, monocyte, and memory T-cell adhesion to cytokine-activated endothelial cells. E-selectin recognizes sialylated carbohydrate groups related to the Lewis X or Lewis A family.
Computer-based representation of physical systems and phenomena such as chemical processes.
A change from planar to elliptic polarization when an initially plane-polarized light wave traverses an optically active medium. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A transmembrane domain containing ephrin that is specific for EPHB1 RECEPTOR; EPHB2 RECEPTOR and EPHB3 RECEPTOR. It is widely expressed in a variety of developing and adult tissues.
A large family of receptor protein-tyrosine kinases that are structurally-related. The name of this family of proteins derives from original protein Eph (now called the EPHA1 RECEPTOR), which was named after the cell line it was first discovered in: Erythropoietin-Producing human Hepatocellular carcinoma cell line. Members of this family have been implicated in regulation of cell-cell interactions involved in nervous system patterning and development.
Cytoplasmic proteins that bind certain aryl hydrocarbons, translocate to the nucleus, and activate transcription of particular DNA segments. AH receptors are identified by their high-affinity binding to several carcinogenic or teratogenic environmental chemicals including polycyclic aromatic hydrocarbons found in cigarette smoke and smog, heterocyclic amines found in cooked foods, and halogenated hydrocarbons including dioxins and polychlorinated biphenyls. No endogenous ligand has been identified, but an unknown natural messenger with a role in cell differentiation and development is suspected.
Nucleotide sequences, generated by iterative rounds of SELEX APTAMER TECHNIQUE, that bind to a target molecule specifically and with high affinity.
A site on an enzyme which upon binding of a modulator, causes the enzyme to undergo a conformational change that may alter its catalytic or binding properties.
A transmembrane domain containing ephrin that binds with high affinity to EPHB1 RECEPTOR; EPHB3 RECEPTOR; and EPHB4 RECEPTOR. Expression of ephrin-B2 occurs in a variety of adult tissues. During embryogenesis, high levels of ephrin-B2 is seen in the PROSENCEPHALON; RHOMBENCEPHALON; developing SOMITES; LIMB BUD; and bronchial arches.
The characteristic 3-dimensional shape and arrangement of multimeric proteins (aggregates of more than one polypeptide chain).
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
A large multinuclear cell associated with the BONE RESORPTION. An odontoclast, also called cementoclast, is cytomorphologically the same as an osteoclast and is involved in CEMENTUM resorption.
Unstable isotopes of iodine that decay or disintegrate emitting radiation. I atoms with atomic weights 117-139, except I 127, are radioactive iodine isotopes.
A notch receptor that interacts with a variety of ligands and regulates SIGNAL TRANSDUCTION PATHWAYS for multiple cellular processes. It is widely expressed during EMBRYOGENESIS and is essential for EMBRYONIC DEVELOPMENT.
Group of chemokines with adjacent cysteines that are chemoattractants for lymphocytes, monocytes, eosinophils, basophils but not neutrophils.
A chromatographic technique that utilizes the ability of biological molecules to bind to certain ligands specifically and reversibly. It is used in protein biochemistry. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A species of CERCOPITHECUS containing three subspecies: C. tantalus, C. pygerythrus, and C. sabeus. They are found in the forests and savannah of Africa. The African green monkey (C. pygerythrus) is the natural host of SIMIAN IMMUNODEFICIENCY VIRUS and is used in AIDS research.
The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability.
Immunoglobulin molecules having a specific amino acid sequence by virtue of which they interact only with the ANTIGEN (or a very similar shape) that induced their synthesis in cells of the lymphoid series (especially PLASMA CELLS).
Proteins that originate from insect species belonging to the genus DROSOPHILA. The proteins from the most intensely studied species of Drosophila, DROSOPHILA MELANOGASTER, are the subject of much interest in the area of MORPHOGENESIS and development.
An inhibitory B7 antigen that has specificity for the T-CELL receptor PROGRAMMED CELL DEATH 1 PROTEIN. CD274 antigen provides negative signals that control and inhibit T-cell responses and is found at higher than normal levels on tumor cells, suggesting its potential role in TUMOR IMMUNE EVASION.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
Large, phagocytic mononuclear leukocytes produced in the vertebrate BONE MARROW and released into the BLOOD; contain a large, oval or somewhat indented nucleus surrounded by voluminous cytoplasm and numerous organelles.
Analysis of the intensity of Raman scattering of monochromatic light as a function of frequency of the scattered light.
The art or process of comparing photometrically the relative intensities of the light in different parts of the spectrum.
The measurement of the amplitude of the components of a complex waveform throughout the frequency range of the waveform. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
A heavy metal trace element with the atomic symbol Cu, atomic number 29, and atomic weight 63.55.
The biosynthesis of RNA carried out on a template of DNA. The biosynthesis of DNA from an RNA template is called REVERSE TRANSCRIPTION.
A technique of culturing mixed cell types in vitro to allow their synergistic or antagonistic interactions, such as on CELL DIFFERENTIATION or APOPTOSIS. Coculture can be of different types of cells, tissues, or organs from normal or disease states.
Large marine mammals of the order CETACEA. In the past, they were commercially valued for whale oil, for their flesh as human food and in ANIMAL FEED and FERTILIZERS, and for baleen. Today, there is a moratorium on most commercial whaling, as all species are either listed as endangered or threatened.

Regulation of body length and male tail ray pattern formation of Caenorhabditis elegans by a member of TGF-beta family. (1/24796)

We have identified a new member of the TGF-beta superfamily, CET-1, from Caenorhabditis elegans, which is expressed in the ventral nerve cord and other neurons. cet-1 null mutants have shortened bodies and male tail abnormal phenotype resembling sma mutants, suggesting cet-1, sma-2, sma-3 and sma-4 share a common pathway. Overexpression experiments demonstrated that cet-1 function requires wild-type sma genes. Interestingly, CET-1 appears to affect body length in a dose-dependent manner. Heterozygotes for cet-1 displayed body lengths ranging between null mutant and wild type, and overexpression of CET-1 in wild-type worms elongated body length close to lon mutants. In male sensory ray patterning, lack of cet-1 function results in ray fusions. Epistasis analysis revealed that mab-21 lies downstream and is negatively regulated by the cet-1/sma pathway in the male tail. Our results show that cet-1 controls diverse biological processes during C. elegans development probably through different target genes.  (+info)

Dominant activity of activation function 1 (AF-1) and differential stoichiometric requirements for AF-1 and -2 in the estrogen receptor alpha-beta heterodimeric complex. (2/24796)

Estrogenic responses are now known to be mediated by two forms of estrogen receptors (ER), ERalpha and ERbeta, that can function as homodimers or heterodimers. As homodimers the two have been recently shown to exhibit distinct transcriptional responses to estradiol (E2), antiestrogens, and coactivators, suggesting that the ER complexes are not functionally equivalent. However, because the three possible configurations of ER complexes all recognize the same estrogen response element, it has not been possible to evaluate the transcriptional properties of the ER heterodimer complex by transfection assays. Using ER subunits with modified DNA recognition specificity, we were able to measure the transcriptional properties of ERalpha-ERbeta heterodimers in transfected cells without interference from the two ER homodimer complexes. We first demonstrated that the individual activation function 1 (AF-1) domains act in a dominant manner within the ERalpha-ERbeta heterodimer: the mixed agonist-antagonist 4-hydroxytamoxifen acts as an agonist in a promoter- and cell context-dependent manner via the ERalpha AF-1, while activation of the complex by the mitogen-activated protein kinase (MAPK) pathway requires only the ERalpha- or ERbeta-responsive MAPK site. Using ligand-binding and AF-2-defective mutants, we further demonstrated that while the ERalpha-ERbeta heterodimer can be activated when only one E2-binding competent partner is present per dimer, two functional AF-2 domains are required for transcriptional activity. Taken together, the results of this study of a retinoid X receptor-independent heterodimer complex, the first such study, provide evidence of different stoichiometric requirements for AF-1 and -2 activity and demonstrate that AF-1 receptor-specific properties are maintained within the ERalpha-ERbeta heterodimer.  (+info)

Neu differentiation factor stimulates phosphorylation and activation of the Sp1 transcription factor. (3/24796)

Neu differentiation factors (NDFs), or neuregulins, are epidermal growth factor-like growth factors which bind to two tyrosine kinase receptors, ErbB-3 and ErbB-4. The transcription of several genes is regulated by neuregulins, including genes encoding specific subunits of the acetylcholine receptor at the neuromuscular junction. Here, we have examined the promoter of the acetylcholine receptor epsilon subunit and delineated a minimal CA-rich sequence which mediates transcriptional activation by NDF (NDF-response element [NRE]). Using gel mobility shift analysis with an NRE oligonucleotide, we detected two complexes that are induced by treatment with neuregulin and other growth factors and identified Sp1, a constitutively expressed zinc finger phosphoprotein, as a component of one of these complexes. Phosphatase treatment, two-dimensional gel electrophoresis, and an in-gel kinase assay indicated that Sp1 is phosphorylated by a 60-kDa kinase in response to NDF-induced signals. Moreover, Sp1 seems to act downstream of all members of the ErbB family and thus may funnel the signaling of the ErbB network into the nucleus.  (+info)

Ligand substitution of receptor targeted DNA complexes affects gene transfer into hepatoma cells. (4/24796)

We have targeted the serpin enzyme complex receptor for gene transfer in human hepatoma cell lines using peptides < 30 amino acids in length which contain the five amino acid recognition sequence for this receptor, coupled to poly K of average chain length 100 K, using the heterobifunctional coupling reagent sulfo-LC SPDP. The number of sulfo-LC SPDP modified poly-L-lysine residues, as well as the degree of peptide substitution was assessed by nuclear magnetic resonance spectroscopy. Conjugates were prepared in which 3.5%, 7.8% or 26% of the lysine residues contained the sulfo-LC SPDP moiety. Each of these conjugates was then coupled with ligand peptides so that one in 370, one in 1039, or one in 5882 lysines were substituted with receptor ligand. Electron microscopy and atomic force microscopy were used to assess complex structure and size. HuH7 human hepatoma cells were transfected with complexes of these conjugates with the plasmid pGL3 and luciferase expression measured 2 to 16 days after treatment. All the protein conjugates in which 26% of the K residues were modified with sulfo-LC SPDP were poor gene transfer reagents. Complexes containing less substituted poly K, averaged 17 +/- 0.5 nm in diameter and gave peak transgene expression of 3-4 x 10(6) ILU/mg which persisted (> 7 x 10(5) ILU) at 16 days. Of these, more substituted polymers condensed DNA into complexes averaging 20 +/- 0.7 nm in diameter and gave five-fold less luciferase than complexes containing less substituted conjugates. As few as eight to 11 ligands per complex are optimal for DNA delivery via the SEC receptor. The extent of substitution of receptor-mediated gene transfer complexes affects the size of the complexes, as well as the intensity and duration of transgene expression. These observations may permit tailoring of complex construction for the usage required.  (+info)

p27 is involved in N-cadherin-mediated contact inhibition of cell growth and S-phase entry. (5/24796)

In this study the direct involvement of cadherins in adhesion-mediated growth inhibition was investigated. It is shown here that overexpression of N-cadherin in CHO cells significantly suppresses their growth rate. Interaction of these cells and two additional fibroblastic lines with synthetic beads coated with N-cadherin ligands (recombinant N-cadherin ectodomain or specific antibodies) leads to growth arrest at the G1 phase of the cell cycle. The cadherin-reactive beads inhibit the entry into S phase and the reduction in the levels of cyclin-dependent kinase (cdk) inhibitors p21 and p27, following serum-stimulation of starved cells. In exponentially growing cells these beads induce G1 arrest accompanied by elevation in p27 only. We propose that cadherin-mediated signaling is involved in contact inhibition of growth by inducing cell cycle arrest at the G1 phase and elevation of p27 levels.  (+info)

Thymic selection by a single MHC/peptide ligand: autoreactive T cells are low-affinity cells. (6/24796)

In H2-M- mice, the presence of a single peptide, CLIP, bound to MHC class II molecules generates a diverse repertoire of CD4+ cells. In these mice, typical self-peptides are not bound to class II molecules, with the result that a very high proportion of H2-M- CD4+ cells are responsive to the various peptides displayed on normal MHC-compatible APC. We show here, however, that such "self" reactivity is controlled by low-affinity CD4+ cells. These cells give spectacularly high proliferative responses but are virtually unreactive in certain other assays, e.g., skin graft rejection; responses to MHC alloantigens, by contrast, are intense in all assays. Possible explanations for why thymic selection directed to a single peptide curtails self specificity without affecting alloreactivity are discussed.  (+info)

Calorimetric studies on the stability of the ribosome-inactivating protein abrin II: effects of pH and ligand binding. (7/24796)

The effects of pH and ligand binding on the stability of abrin II, a heterodimeric ribosome-inactivating protein, and its subunits have been studied using high-sensitivity differential scanning calorimetry. At pH7.2, the calorimetric scan consists of two transitions, which correspond to the B-subunit [transition temperature (Tm) 319.2K] and the A-subunit (Tm 324.6K) of abrin II, as also confirmed by studies on the isolated A-subunit. The calorimetric enthalpy of the isolated A-subunit of abrin II is similar to that of the higher-temperature transition. However, its Tm is 2.4K lower than that of the higher-temperature peak of intact abrin II. This indicates that there is some interaction between the two subunits. Abrin II displays increased stability as the pH is decreased to 4.5. Lactose increases the Tm values as well as the enthalpies of both transitions. This effect is more pronounced at pH7.2 than at pH4.5. This suggests that ligand binding stabilizes the native conformation of abrin II. Analysis of the B-subunit transition temperature as a function of lactose concentration suggests that two lactose molecules bind to one molecule of abrin II at pH7.2. The presence of two binding sites for lactose on the abrin II molecule is also indicated by isothermal titration calorimetry. Plotting DeltaHm (the molar transition enthalpy at Tm) against Tm yielded values for DeltaCp (change in excess heat capacity) of 27+/-2 kJ.mol-1.K-1 for the B-subunit and 20+/-1 kJ.mol-1.K-1 for the A-subunit. These values have been used to calculate the thermal stability of abrin II and to surmise the mechanism of its transmembrane translocation.  (+info)

The integrin alpha v beta 6 binds and activates latent TGF beta 1: a mechanism for regulating pulmonary inflammation and fibrosis. (8/24796)

Transforming growth factor beta (TGF beta) family members are secreted in inactive complexes with a latency-associated peptide (LAP), a protein derived from the N-terminal region of the TGF beta gene product. Extracellular activation of these complexes is a critical but incompletely understood step in regulation of TGF beta function in vivo. We show that TGF beta 1 LAP is a ligand for the integrin alpha v beta 6 and that alpha v beta 6-expressing cells induce spatially restricted activation of TGF beta 1. This finding explains why mice lacking this integrin develop exaggerated inflammation and, as we show, are protected from pulmonary fibrosis. These data identify a novel mechanism for locally regulating TGF beta 1 function in vivo by regulating expression of the alpha v beta 6 integrin.  (+info)

Clearly, the reliability of the relative affinity of a candidate ligand relies on the validity of Eq.(6), and requires the simultaneous satisfaction of the following prerequisites for the pair of the candidate ligand and its reference ligand. (a) The candidate ligand and its reference ligand bind to the same site(s) on the target. In practice, the binding site(s) of the candidate ligand can be judged based on its competitive binding against a reference ligand but can not be optimized. (b) The candidate ligand and its reference ligand, in both the PMFS and the concentrated extract, produce peak areas within their own linear ranges. (c) The candidate ligand and its reference ligand, in both the PMFS and the concentrated extract, produce peak areas over five times the absolute values of their own intercepts of linear response. (d) The candidate ligand and its reference ligand have binding ratios of below 10% in the competitive binding system. All the later three prerequisites should be met by ...
TY - JOUR. T1 - Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism. AU - Shiau, Andrew K.. AU - Barstad, Danielle. AU - Radek, James T.. AU - Meyers, Marvin J.. AU - Nettles, Kendall W.. AU - Katzenellenbogen, Benita S.. AU - Katzenellenbogen, John A.. AU - Agard, David A.. AU - Greene, Geoffrey L.. N1 - Funding Information: We thank T. Earnest for advice and assistance at beamline 5.0.2 (ALS is funded by the US Department of Energy Office of Basic Energy Sciences). We also thank M. Butte, N. Ota and Y. Shibata for assistance with data collection; P. Coward, A. Derman, and Y. Li for comments on the manuscript; and H. Deacon for extensive graphical assistance. This work was supported by the NIH (B.S.K, J.A.K. and D.A.A), the Howard Hughes Medical Institute (D.A.A.), the Susan G. Komen Breast Cancer Foundation (G.L.G.), the USAMRMC (G.L.G.) and the Illinois Department of Public Health (G.L.G). In the initial phases of this work, A.K.S. ...
Protein target information for Chain A, ESTRADIOL RECEPTOR (human). Find diseases associated with this biological target and compounds tested against it in bioassay experiments.
Ligand binding assays (LBA) is an assay, or an analytic procedure, whose procedure or method relies on the binding of ligand molecules to receptors, antibodies or other macromolecules. A detection method is used to determine the presence and extent of the ligand-receptor complexes formed, and this is usually determined electrochemically or through a fluorescence detection method. This type of analytic test can be used to test for the presence of target molecules in a sample that are known to bind to the receptor. There are numerous types of ligand binding assays, both radioactive and non-radioactive. As such, ligand binding assays are a superset of radiobinding assays, which are the conceptual inverse of radioimmunoassays (RIA). Some newer types are called mix-and-measure assays because they do not require separation of bound ligands. Ligand binding assays are used primarily in pharmacology for various demands. Specifically, despite the human bodys endogenous receptors, hormones, and other ...
The nature of the ligands dictates the composition, molecular formulae, atomic structure and the physical properties of thiolate protected gold nanomolecules, Aun(SR)m. In this review, we describe the ligand effect for three classes of thiols namely, aliphatic, AL or aliphatic-like, aromatic, AR, or bulky, BU thiol ligands. The ligand effect is demonstrated using three experimental setups namely: (1) The nanomolecule series obtained by direct synthesis using AL, AR, and BU ligands; (2) Molecular conversion and interconversion between Au38(S-AL)24, Au36(S-AR)24, and Au30(S-BU)18 nanomolecules; and (3) Synthesis of Au38, Au36, and Au30 nanomolecules from one precursor Aun(S-glutathione)m upon reacting with AL, AR, and BU ligands. These nanomolecules possess unique geometric core structure, metal-ligand staple interface, optical and electrochemical properties. The results unequivocally demonstrate that the ligand structure determines the nanomolecules atomic structure, metal-ligand interface and
TY - CHAP. T1 - Induction of cell adhesion and cell spreading by various cell surface ligands. AU - Grinnell, F.. PY - 1977. Y1 - 1977. UR - http://www.scopus.com/inward/record.url?scp=17344391658&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=17344391658&partnerID=8YFLogxK. M3 - Chapter. AN - SCOPUS:17344391658. VL - 6. BT - Journal of Supramolecular and Cellular Biochemistry. ER - ...
Glyconanomaterials, nanomaterials carrying multiple carbohydrate ligands, provide an excellent platform for sensitive protein recognition. Using nanomaterials as the scaffold, multivalent interactions between glycan ligands and proteins have been demonstrated. However, the quantitative analysis of the binding affinity of these glyconanomaterials has been lacking. In this Article, we report a new method to measure the binding affinity of glyconanoparticle (GNP)-protein interactions based on a fluorescent competition binding assay, which yielded the apparent dissociation constant (K-d) of GNPs with the interacting protein. Au nanoparticles conjugated with underivatized mono-, oligo-, and polysaccharides were synthesized using our recently developed photocoupling chemistry. The affinities of these GNPs with lectins were measured and were several orders of magnitude higher than the corresponding free ligands with lectins. The effect of ligand display on the binding affinity of GNPs was, furthermore, ...
PREFACE TO THE SIXTH EDITION. ABBREVIATIONS.. 1. Applications in Coordination Chemistry.. 1.1. Ammine, Amido, and Related Complexes.. 1.2. Complexes of Ethylenediamine and Related Ligands.. 1.3. Complexes of Pyridine and Related Ligands.. 1.4. Complexes of Bipyridine and Related Ligands.. 1.5. Metalloporphyrins.. 1.6. Metallochlorins, Chlorophylls, and Metallophthalocyanines.. 1.7. Nitro and Nitrito Complexes.. 1.8. Lattice Water and Aquo and Hydroxo Complexes.. 1.9. Complexes of Alkoxides, Alcohols, Ethers, Ketones, Aldehydes, Esters, and Carboxylic Acids.. 1.10. Complexes of Amino Acids, EDTA, and Related Ligands.. 1.11. Infrared Spectra of Aqueous Solutions.. 1.12. Complexes of Oxalato and Related Ligands.. 1.13. Complexes of Sulfate, Carbonate, and Related Ligands.. 1.14. Complexes of b-Diketones.. 1.15. Complexes of Urea, Sulfoxides, and Related Ligands.. 1.16. Cyano and Nitrile Complexes.. 1.17. Thiocyanato and Other Pseudohalogeno Complexes.. 1.18. Complexes of Carbon Monoxide.. 1.19. ...
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Multivalency achieves strong, yet reversible binding by the simultaneous formation of multiple weak bonds. It is a key interaction principle in biology and promising for the synthesis of high-affinity inhibitors of pathogens. We present a molecular model for the binding affinity of synthetic multivalent ligands onto multivalent receptors consisting of n receptor units arranged on a regular polygon. Ligands consist of a geometrically matching rigid polygonal core to which monovalent ligand units are attached via flexible linker polymers, closely mimicking existing experimental designs. The calculated binding affinities quantitatively agree with experimental studies for cholera toxin (n = 5) and anthrax receptor (n = 7) and allow to predict optimal core size and optimal linker length. Maximal binding affinity is achieved for a core that matches the receptor size and for linkers that have an equilibrium end-to-end distance that is slightly longer than the geometric separation between ligand core ...
This invention is directed to a ligand-receptor assay for determining the presence of at least one target ligand, capable of competing with a ligand analogue conjugate for binding sites available on a ligand receptor, said ligand analogue conjugate comprising at least one ligand analogue coupled to a colloidal gold particle, in a fluid sample suspected of containing said target ligand comprising the steps of: a. contacting said fluid sample with said ligand analogue conjugate and said ligand receptor to form a homogeneous reaction mixture, the relative amounts of said ligand analogue conjugate and said ligand receptor being selected such that in the absence of said target ligand and subsequent to substantially equilibrium binding in said reaction mixture, substantially all of said ligand analogue conjugate is bound to said ligand receptor such that no unbound ligand analogue conjugate is detected as a result of the assay method; b. detecting unbound ligand analogue conjugates in said reaction mixture by
Antagonist-bound closed state GluA2 density map quality and resolutiona,b, GluA2em antagonist-bound closed state density map with coordinates for ATD dimers, LB
The new β2 Adrenoceptor (β2AR) crystal structures provide a high-resolution snapshot of receptor interactions with two particular partial inverse agonists, (−)-carazolol and timolol. However, both...
TY - JOUR. T1 - Comparison between single saturating dose ligand binding assay and enzyme immunoassay for low-salt extractable oestrogen and progesterone receptors in breast cancer. T2 - A multicentre study. AU - Gion, Massimo. AU - Dittadi, Ruggero. AU - Leon, Antonette E.. AU - Bruscagnin, Giuliano. AU - Pelizzola, Dario. AU - Giovannini, Gloria. AU - Giganti, Melchiorre. AU - Messeri, Gianni. AU - Quercioli, Massimo. AU - Flamini, Emanuela. AU - Riccobon, Angela. AU - Bozzetti, Cecilia. AU - Benecchi, Magda. AU - De Lena, Mario. AU - Paradiso, Angelo. AU - Ruggeri, Giuseppina. AU - Luisi, Patrizia. AU - Piffanelli, Adriano. PY - 1991. Y1 - 1991. N2 - An excellent correlation between ligand binding assay (LBA) and enzyme immunoassay (EIA) for both oestrogen (ER) and progesterone (PR) receptors has been reported. Nevertheless, considering that the clinical value of any discrepancy between LBA and EIA probably varies with the receptor level, we undertook a collaborative study in which a single ...
article{8565564, abstract = {Currently, there is mounting evidence that intermolecular receptor-receptor interactions may result in altered receptor recognition, pharmacology and signaling. Heterobivalent ligands have been proven useful as molecular probes for confirming and targeting heteromeric receptors. This report describes the design and synthesis of novel heterobivalent ligands for dopamine D-2-like receptors (D-2-likeR) and the -opioid receptor (OR) and their evaluation using ligand binding and functional assays. Interestingly, we identified a potent bivalent ligand that contains a short 18-atom linker and combines good potency with high efficacy both in -arrestin2 recruitment for OR and MAPK-P for D4R. Furthermore, this compound was characterized by a biphasic competition binding curve for the D4R-OR heterodimer, indicative of a bivalent binding mode. As this compound possibly bridges the D4R-OR heterodimer, it could be used as a pharmacological tool to further investigate the ...
Описан подробный протокол для выполнения титрования ELISA. Кроме того представлен Роман алгоритм оценки титрования ELISAs и получить...
In case functional assays are available TriCEPS coupled ligands can also be tested to see if a similar output is achievable with a TriCEPS coupled ligand compared to a ligand that is not coupled to TriCEPS.. In addition, TriCEPS V2.0 can be utilized as Flow Cytometry (FACS) reagent for detecting binding of primary amine containing molecules to cells.. As first step, the TriCEPS v.2.0 molecule is coupled to the ligand of interest (peptide, protein, Antibody, ADC or other primary amine containing molecules) and to the positive control ligand (e.g. transferrin) and negative control ligand (e.g. glycine). This coupling reaction is tested with Dot blot to assess if the coupling worked.. Then, the TriCEPS coupled ligands are then added to the non-oxidized cells to show that the ligand binds to the unknown targets at the cell surface and TriCEPS does not interfere with the ligand receptor interaction.. Flow Cytometry tests with TriCEPS coupled ligand on oxidized cells can be further performed to test ...
Binding Affinity Prediction of Protein-Ligand complex containing Zinc [ BAPPL-Z ] server computes the binding free energy of a zinc containing metalloprotein-ligand complex using an all atom energy based empirical scoring function
Recently the first community-wide assessments of the prediction of the structures of complexes between proteins and small molecule ligands have been reported in the so-called GPCR Dock 2008 and 2010 assessments. In the current review we discuss the different steps along the protein-ligand modeling workflow by critically analyzing the modeling strategies we used to predict the structures of protein-ligand complexes we submitted to the recent GPCR Dock 2010 challenge. These representative test cases, focusing on the pharmaceutically relevant G Protein-Coupled Receptors, are used to demonstrate the strengths and challenges of the different modeling methods. Our analysis indicates that the proper performance of the sequence alignment, introduction of structural adjustments guided by experimental data, and the usage of experimental data to identify protein-ligand interactions are critical steps in the protein-ligand modeling protocol.
Background: Using the popular program AutoDock, computer-aided docking of small ligands with 6 or fewer rotatable bonds, is reasonably fast and accurate. However, docking large ligands using AutoDocks recommended standard docking protocol is less accurate and computationally slow. Results: In our earlier work, we presented a novel AutoDock-based incremental protocol (DINC) that addresses the limitations of AutoDocks standard protocol by enabling improved docking of large ligands. Instead of docking a large ligand to a target protein in one single step as done in the standard protocol, our protocol docks the large ligand in increments. In this paper, we present three detailed examples of docking using DINC and compare the docking results with those obtained using AutoDocks standard protocol. We summarize the docking results from an extended docking study that was done on 73 protein-ligand complexes comprised of large ligands. We demonstrate not only that DINC is up to 2 orders of magnitude ...
TGF-β Ligands Structure Mature and active TGF-β ligands are formed by much larger precursor molecules. The active precursors include two of the carboxy-terminal mature domains in either homo- or heterodimer conformations. The amino-terminal signal p..
While human and mouse genetics consistently have unveiled various physiological roles of members of the pGC family, overall the mode of ligand‐dependent as well as ligand‐independent activation of these transmembrane enzymes leading to intracellular cGMP synthesis remains enigmatic. The intracellular region of pGCs consists of a juxtamembranous protein kinase-homology domain, an amphipathic α‐helical or hinge region, and the C‐terminal cyclase catalytic domain (Fig 1) (reviewed by Potter, 2011). The hinge region is involved in higher order oligomerization. Hence, although pGCs contain a single cyclase site per polypeptide chain, receptor dimerization is essential for the activation of this cGMP‐synthesizing domain (Potter, 2011). The crystal structures of the extracellular domain of GC‐A, in complex with atrial natriuretic peptide, or in absence of the ligand, suggested that hormone binding induces a rotation of the juxtamembrane domains, which is transmitted across the ...
The use of surrogates either as native orthologous proteins or as optimized chimeras, which can be readily crystallized and soaked with small molecules, has been validated by its success in other fields, particularly in guiding kinase inhibitor development (Ikuta et al., 2001; Breitenlechner et al., 2004). One should bear in mind, however, that the surrogate approach has its limitations, and local structural differences may have considerable effect on ligand binding (Davies et al., 2007). HIV-1 and PFV INs are fully orthologous, with identical canonical domain folds and stoichiometry. Fortuitously, all intasome atoms (protein, DNA, metal ions) that are in contact with the soaked INSTI molecules are invariant between HIV-1 and PFV (Hare et al., 2010a). Thus, we expect that structural differences between HIV-1 and PFV intasomes that are directly relevant to INSTI binding will be small. An unbiased test of this idea can be made by comparing the active sites in isolated catalytic core domains from ...
Recently, N,N-trans Re(O)(LN-O)2X (LN-O = monoanionic N-O chelates; X = Cl or Br prior to being replaced by solvents or alkoxides) complexes have been found to be superior to the corresponding N,N-cis isomers in the catalytic reduction of perchlorate via oxygen atom transfer. However, reported methods for Re(O)(LN-O)2X synthesis often yield only the N,N-cis complex or a mixture of trans and cis isomers. This study reports a geometry-inspired ligand design rationale that selectively yields N,N-trans Re(O)(LN-O)2Cl complexes. Analysis of the crystal structures revealed that the dihedral angles (DAs) between the two LN-O ligands of N,N-cis Re(O)(LN-O)2Cl complexes are less than 90°, whereas the DAs in most N,N-trans complexes are greater than 90°. Variably sized alkyl groups (−Me, −CH2Ph, and −CH2Cy) were then introduced to the 2-(2′-hydroxyphenyl)-2-oxazoline (Hhoz) ligand to increase steric hindrance in the N,N-cis structure, and it was found that substituents as small as −Me ...
In the case of the CaM-CaMKK complex, we obtained a set of desired near-native decoys with lowest interaction energy (Figure 3) and high Tc-IFPs (Figure 4). These results are explained by the structure of the CaM-CaMKK complex, which is different from those of the CaM-CNG and CaM-PMCA complexes. The globular cognate structure of CaM in the CaM-CaMKK complex differed only slightly from that of the CaM-CNG complex, indicating that the cavity of the CaM-CaMKK complex is narrower than that of the CaM-CNG complex, as shown in Figure 2. In contrast to the simple alpha helical structure of the CNG and PMCA ligand peptides, the CaMKK ligand peptide has an additional loop region in the C-terminal end. These structural features of the ligand have contributed in obtaining a set of near-native decoys for the CaM-CaMKK complex. In context with the shape of the ligand peptide, it is noteworthy that we found CaM-CNG b-decoys in which the CNG was bound to the CaM cavity in an inverse manner as compared to the ...
A soluble factor produced by HTU-34 cells is responsible for αvβ3 ligand-binding activity and recruitment to FCs. (A) Adhesion assay. Treatment of HTU-34 cel
Hi, When you say wrong postion, what does it mean? are the 2 ligands you are trying to refine being pushed away from each other? If that is the case first thing I would check is the ALTLOC comlumn of their pdb file entries. Make sure one is ALTLOC A and the other ALTLOC B. I have refined with ligands in four different positions before using phenix before and got satisfactory results... Hope this helps, -- Yuri Pompeu ...
The fact that over 30% of current pharmaceuticals target heptahelical G protein-coupled receptors (GPCRs) attests to their tractability as drug targets. While GPCR drug development has traditionally focused on conventional agonists and antagonists, the growing appreciation that GPCRs mediate physiologically relevant effects via both G protein and non-G protein effectors has prompted the search for ligands that can bias downstream signaling in favor of one or the other process. Biased ligands are novel entities with distinct signaling profiles dictated by ligand structure, and the potential prospect of biased ligands as better drugs has been pleonastically proclaimed. Indeed, preclinical proof-of-concept studies have demonstrated that both G protein and arrestin pathway-selective ligands can promote beneficial effects in vivo while simultaneously antagonizing deleterious ones. But along with opportunity comes added complexity and new challenges for drug discovery. If ligands can be biased, then ...
Carroll, F., Blough, B., Mascarella, S., Xu, H., Goodman, C. B., & Rothman, R. B. (1993). Synthesis and Ligand Binding at PCP Sites 1 and 2 for Hexahydro-2-substituted-1-methylindeno[1,2-b]pyrroles. Medicinal Chemistry Research, 3, 178 ...
The Rho GTPases are known regulators of the actin cytoskeleton and affect multiple cellular activities including cell morphology, polarity, migration, proliferation and apoptosis, phagocytosis, cytokinesis, adhesion, vesicular transport, transcription, and neurite extension and retraction. Like DOCK2, DOCK8 is likely to regulate the activity of GTPases and thus be involved in cytoskeletal changes associated with various cellular processes. DOCK8 is proposed to serve as an effector downstream of CD19 and PI3K to promote G protein signaling events critical for integrin polarization at the synapse and for the survival of marginal zone B cells and germinal center (GC) B cells. During a T cell-dependent humoral immune response, CD4+ T helper cell subsets including TFH, Th1 and Th2 cells migrate to the T cell/B cell borders in secondary lymphoid organs, and interact with cognate antigen-specific B cells through the pairing of T cell and B cell surface ligands and receptors such as CD40 with its ligand ...
Flt3-ligand (FMS related tyrosine kinase 3 ligand, flk-2 ligand) is involved in proliferation and differentiation of early hematopoietic cells. Flt3-ligand synergizes with other CSFs and interleukins to induce proliferation of early hematopoietic cells but does not stimulate growth or differentiation alone. Flt3-ligand binds to cells expressing the tyrosine kinase receptor Flt3. Multiple isoforms of Flt3 ligand have been identified but the predominant biologically active isoform is a transmembrane protein which can be proteolytically cleaved to generate a biologically active soluble form. ...
Low-affinity ligands can be efficiently optimized into high-affinity drug leads by structure based drug design when atomic-resolution structural information on the protein/ligand complexes is availabl
The problem with method #1 is that it is very labor intensive, and that any compound proposed may be difficult and/or expensive to acquire. The problem with approach #2 is that the compounds may still be difficult to acquire, although there are strategies to overcome this limitation. It can also be, relatively speaking, slow. The third approach, docking, is the one taken by DOCK and its graphical user interface, DOCK Blaster. It is particularly pragmatic when used to screen a database of compounds that can be acquired rapidly, such as those in ZINC, because the time from hypothesis to experimental test can be very short, and the project can progress rapidly. ...
Serotonin receptors (5-HTRs), especially the 5-HT1A subtype, have been the subject of intensive research for the past decade, due to their function in human physiology. Several structurally different classes of ligands are known to bind to the 5-HT1A receptor, but arylpiperazine derivatives are among the most important ligands. In the work, docking analyses were used to explain the binding affinities of a series of ligands with different N-1 substituent. All ligands had in common the arylpiperazine structure, while the N-1 subsistent was modified to investigate the influence of ligand structure on its binding affinity. The shape and size, as well as the rigidity of the subsistents were altered to investigate the possible effects on the formation of the receptor - ligand complex ...
Ligand binding affinities at G-protein coupled receptors (GPCRs) have historically been determined using a radioligand that competes for receptor binding sites against an unlabeled drug-like compound. But the potential hazards of open-source radioisotope handling, and the environmental impact of radioisotope disposal, make this a less desirable and costly technology. Therefore, new fluorescent based alternatives have been developed to replace radioligands.
Aspartate mutation distinguishes ETA but not ETB receptor subtype-selective ligand binding while abolishing phospholipase C activation in both receptors.: The e
Photoaffinity cross‐linking is a rapidly developing technology for studying biomolecular interactions, including protein ligand‐receptor binding
One of the major challenges in the field of system biology is to understand the interaction between a wide range of proteins and ligands. In the past, methods have been developed for predicting binding sites in a protein for a limited number of ligands.. ...
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Soluble ligands have growing interest as targets and constitute 10% of novel targets in clinical trials. Photograph: Matton Soluble ligands have...
Supplementary Materialscancers-12-01427-s001. we show that RL2 is usually targeted to mitochondria after internalization into the cells, where it can also be found in the dimeric form. The importance of TOM70 and RL2 conversation in RL2-induced reduction in ATP levels was validated by siRNA-induced downregulation of CEP33779 TOM70, resulting in the partial rescue of ATP production. Taken together, this study demonstrates that RL2CTOM70 conversation plays a key role in RL2-mediated cell death and targeting this pathway may provide new therapeutic options for treating breast malignancy. 0.05), ** (significant; 0.01), *** (significant; 0.005), **** (significant; 0.001). You will find two ways of apoptosis induction: extrinsic and intrinsic. The extrinsic apoptotic signaling is usually brought on by ligand binding to the death receptors (DRs), e.g., CD95 (APO-1/Fas) [13,14] CEP33779 or TRAIL-R1/2 [15]. The specific ligand binding to the receptor results in formation of the death inducing signaling ...
Structural and Dynamical Insight into PPARγ Antagonism: In silico Study of the Ligand-Receptor Interactions of non-Covalent Antagonists
ParDOCK is an all-atom energy based Monte Carlo protein ligand docking, implemented in a fully automated, parallel processing mode which predicts the binding mode of the ligand in receptor target site
A method is disclosed for coupling a ligand within a porous support. The method involves mixing ligand and porous support under conditions sufficient to suppress coupling conditions of the ligand to the porous support while enhancing the relative rate of diffusion, to the rate of reaction, of the ligand into and within the porous support, and then altering the conditions to enhance rapid coupling of the ligand within the porous support. The alteration from diffusion conditions to coupling conditions involves a change in the reaction solution of pH, ionic strength, temperature, coupling competitor, such that a relatively lower Thiele Modulus during diffusion conditions changes to a relatively higher Thiele Modulus during coupling conditions. Derivatized porous supports produced according to the method are also disclosed. The derivatized porous support has enhanced functional efficiency. Derivatized porous supports prepared from azlactone-functional porous supports are also disclosed ...
TFA Salt. Storage:. Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.. Note:. This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.. Documents:. MSDS ...
Users can interactively analyze protein-small ligand binding modes with statistically determined interaction patterns rather than relying on a priori knowledge of the users.
Bishwa I am using Phenix 1.0-1069 for refinement and coot 0.7-pre-1 for , visualization , and rebuilding. I used SMILES in coot to build the ligand and then merged , them , with PDB.I had to do this as a separate step for both chains and the .cif , file , so produced was not accepted for refinement. , Why? Can you send me the files directly? , , I used readyset to obtain the restrains for refinement using .pdb file, , even , though my refinement works, when i try to run real build refine in coot I , get , this error message: , It would be better to generate the restraints using the SMILES in eLBOW and then pass the restraints file to ReadySet!. Send me the file and we can fix them Nigel NB. Any files sent to me will be held in strictest confidence. , , Failed to match (to the dictionary) the following model atom names: , HB3 , O6 C10 C11 C12 O7 C13 O5 C8 C9 ...... , That would cause exploding atoms, so the refinement didnt start. , , Could someone help me with fixing this ...
Reactome is pathway database which provides intuitive bioinformatics tools for the visualisation, interpretation and analysis of pathway knowledge.
Reactome is pathway database which provides intuitive bioinformatics tools for the visualisation, interpretation and analysis of pathway knowledge.
... tripodal ligand topologically similar to the more common Tp ligands, but the two classes of ligands differ in several ways. ... They are examples of scorpionate ligands. Various ligands in this family are known, differing in what substituents are on the ... The TmR anion simulates the environment provided by three facial thiolate ligands but without the 3- charge of a facial ... In coordination chemistry, Tm is an abbreviation for anionic tridentate ligand based on three imidazole-2-thione groups bonded ...
Ligands can also influence the chemoselectivity of the catalyst. The Josiphos ligands, often called privileged ligands, are ... Xyliphos ligand The ligands are also used in non-enantioselective reactions. They have been good ligands in Pd-catalyzed ... Josiphos ligands were developed in the 1990s by Antonio Togni in studies on ferrocenyl ligands previously discovered by T. ... Diphosphine ligands were prepared with secondary phosphines, they are today known as Josiphos ligands family, which gets the ...
... , also known as phosphorane iminato ligands, are any of a class of organic compounds of the general ... These dimeric complexes yield different M-N bond lengths depending on the ligands present in the rest of the ligand sphere of M ... The terminally bound bent ligands are primarily commonly have M-N-P bond angles ranging from 120-150°. Both the M-N and N-P ... By varying the R groups on P, a variety of ligands with different electronic and steric properties can be produced, and due to ...
... are phosphine ligands that are used in homogeneous catalysis. They have proved useful in ... Reported in 2015, this ligand Coupling reaction Organometallic chemistry Ligand Surry, David S.; Buchwald, Stephen L. (2011). " ... This ligand has been utilized in multiple reactions including the amination of a range of aryl halides and triflates as well as ... Complexes of this ligand also catalyze a wide array of reactions, including the arylation of ketones and esters, borylation of ...
In the area of organometallic chemistry, a bulky cyclopentadienyl ligand is jargon for a ligand of the type C 5H 5−nR− n where ... These large ligands stabilize highly unsaturated derivatives such as (C5H2tBu3)2Fe2N2. The (tert-butyl)cyclopentadiene is ... Because they cannot closely approach the metal, these bulky ligands stabilize high spin complexes, such as (C5H2tBu3)2Fe2I2. ... Illustrative of the unusual complexes made possible with these bulky ligands is molecular iron nitrido complex (tBu3C5H2)2Fe2N2 ...
... are a subset of chiral ligands. Chiral ligands, including C2-symmetric ligands, combine with metals or ... This ligand was used in the industrial production of L-DOPA. Some classes of C2-symmetric ligands are called privileged ligands ... C2-symmetric diene ligand. Both bi- and tridentate bis(oxazoline) ligands are used in organic synthesis Both enantiomers of ... Ligands and Complexes The C2-symmetric diphosphine DIOP is historically significant. DuPhos ligands are a class of C2-symmetric ...
The primary ligands for the co-receptors GFRα1, GFRα2, GFRα3, and GFRα4 are GDNF, NRTN, ARTN, and PSPN, respectively. Upon ... However, natural GDNF ligands are of a limited clinical use. As positively charged polypeptides GFLs are unable to penetrate ... GDNF+Family+Ligands at the US National Library of Medicine Medical Subject Headings (MeSH) (TGFβ domain, Protein families, ... The GDNF family of ligands (GFL) consists of four neurotrophic factors: glial cell line-derived neurotrophic factor (GDNF), ...
Bridging carbonyl Crystal field theory DNA binding ligand Inorganic chemistry Josiphos ligands Ligand dependent pathway Ligand ... A ligand exchange (also ligand substitution) is a type of chemical reaction in which a ligand in a compound is replaced by ... Example is alkoxy ligands( which is regularly known as X ligand too). L ligands are derived from charge-neutral precursors and ... Look up ligand in Wiktionary, the free dictionary. Wikimedia Commons has media related to Ligands. See the modeling of ligand- ...
In addition to shape, tetradentate ligands can be classified by the ligating atoms on the ligand. For linear ligands the order ... Such a ligand bound to a metal in tetrahedral coordination can only connect in one way, though if the ligand is unsymmetrical ... Tetradentate ligands are common in nature in the form of chlorophyll, which has a core ligand called chlorin, and heme, which ... Ligands are also characterized by charge. Tetradentate ligands can be neutral so that the charge of the whole complex is the ...
A tridentate ligand (or terdentate ligand) is a ligand that has three atoms that can function as acceptor atoms in a ... with two atoms of the ligand opposite each other. Fac tridentate ligands are termed scorpionate ligands, especially in ... Two tridentate ligands may form a complex with such an atom. There are two possible arrangements for such a complex: fac where ... If the tridentate ligand is not symmetrical, then in the fac complexes in octahedral coordination there are three possible ...
The tropocoronand ligand (H2TC-m,n) is a macrocyclic ligand in which two aminotroponiminate rings are connected to one another ... Tropocoronand ligands (TC-m,n) 2− are known for a range of methylene bridges, m and n, in the arms connecting the two ... 5 ligand adopts a larger dihedral angle for the Co2+ ion, likely resulting due to its greater preference for tetrahedral over ... where the iron retains the nitrosyl and the nitrite becomes bound to the ligand. Seichi Imajo and Koji Nakanishi. J. Am. Chem. ...
Fas forms the death-inducing signaling complex (DISC) upon ligand binding. Membrane-anchored Fas ligand trimer on the surface ... Fas ligand (FasL or CD95L or CD178) is a type-II transmembrane protein that belongs to the tumor necrosis factor (TNF) family. ... Fas ligand/receptor interactions play an important role in the regulation of the immune system and the progression of cancer. ... Fas ligand has been shown to interact with: CASP8, EZR, FADD, FNBP1, FYN, FAS, Grb2, PACSIN2, and TNFRSF6B. FAF1 GRCh38: ...
The name "salen ligands" is used for tetradentate ligands which have similar structures. For example, in salpn there is a ... Chiral ligands may be used in asymmetric synthesis reactions, such as the Jacobsen epoxidation: A class of tetradentate ligands ... The salan and salalen ligands are similar in structure to salen ligands, but have one or two saturated nitrogen-aryl bonds ( ... which are structurally related to the classical salen ligand, primarily bis-Schiff bases. Salen ligands are notable for ...
"Monodesmic" ligands (μόνος: single, δεσμός: binding) are ligands that bind a single protein chain, while "polydesmic" ligands ( ... High-affinity ligand binding implies that a relatively low concentration of a ligand is adequate to maximally occupy a ligand- ... In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The ... Ligand efficacy refers to the ability of the ligand to produce a biological response upon binding to the target receptor and ...
A hexadentate ligand in coordination chemistry is a ligand that combines with a central metal atom with six bonds. One example ... A commercially important hexadentate ligand is EDTA. The denticity of hexadentate ligands is often denoted with the prefix κ6. ... v t e (Articles with short description, Short description matches Wikidata, Ligands, Hexadentate ligands, All stub articles, ... Sharrad, Clint A.; Lüthi, Stefan R.; Gahan, Lawrence R. (2003). "Embracing ligands. A synthetic strategy towards new nitrogen- ...
The Kläui ligand is the anion {(C5H5)Co[(CH3O)2PO]3}−. The ligand, popularized by Wolfgang Kläui, binds metals and metalloids ... Related tridentate and tripodal anionic ligands include trispyrazolylborates. The ligand is derived from the cationic complex ... Using other phosphites and other cyclopentadienyl ligands, a large variety of derivatives are possible. The parent acid {(C5H5) ...
These ligands are sometimes referred to as ancillary ligands. Several different classes of ligand exist that can be considered ... Instead, spectator ligands (vs "actor ligands") occupy coordination sites. Spectator ligands tend to be of polydentate, such ... In coordination chemistry, a spectator ligand is a ligand that does not participate in chemical reactions of the complex. ... ethane ligands (dppe). Varying the substituents on the spectator ligands greatly influences the solubility, stability, ...
The ligands for this transformation require generating a chiral center on the amine portion of the ligand. These ligands afford ... A phosphoramidite ligand is any phosphorus-based ligand with the general formula P(OR1)(OR2)(NRR'). Chiral versions of these ... It is worth noting that the ligand shown (Figure 4.) is the only ligand known to afford greater than 90% enantioslectivity for ... This paradigm shift using monodentate phosphine ligands challenged the belief that a tight metal-ligand complex is necessary ...
As in the case of salen compound, the actual ligand is usually the conjugate base salpn2-, the divalent anion that result from ... Salpn is the common name for a chelating ligand, properly called N,N′-bis(salicylidene)-1,2-propanediamine, used as a motor oil ... can be described as the salen ligand with a methyl group attached to the ethylene bridge that links the two nitrogen atoms. ...
Optimer ligands are being explored by many partners as potential affinity ligands for use in bioprocessing and as critical ... Optimer ligands form secondary and tertiary structures with compatible internal base-pairing at specific portions of the ligand ... Optimer ligands are short synthetic oligonucleotide molecules composed of DNA or RNA that bind to a specific target molecule. ... Optimer ligands are composed of single-stranded DNA or RNA polymers. These nucleic acid molecules can exhibit cognate base- ...
"Ligand to pay $12.2 million to settle lawsuits". The San Diego Union-Tribune. Retrieved 2018-09-12. "Ligand Announces Recently ... "Ligand loses its listing on Nasdaq". The San Diego Union-Tribune. Retrieved 2018-09-12. "Ligand Announces SEC Investigation". ... LGND)". Ligand. Retrieved 2018-09-12. Bigelow, Bruce (March 25, 2011). "San Diego's Ligand Takes Advantage of the Great ... "Ligand Pharmaceuticals facing securities class action". Battea Class Action Services. 2016-12-28. Retrieved 2018-09-12. "Ligand ...
Some Macrocyclic Ligands and Their Complexes The silver complex of a thia-crown ether [Ag(18-ane-S6)]2+ Crystal structure of a ... Macrocyclic ligands exhibit high affinity for metal ions. Porphyrins and phthalocyanines have long been recognized as potent ... Macrocyclic ligands occur in many cofactors in proteins and enzymes. Of particular interest are tetraazamacrocycles. Heme, the ... The high affinity of macrocyclic ligands is thought to be a combination of the entropic effect seen in the chelate effect, ...
In chemistry, bis(oxazoline) ligands (often abbreviated BOX ligands) are a class of privileged chiral ligands containing two ... ligands are used in asymmetric catalysis. These ligands are examples of C2-symmetric ligands. The synthesis of oxazoline rings ... These ligands were used in the hydrosilylation of ketones; achieving ee's of up to 93% The first BOX ligands were reported a ... ligands". Journal of Organometallic Chemistry. 603 (1): 6-12. doi:10.1016/S0022-328X(00)00024-3. (Ligands, Oxazolines). ...
In 2007 Inte:Ligand was the recipient of the NÖ Innovation prize (Innovationpreis) for the development of the simulation ... Inte:Ligand was founded in Maria Enzersdorf, Lower Austria (Niederösterreich) in 2003. They established the company ... LigandScout Essential, is a scientific software program for de novo molecule design, to derive structure-based and ligand-based ... LigandScout Expert KNIME Extensions provide more than 45 Inte:Ligand scientific algorithms wrapped into KNIME extensions to be ...
A Z-ligand is usually accompanied by an L-ligand, as the presence of the L-ligand adds stability to the complex. As the ... if one Z-ligand is accompanied by one L type ligand, it can be written as a complex containing two X type ligands; i.e. MLZ ... and L-type ligands, which form a bond with the ligand donating two electrons. Typically, these Z-type ligands are Lewis acids, ... a Z-type ligand refers to a ligand that accepts two electrons from the metal center. This is in contrast to X-type ligands, ...
... ligand lipophilicity index (LLEAT) ligand efficiency dependent lipophilicity (LELP), fit quality scaled ligand efficiency (LE_ ... Ligand efficiency is a measurement of the binding energy per atom of a ligand to its binding partner, such as a receptor or ... Mathematically, ligand efficiency (LE) can be defined as the ratio of Gibbs free energy (ΔG) to the number of non-hydrogen ... Ligand efficiency is used in drug discovery research programs to assist in narrowing focus to lead compounds with optimal ...
... ligand isomerism is a type of structural isomerism in coordination complexes which arises from the presence of ligands which ... 1,2-Diaminopropane and 1,3-Diaminopropane are the examples that each feature a different isomer would be ligand isomers. v t e ...
Ligands that are not bridging are called terminal ligands. Virtually all ligands are known to bridge, with the exception of ... In coordination chemistry, a bridging ligand is a ligand that connects two or more atoms, usually metal ions. The ligand may be ... In triiron dodecarbonyl, two CO ligands are bridging and ten are terminal ligands. The terminal and bridging CO ligands ... Common bridging ligands include most of the common anions. Many simple organic ligands form strong bridges between metal ...
Other C2-symmetric ligands derived from trans-1,2-diaminocyclohexane (DACH) have been developed, such as the (R,R)-DACH- ... naphthyl ligand derived from 2-diphenylphosphino-1-naphthalenecarboxylic acid. Related bidentate phosphine-containing ligands ... Sigma-Aldrich: Trost Ligands Trost Research Group v t e (Articles without EBI source, Articles without KEGG source, Articles ... The Trost ligand is a diphosphine used in the palladium-catalyzed Trost asymmetric allylic alkylation. ...
Ligand may refer to: Ligand, an atom, ion, or functional group that donates one or more of its electrons through a coordinate ... in host-guest chemistry Ligand-gated ion channel This disambiguation page lists articles associated with the title Ligand. If ... covalent bond to one or more central atoms or ions Ligand (biochemistry), a substance that binds to a protein a 'guest' ...
This page was last modified on 14 August 2009, at 20:42 ...
Estrogen Receptor Alpha Ligand Binding Domain in Complex with Lasofoxifene ... Estrogen Receptor Alpha Ligand Binding Domain in Complex with Lasofoxifene. *PDB DOI: 10.2210/pdb6VJD/pdb ... 3D View: Structure , 1D-3D View , Electron Density , Validation Report , Ligand Interaction ... 3D View: Structure , 1D-3D View , Electron Density , Validation Report , Ligand Interaction ...
... Nat Rev Drug Discov. 2004 Oct;3(10):845-52. doi: 10.1038/nrd1522. ... which have brought us closer to therapeutic applications of kinin receptor ligands in various indications. The potential of ...
"Gene Family: Ligand gated ion channels". HUGO Gene Nomenclature Committee.. *^ "ligand-gated channel" at Dorlands Medical ... Ligand-gated ion channels (LICs, LGIC), also commonly referred to as ionotropic receptors, are a group of transmembrane ion- ... Ligand-gated ion channels are likely to be the major site at which anaesthetic agents and ethanol have their effects, although ... When ligands bind to the receptor, the ion channel portion of the receptor opens, allowing ions to pass across the cell ...
FAD is a Ligand Of Interest in 1QLU designated by the RCSB. ...
Evaluation of serum levels and significance of soluble CD40 ligand in screening patients with hepatitis C virus-related ...
... the complexes are labile and ligand exchange is complete within mixing time in CDCN solutions to give libraries of heteroleptic ... can be amplified by specific reaction of the fac stereoisomer with a triamine to give a new hexadentate ligand, although other ... the complexes are labile and ligand exchange is complete within mixing time in CD3CN solutions to give libraries of ... assembly of combinatorial libraries-principles and establishment of equilibrated libraries with oligopyridine ligands B. Brisig ...
Chiral Quest Ligands Kit I; find Sigma-Aldrich-687464 MSDS, related peer-reviewed papers, technical documents, similar products ...
5 Common ligands *5.1 Examples of common ligands (by field strength). *5.2 Other generally encountered ligands (in alphabetical ... In complexes of non-innocent ligands, the ligand is bonded to metals via conventional bonds, but the ligand is also redox- ... strong field ligands, by definition, increase Δo more than weak field ligands. Ligands can now be sorted according to the ... Common ligands. See Complex (chemistry).. Virtually every molecule and every ion can serve as a ligand for (or "coordinate to ...
... ligands, small molecules and monomers) referred in PDB entries and maintained by the wwPDB ...
Ligand Pharmacueticals, sponsor of - The meeting place for vaccine professionals from industry, academia, non-profit ...
NKG2D ligand 3 (244 aa, ~28 kDa) is encoded by the human ULBP3 gene. This protein is involved in activation of multiple ... NKG2D Ligand 3. Known as: Alcan-Gamma, Retinoic Acid Early Transcript 1N, UL16-Binding Protein 3 ... NKG2D ligand 3 (244 aa, ~28 kDa) is encoded by the human ULBP3 gene. This protein is involved in activation of multiple ...
However, gain-of-function studies using RSPO ligands and a new non-lipidated Wnt analogue reveal that these ligands have ... Palmitoylated Wnt ligands engage cell-surface frizzled (FZD) receptors and LRP5 and LRP6 co-receptors, enabling β-catenin ... Here we identify the functional roles of Wnt and RSPO ligands in the intestinal crypt stem-cell niche. We show that the default ... Wnt ligands interact with FZD and Lrp5/6-type receptors to influence diverse developmental, homeostatic and pathologic ...
Evidence That the Density of Self Peptide-MHC Ligands Regulates T-Cell Receptor Signaling. Nadia Anikeeva et al.. PLOS One ... Noncognate or self peptide-MHC (pMHC) ligands productively interact with T-cell receptor (TCR) and are always in a large access ... Evidence that the Density of Self Peptide-MHC Ligands Regulates T-Cell Receptor Signaling. Nadia Anikeeva1, Dimitry Gakamsky2, ... We assembled soluble cognate and noncognate pMHC class I (pMHC-I) ligands at designated ratios on various scaffolds into ...
C-X-C motif chemokine ligand 10provided by HGNC. Primary source. HGNC:HGNC:10637 See related. Ensembl:ENSG00000169245 MIM: ... HIV-1 and the viral protein Tat modulate the expression of chemokine (C-X-C motif) ligand 10 (CXCL10; IP-10) in immature ... This antimicrobial gene encodes a chemokine of the CXC subfamily and ligand for the receptor CXCR3. Binding of this protein to ... CXCL10 C-X-C motif chemokine ligand 10 [ Homo sapiens (human) ] Gene ID: 3627, updated on 30-Nov-2022 ...
... Author(s). Cordero, Etchell Ann, 1969- ...
phenix.reel ligand.cif ligand.pdb and to use the --overlay option to force it in the case of slightly different ligand details ... Edit the geometry restraints of a ligand using a Graphical User Interface (GUI) including a 3D view of the ligand and a tabular ... chem option so load the cartesian coordinates and atom names of a certain ligand. ...
... lymphaticCongenitalSkinEndocrineAnimalWoundsKinasesProteasesPhosphatasesNuclear receptorsOthersPPI modulatorsReceptors ligands ...
Chromium complexes of ligands of the type Ar2PN(Me)PAr2 (Ar = ortho-methoxy-substituted aryl group), on activation with MAO, ... High activity ethylene trimerisation catalysts based on diphosphine ligands† Anthea Carter,a Steven A. Cohen,b Neil A. Cooley,a ... based on diphosphine ligands A. Carter, S. A. Cohen, N. A. Cooley, A. Murphy, J. Scutt and D. F. Wass, Chem. Commun., 2002, 858 ... ligands. of the type Ar2PN(Me)PAr2 (Ar = ortho-methoxy-substituted aryl group), on activation. with MAO, are extremely active ...
... derivatives such as Josiphos rank amongst the most versatile and efficient ligands. ... derivatives such as Josiphos rank amongst the most versatile and efficient ligands. In this thesis, a chiral ferrocene was used ... derivatives such as Josiphos rank amongst the most versatile and efficient ligands. In this thesis, a chiral ferrocene was used ...
Roles as Enzyme Ligand. Substrate in Enzyme-catalyzed Reactions (1 result). top print hide ... Ligand 2-N-(5-L-Glutamyl)L-lysine. Please wait a moment until all data is loaded. This message will disappear when all data is ...
Unfortunately Tocriscreen GABA/glycine Ligands (Cat. No. 1720) has been withdrawn from sale for commercial reasons. ... Keywords: Tocriscreen GABA/glycine Ligands, Tocriscreen GABA/glycine Ligands supplier, , Tocris Bioscience ... Have you used TocriscreenTM GABA/Glycine Ligands?. Submit a review and receive an Amazon gift card.. $50/€35/£30/$50CAN/¥300 ... Reviews for TocriscreenTM GABA/Glycine Ligands. There are currently no reviews for this product. Be the first to review ...
Other ligands, Catalysis/inorganics at LGC Standards. Over 100,000 Products Online, Explore our Extensive Range and Purchase ...
Peroxisome proliferator-activated receptor γ ligands inhibit development of atherosclerosis in LDL receptor-deficient mice. ... Peroxisome proliferator-activated receptor γ ligands inhibit development of atherosclerosis in LDL receptor-deficient mice. ... PPARγ agonists may exert antiatherogenic effects in diabetic patients and provide impetus for efforts to develop PPARγ ligands ...
Biologically active small molecules are typically discovered in designsynthesis-purify-test cycles. These workflows are underpinned by a remarkably narrow toolkit of robust and reliable chemical transformations and place equal resources on all molecules regardless of their biological function. Activity-directed synthesis harnesses the potential of chemical reactions that can form more than one possible product and allows resources to be focussed on small molecules with biological activity. The discovery of small molecules through activity-directed synthesis emerge in parallel to their associated synthetic routes. A feedback mechanism can serve to optimise the range of bioactive products, analogous to the emergence of natural products through the evolution of biosynthetic pathways found in nature. The implementation of fragments as substrates in activity-directed synthesis has the potential to enable their optimisation into lead-like compounds without the target molecule being predefined, ...
wwPDB/CCDC/D3R Ligand Validation Workshop. Confirmed Participants. table.data { margin-left:20px; } table.data td { padding:4px ...
... is a glycosylated 133 amino acid protein corresponding to the extracellular TNF homologous ...
YPhos ligands tend to be surprisingly stable when complexed with a metal owing to additional interactions between the ligand ... The progress in ligand design that has been facilitated by Umicore PMCs academic partners are directly relevant to industrial ... The low amounts of the catalyst required, enabled by both the YPhos and PAd3 ligands, means less palladium is required. This ... The general design of a YPhos ligand. Instead of an aryl or alkyl group, the phosphine contains an ylide group (coloured blue). ...
Improved Technologies and Ligands for Non-invasive Brain Imaging (R41/R42) RFA-DA-17-010. NIDA ... For example, there is currently no ligand available for non-invasive imaging of latent HIV in the human brain, which would be ... The development of ligands targeting specific glial cells (e.g., oligodendrocytes, astrocytes, microglia) or markers for state ... More research is needed to improve the ability of existing imaging ligands and technologies (e.g., analytical programs) for non ...
  • This review discusses recent progress in our understanding of the genetics, molecular biology and pathophysiology of kinins and their receptors, as well as developments in medicinal chemistry, which have brought us closer to therapeutic applications of kinin receptor ligands in various indications. (nih.gov)
  • When ligands bind to the receptor, the ion channel portion of the receptor opens, allowing ions to pass across the cell membrane . (wikipedia.org)
  • These receptor proteins are typically composed of at least two different domains: a transmembrane domain which includes the ion pore, and an extracellular domain which includes the ligand binding location (an allosteric binding site). (wikipedia.org)
  • [4] [5] A binding site in the extracellular N-terminal ligand-binding domain gives them receptor specificity for (1) acetylcholine (AcCh), (2) serotonin, (3) glycine, (4) glutamate and (5) γ-aminobutyric acid (GABA) in vertebrates. (wikipedia.org)
  • The prototypic ligand-gated ion channel is the nicotinic acetylcholine receptor . (wikipedia.org)
  • Wnt proteins are unable to induce Lgr5 + ISC self-renewal, but instead confer a basal competency by maintaining RSPO receptor expression that enables RSPO ligands to actively drive and specify the extent of stem-cell expansion. (nature.com)
  • Noncognate or self peptide-MHC (pMHC) ligands productively interact with T-cell receptor (TCR) and are always in a large access over the cognate pMHC on the surface of antigen presenting cells. (edinst.com)
  • Our data demonstrate that the density of self pMHC-I proteins promotes their interaction with CD8 co-receptor, which plays a critical role in recognition of a small number of cognate pMHC-I ligands. (edinst.com)
  • This antimicrobial gene encodes a chemokine of the CXC subfamily and ligand for the receptor CXCR3. (nih.gov)
  • CD27 Ligand expression is induced by antigen-receptor activation in B cells. (rndsystems.com)
  • Bone morphogenetic protein (BMP)9 and BMP10 are high affinity ligands for activin receptor-like kinase 1 (ALK1), a type I BMP receptor mainly expressed on vascular endothelial cells (ECs). (portlandpress.com)
  • Although there is considerable variability in the physiologic ligands responsible for receptor activation, all receptors in this group interact with trimeric, guanine nucleotide-binding proteins to initiate signaling cascades in the cell cytosol. (jcvi.org)
  • Because of the strong homology that exists within this family of receptor proteins, the results of this work are applicable to other systems and, therefore, can help to establish a more complete understanding of ligand-receptor interactions. (jcvi.org)
  • In an attempt to determine which of these receptor interactions are involved in the in vivo effects of ibogaine, ligands for sigma, PCP, and opiate receptors were assessed for their ability to substitute for or to antagonize the ibogaine-induced discriminative stimulus (10 mg/kg I.P., 60 min presession) in Fischer-344 rats. (erowid.org)
  • Sigma receptor ligands inhibit rat tail artery contractile responses by multiple mechanisms. (aspetjournals.org)
  • The multiple functional effects of this group of putative sigma receptor ligands suggests that they have only limited utility for exploration of the potential physiological role of the sigma receptor. (aspetjournals.org)
  • Selective high affinity retinoic acid receptor alpha or beta-gamma ligands. (aspetjournals.org)
  • The methodology was used to establish the ligand requirements of human Roundabout receptor 1 (Robo1), which is involved in a number of developmental processes. (uu.nl)
  • GW-3965 is a liver X receptor ligand. (rcsb.org)
  • These ligands-glial cell line-derived neurotrophic factor (GDNF), neurturin, persephin, and artemin-also interact with one of four coreceptors in the GDNF-family receptor-alpha family. (medscape.com)
  • Cell Surface Receptor-Ligand Recognition and. (hhmi.org)
  • Ligand-receptor interaction and pathway analysis reveals novel crosstalk between cellular compartments and associates new pathways with differentiation of nephron and ureteric epithelium cell types. (lazappi.id.au)
  • Introduction: A key to understanding the biological function(s) of the aryl hydrocarbon receptor (AHR) - a xenobiotic-activated receptor - is to identify its endogenous ligand(s). (cdc.gov)
  • If these receptors are ligand-gated ion channels, a resulting conformational change opens the ion channels, which leads to a flow of ions across the cell membrane. (wikipedia.org)
  • The receptors are subdivided with respect to the type of ion that they conduct (anionic or cationic) and further into families defined by the endogenous ligand. (wikipedia.org)
  • the development of imaging ligands for visualizing changes in receptors or other brain proteins relevant to substance abuse and co-occurring psychiatric disorders (e.g., anxiety, depression), 4. (nih.gov)
  • Several genetic mutations in the genes encoding the ligands and receptors of this pathway have been reported in two cardiovascular diseases, pulmonary arterial hypertension (PAH) and hereditary haemorrhagic telangiectasia (HHT). (portlandpress.com)
  • Development of selective antagonists and subtype selective ligands for the D-myo-inositol 1,4,5-trisphosphate receptors. (europa.eu)
  • Structure and functional analysis of G protein-coupled receptors and potential diagnostic ligands. (jcvi.org)
  • To investigate the structural motifs responsible for ligand binding, we have established a model system to express heterologously human G protein-coupled receptors in a mammalian cell line. (jcvi.org)
  • This combined molecular and biochemical approach to the study of G protein-coupled receptors can pave the way for the development of isoform-specific ligands that may be used for radionuclide imaging and therapy. (jcvi.org)
  • In chemistry , a ligand is an atom , ion , or molecule that generally donates one or more of its electrons through a coordinate covalent bond to, or shares its electrons through a covalent bond with, one or more central atoms or ions. (newworldencyclopedia.org)
  • But in organic chemistry , ligands are also used to protect functional groups or to stabilize reactive compounds. (newworldencyclopedia.org)
  • Over the course of the last 70 years, cross-coupling has grown and adapted with an array of new ligands being developed allowing it to fulfil a range of new uses in synthetic chemistry. (chemistryworld.com)
  • The primary objectives of this project were to synthesize triple-stranded poly(dipyrromethene) complexes and explore the octahedral coordination chemistry of poly(dipyrromethene) ligands. (ubc.ca)
  • the complexes are labile and ligand exchange is complete within mixing time in CD 3 CN solutions to give libraries of heteroleptic complexes which have been fully characterised by one- and two-dimensional 1 H NMR spectroscopy. (rsc.org)
  • Metal ions bound to strong-field ligands follow the Aufbau principle, whereas complexes bound to weak-field ligands follow Hund's rule. (newworldencyclopedia.org)
  • Chromium complexes of ligands of the type Ar 2 PN(Me)PAr 2 (Ar = ortho -methoxy-substituted aryl group), on activation with MAO, are extremely active and selective catalysts for the trimerisation of ethylene . (rsc.org)
  • A series of bimetallic and trimetallic complexes has been prepared by N-alkylation of mononuclear half-sandwich rhodium and iridium di-NHC complexes featuring bidentate chelate ligands composed of a classical NHC and a C-azolato donor. (chemie.de)
  • Analogous to porphyrins, poly(dipyrromethene) ligands can endow their metal complexes with intense absorption bands in the visible region. (ubc.ca)
  • A series of α,α'-linked and β,β'-linked bis(dipyrromethene) ligands were synthesized and examined for the formation of triple-stranded complexes. (ubc.ca)
  • In vitro assays against three tumor cell lines (B16-F10, HCT-8 and MDA-MB-231) showed that the gold(III) complexes display remarkable antiproliferative effects on human breast adenocarcinoma cell line with influence of the co-ligands. (unesp.br)
  • The AlaSTAT Microplate Allergen-Specific IgE system is an enzyme-labeled immunometric assay, based on liquid allergen complexes, monoclonal antibodies, and separation by ligand-coated wells. (cdc.gov)
  • Ligand-labeled allergen complexes and a patient sample are pipetted into ligand-coated wells and then incubated for 1 hour. (cdc.gov)
  • Addition of a multivalent anti-ligand creates a bridge between the allergen/IgE complexes and the ligand-coated wells during the second 1-hour incubation. (cdc.gov)
  • Both POVPC-BSA and POVPC-peptide adducts were high-affinity ligands for CD36 and potent inhibitors of OxLDL binding. (eurekamag.com)
  • High affinity ligands were able to reverse a reduction in endothelial cell migration induced by Slit2-Robo1 signaling. (uu.nl)
  • This webinar showcases the features - including Visualizing Protein-Ligand Interactions - that are in the latest release of OpenEye's Orion molecular design platform. (eyesopen.com)
  • To learn more about how you can take advantage of the latest improvements in the Orion platform to make your work more successful and efficient, please view the webinar "Visualize Protein-Ligand Interactions in Latest Orion Update , " during which Matt Geballe, PhD, VP of Product at OpenEye provides an overview of the new features in Orion. (eyesopen.com)
  • N atural L igand D ata B ase - A database of protein-ligand interactions in three-dimension. (tohoku.ac.jp)
  • A modular synthetic approach was employed to prepare the target compound, and binding studies by surface plasmon resonance (SPR) confirmed it to be a high affinity ligand for Robo1. (uu.nl)
  • Industry-best custom affinity resin development from Repligen offers unparalleled ligand diversity, process development and proven success across a broad array of biomolecules. (repligen.com)
  • For other types of ligands, e.g. longer nucleotides and peptides, a manually drawn representation of the molecule may be provided. (guidetopharmacology.org)
  • The ligand in the database is a "natural ligand" generated by the knowledge of enzymatic reactions appeared in KEGG combined with a three-dimensional data of protein-analog interactions in PDB. (tohoku.ac.jp)
  • Nonbonded energy interactions are able to account for the increases of regiospecificity experimentally observed for zirconocene-based catalytic systems when the π-ligands are alkyl substituted in position 2 or 3 as well as the decrease of regiospecificity observed when the π-ligands are dimethyl substituted in positions 4 and 7. (edu.sa)
  • CD27 Ligand, also known as CD70 and TNFSF7, is a type II transmembrane glycoprotein belonging to the TNF superfamily (TNFSF). (rndsystems.com)
  • CD27 Ligand/TNFSF7 " has 28 results in Products. (rndsystems.com)
  • Combinations of anti-LFA-1, everolimus, anti-CD40 ligand, and allogeneic bone marrow induce central transplantation tolerance through hemopoietic chimerism, including protection from chronic heart allograft rejection. (novartis.com)
  • Combining anti-LFA-1 with anti-CD40 ligand (CD40L) induced high incidences and levels of stable multilineage hemopoietic chimerism comparable to chimerism achieved with anti-CD40L and everolimus (40-O-(2-hydroxyethyl)-rapamycin) under conditions where neither Ab alone was effective. (novartis.com)
  • Intermediate levels of generalization were observed with the subtype nonselective sigma ligands 3-(3-hydroxyphenyl)-N-(1-propyl)-piperidine [(+)-3-PPP] (69.0%) and 1,3-di(2-tolyl)guanidine (DTG) (73.5%) but not with the sigma1-selective agents (+)-N-allylnormetazocine [(+)-SKF 10,047] and (+)-pentazocine. (erowid.org)
  • and the two newly identified sigma ligands, N-(1-adamant-1- yl)-N'-(2-iodophenyl)guanidine and 2-amino-(3-phenyl)-3,4-dihydroquinazoline. (aspetjournals.org)
  • C-C motif chemokine ligand 2 (CCL2) is a small chemokine which belongs to the CC-type chemokine family, and has chemoattractant activity for recruitment of monocytes to sites of inflammation. (ewha.ac.kr)
  • Expert opinion: The recognition of FICZ as a potent, endogenous ligand of AHR provided a molecular link between light exposure and AHR signaling and function. (cdc.gov)
  • Dalantercept, an Fc-fusion protein of the extracellular domain of ALK1 and a ligand trap for BMP9 and BMP10, is in phase II clinical trials for anti-tumour angiogenesis. (portlandpress.com)
  • The extracellular domain interacts with one of four ligands identified to date. (medscape.com)
  • In general, ligands donate electron density to the (electron deficient) central atom-that is, they overlap between the highest occupied molecular orbital (HOMO) of the ligand with the lowest unoccupied molecular orbital (LUMO) of the central atom. (newworldencyclopedia.org)
  • From a molecular orbital theory point of view, the HOMO of the ligand should have an energy that makes overlap with the LUMO of the metal preferential. (newworldencyclopedia.org)
  • Binding of the metal with the ligands results in a set of molecular orbitals, where the metal can be identified with a new HOMO and LUMO (the orbitals defining the properties and reactivity of the resulting complex) and a certain ordering of the five d-orbitals (which may be filled, or partially filled with electrons). (newworldencyclopedia.org)
  • This functionally non-equivalent yet cooperative interaction between Wnt and RSPO ligands establishes a molecular precedent for regulation of mammalian stem cells by distinct priming and self-renewal factors, with broad implications for precise control of tissue regeneration. (nature.com)
  • Our TLR ligands cover those pathogen-associated molecular patterns (PAMPs) and are suited for human or mouse immune cell activation. (miltenyibiotec.com)
  • We assembled soluble cognate and noncognate pMHC class I (pMHC-I) ligands at designated ratios on various scaffolds into oligomers that mimic pMHC clustering and examined how multivalency and density of the pMHCs in model clusters influences the binding to live CD8 T cells and the kinetics of TCR signaling. (edinst.com)
  • Since this time, several new phosphine ligand scaffolds have been developed, each tuned for specific properties. (chemistryworld.com)
  • In this context, synthetic retinoids that would behave as selective ligands would be invaluable for studying the respective roles of each RAR type in cultured cells, whole animals, and embryos. (aspetjournals.org)
  • A molecule of EDTA (black) forms several bonds with a central metal atom (red M) . EDTA is a chelating agent that is classified as a polydentate ligand. (newworldencyclopedia.org)
  • In a smaller number of cases, a ligand is a molecule that accepts electrons from a Lewis base. (newworldencyclopedia.org)
  • The molecule resulting from the coordination of a ligand (or an array of ligands) to a central atom is called a complex . (newworldencyclopedia.org)
  • HIV preferentially infects and replicates in cells expressing the CD4 molecule, the ligand for viral attachment and subsequent cell entry (1). (cdc.gov)
  • abstract = " A possible rationalization of the dependence of regiospecificity of propene polymerization for catalytic systems based on C 2 -symmetric ansa-zirconocenes (and hafnocenes) on the π-ligand alkyl substitutions is presented. (edu.sa)
  • From literature, I learned that the specificity is determined by the second step of the mechanism in which the ligand is covalently bound to D281 of an enzyme (see the attached picture showing the mechanism). (rosettacommons.org)
  • If so, how can I parameterize the ligand (which is covalently bound to the protein)? (rosettacommons.org)
  • Mixtures of ligands also result from incomplete or partial ligand exchange reactions wherein one that is more tightly bound replaces a weakly bound ligand. (oregonstate.edu)
  • Further, the impact of residual weakly bound ligands is not understood. (oregonstate.edu)
  • To examine the biological impacts due to weakly bound ligands within a mixed ligand shell, a series of six types of gold nanoparticles (AuNPs) were synthesized that have the same core size and possess ligand shells that are predominately either 2-mercaptoethanesulfonate (MES) or N , N , N -trimethylammoniumethanethiol (TMAT), but contain varying (small) amounts of residual triphenylphosphine (TPP). (oregonstate.edu)
  • The influence of the residual, weakly bound TPP ligands upon the biological activity of the nanoparticles (NPs) was evaluated in zebrafish embryos and subsequently in human keratinocyte cells. (oregonstate.edu)
  • The results of these studies suggest that the use of strongly bound ligands that passivate the surface of the inorganic core can prevent ROS and, therefore, yield nanoparticles with reduced biological effects. (oregonstate.edu)
  • The way the binding energy is calculated for ligand docking is the ligand is taken and moved ~500 angstroms away from the protein (far out of interaction distance) and the difference in energy between the two states (bound and unbound) are calculated. (rosettacommons.org)
  • Allergens, in a liquid format, are covalently bound to a soluble polymer/copolymer matrix, which in turn is labeled with a ligand - the same ligand used for coating the reaction wells. (cdc.gov)
  • A library comprising mer and fac isomers of [CoL 3 ] 2+ (L = 2,2′-bipyridine-5-carbaldehyde) can be amplified by specific reaction of the fac stereoisomer with a triamine to give a new hexadentate ligand, although other ligand exchange processes compete. (rsc.org)
  • Isomerization in a homoleptically coordinated cluster utilizing a mixed nitrogen- and sulfur-donating ligand is investigated as a model for ligand rearrangement processes during iron sulfur cluster biogenesis. (cuvillier.de)
  • RÉSUMÉ L'objectif de l'étude était d'évaler l'importance clinique du ligand de CD40 soluble (sCD40L) chez des patients atteints d'un carcinome hépatocellulaire (CHC) associé au virus de l'hépatite C (VHC). (who.int)
  • Methods: Proteasome inhibitors (PIs) and TNFá-Related Apoptosis Inducing Ligand (TRAIL), have emerged as promising new anti-MPM agents. (cdc.gov)
  • If instead of "-protocol abbrev2" you use "-protocol rescore" and provide it as input the file(s) with the docking output, the ligand_dock application will skip the docking step and just rescore the structures that have already been produced. (rosettacommons.org)
  • Further analysis was performed by sequential permethylation, desulfation, and pertrideuteroacetylation followed by online separation and structural analysis by MS/MS. Sequences of tetrasaccharides could be deduced from the data, and by combining the compositional and sequence data, a putative octasaccharide ligand could be proposed (GlA-GlcNS6S-IdoA-GlcNS-IdoA2S-GlcNS6S-IdoA-GlcNAc6S). (uu.nl)
  • Factors that characterize the ligands are their charge, size (bulk), and the nature of the constituent atoms. (newworldencyclopedia.org)
  • Single-crystal X-ray diffraction analysis showed that the ligand (HTriaz) is an NNO tridentate chelate via two N-atoms from the s-triazine and hydrazone moieties and one oxygen from the deprotonated phenolic OH. (jyu.fi)
  • The ligand thus acts as a Lewis base by donating electron density (in general, electron pairs) to the central atom, acting as a Lewis acid. (newworldencyclopedia.org)
  • In some cases, ligands donate only one electron from a singly occupied orbital (the donating atom in these ligands is a radical ). (newworldencyclopedia.org)
  • Some metal centers in combination with certain ligands (e.g. carbon monoxide (CO)) can be further stabilized by donating electron density back to the ligand in a process known as back-bonding . (newworldencyclopedia.org)
  • Within the coordination sphere of 10 and 12 to 16 electron LnM transition-metal complex fragments P2 to P6, P8, and P10 have been stabilized as acyclic, cyclic, and polycyclic Pn ligands. (uni-konstanz.de)
  • Each member of the series was carefully examined to determine the core size (by small-angle X-ray scattering and transmission electron microscopy) and ligand shell composition (by 1H NMR spectroscopy and X-ray photoelectron spectroscopy). (oregonstate.edu)
  • The amounts of the electron transfer from the ligand groups to Pt(II) metal center were predicted using NBO calculations. (jyu.fi)
  • However, the interchangeability, functional cooperation and relative contributions of Wnt versus RSPO ligands to in vivo canonical Wnt signalling and ISC biology remain unknown. (nature.com)
  • Click on the image to access the chemical structure search tool with the ligand pre-loaded in the structure editor. (guidetopharmacology.org)
  • This work uses synthetic [2Fe-2S] analogues to explore the role alternative ligands play in determining the reactivity of iron sulfur clusters. (cuvillier.de)
  • Many LICs are additionally modulated by allosteric ligands , by channel blockers , ions , or the membrane potential . (wikipedia.org)
  • Here we identify the functional roles of Wnt and RSPO ligands in the intestinal crypt stem-cell niche. (nature.com)
  • We have used this expression system in conjunction with an experimental strategy of site-directed mutagenesis to identify amino-acid residues that have a functional role in ligand binding. (jcvi.org)
  • These biosensors are thermodynamically stable, functional, and highly sensitive to ligands of the CaM. (bvsalud.org)
  • The ligands in a complex stabilize the central atom, and dictate the reactivity of the central atom. (newworldencyclopedia.org)
  • If the inner-sphere ligands do not balance the charge of the central atom (the oxidation number), this may be done by simple ionic bonding with another set of counter ions (the "outer-sphere" ligands). (newworldencyclopedia.org)
  • In this case, a filled, central-atom-based orbital donates density into the LUMO of the (coordinated) ligand. (newworldencyclopedia.org)
  • The Chemical Components database can also be accessed using the --chem option so load the cartesian coordinates and atom names of a certain ligand. (phenix-online.org)
  • It also allows the atom names to be assigned or copied from a partial match, so one can be consistent or do a ligand switcheroo. (rosettacommons.org)
  • I have another module, Fragmenstein , which can be used for a ligand switcheroo ( example ), but if it is a one off, it's easier to remove an atom or two in PyMol. (rosettacommons.org)
  • Moreover, I am confused how the OG1 of the enzyme can be used as an atom for the ligand. (rosettacommons.org)
  • I just picked a C-atom from the PDB that was 'centered' in the ligand conformation. (rosettacommons.org)
  • Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (bvsalud.org)
  • Go to the GPCR list to see GPCRs with which this ligand interacts. (umich.edu)
  • The complex of the metal with the inner sphere ligands is then called a complex ion (which can be either cationic or anionic). (newworldencyclopedia.org)
  • The magnitude of Δ t is smaller than for Δ o , because in a tetrahedral complex only four ligands influence the d-orbitals, whereas in an octahedral complex the d-orbitals are influenced by six ligands. (newworldencyclopedia.org)
  • The reaction of PtCl2 with s-triazine-type ligand (HTriaz) (1:1) in acetone under heating afforded a new [Pt(Triaz)Cl] complex. (jyu.fi)
  • These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. (guidetopharmacology.org)
  • They are usually pentameric with each subunit containing 4 transmembrane helices constituting the transmembrane domain, and a beta sheet sandwich type, extracellular, N terminal, ligand binding domain. (wikipedia.org)
  • Recombinant Human sOX40 Ligand is a glycosylated 133 amino acid protein corresponding to the extracellular TNF homologous domain of the full length transmembrane protein. (peprotech.com)
  • Bis(diphenylphosphino)amine ligands were supported on Merrifield's resin and tested in catalytic ethylene oligomerization reactions with a chromium source. (scielo.org.za)
  • The goal of this study was to further explore the mechanism of action by which several sigma ligand inhibit vascular contractile responses. (aspetjournals.org)
  • Each sigma ligand exhibited a distinct individual inhibitory profile with respect to preferential actions on either norepinephrine- or serotonin-induced contractions, suggesting that these ligands act by several mechanisms to inhibit contractile responses in the rat tail artery. (aspetjournals.org)
  • Potential targets for immune checkpoint inhibition are lymphocyte-activation gene 3 (LAG3) and its ligands. (aabioetica.org)
  • However, gain-of-function studies using RSPO ligands and a new non-lipidated Wnt analogue reveal that these ligands have qualitatively distinct, non-interchangeable roles in ISCs. (nature.com)
  • Visualization of a protein ligand binding site in Orion. (eyesopen.com)
  • If there's some sort of distance constraint between the protein and the ligand, that translation can cause it to blow up in energy, making it look like there's a greatly beneficial energy of binding. (rosettacommons.org)
  • I tried with some centroid start coordinates (the 'start_from' option), without tether_ligand, but it still shifted the ligand too far out of the binding pocket. (rosettacommons.org)
  • How I should modify this parameter file to ensure the O1 of the ligand (OG1 of D281 of enzyme) is connected to CG of D281 of the enzyme. (rosettacommons.org)
  • Currently there are no citations for Tocriscreen TM GABA/Glycine Ligands. (tocris.com)