Structurally related ligands. Medical search. Frequent questions

3) Mutations of Q12, A53, and Y54 of GFKAR beta indicate that these three residues are important for ligand binding (particularly L-glutamate), which is consistent with the sequence homology to bacterial periplasmic binding proteins. (aspetjournals.org)
These results are consistent with the notion that the ligand-binding domain has close structural similarities to bacterial periplasmic binding proteins. (aspetjournals.org)
Wnt-3a belongs to Wnt family of proteins that consist of structurally related genes encoding highly conserved cysteine rich secreted glycoproteins. (biolegend.com)
While fungal and mammalian pepsins are bilobal proteins with structurally related N- and C-termini, retropepsins are half as long as their fungal and mammalian counterparts. (nih.gov)
Cadherins are evolutionary related to the desmogleins which are component of intercellular desmosome junctions involved in the interaction of plaque proteins. (embl.de)
This entry represents the extracellular repeated domains found in cadherins and related proteins. (embl.de)
Analysis of virulence related gene expression and computational simulations of pivotal proteins involved in pathogenesis demonstrate that myricetin downregulates the saeR global regulator and interacts with sortase A and α-hemolysin. (nature.com)
Fibroblast Growth Factors (FGFs) comprise a family of at least eighteen structurally realted proteins that are involved in a multitude of physiological and pathological cellular processes, including cell growth, differentation, angiogenesis, wound healing and tumorgenesis. (prospecbio.com)
A greater understanding of the mechanism of transcriptional regulation by nuclear receptors has lead to the identification of multiple accessory proteins that bind to the nuclear receptors in a ligand-dependent manner. (sigmaaldrich.com)
furthermore, by analyzing chimeric proteins between Argos and the activating ligand, Spitz (a transforming growth factor-alpha-like factor), we have examined what makes one inhibitory and the other activating. (ox.ac.uk)
Members of this family are membrane-anchored proteins structurally related to snake venom disintegrins, and have been implicated in a variety of biological processes involving cell-cell and cell-matrix interactions, including fertilization, muscle development, and neurogenesis. (nih.gov)

Although these receptors are structurally similar, they determine specificity for four ligands-GDNF, Neurturin (NRTN), Artemin (ARTN) and Persephin (PSPN). (medsci.org)
The lysophospholipid ligands of these receptors are structurally similar, however recognition of these lipids by these receptors is highly selective. (biomedcentral.com)

The synthetic compounds discussed below contain highly oxidized iron in general, as the concepts are closely related. (wikipedia.org)
Nitridoiron and imidoiron compounds are closely related to iron-dinitrogen chemistry. (wikipedia.org)
Several structurally characterized nitridoiron(IV) compounds exist. (wikipedia.org)
Tests with a series of compounds structurally related to 1-indanone show that 2-methyl-1-indanone, 2-ethyl-1-indanone, 3-methyl-1-indanone, and 1-indanone elicit a strong response from both ORs. (frontiersin.org)
In search of new dual-acting histamine H/sigma-1 receptor ligands, we designed a series of compounds structurally based on highly active ligands previously studied and described by our team. (iasp-pain.org)
However, we kept in mind that within the previous series, a pair of closely related compounds, and , differing only in the piperazine/piperidine moiety in the structural core showed a significantly different affinity at sigma-1 receptors (σRs). (iasp-pain.org)
Whereas for several metals a division has traditionally been made into a class of strong ligands (L1) and a more abundant class of weaker ligands (L2), based on the observed stability constants ( Coale and Bruland, 1988 ), it has been argued that such divisions are an instrumental artifact and actually reflect a continuum of compounds spanning a broad window of metal affinities ( Town and Filella, 2000 ). (frontiersin.org)
Selective compounds have been developed that target either the extracellular ligand-binding region of the EGFR (including a number of monoclonal antibodies [MAbs], immunotoxins, and ligand-binding cytotoxic agents) or the intracellular tyrosine kinase region (including various small-molecule inhibitors). (medscape.com)
The strong functional union of this family is reflected in the paucity of ligands that will discriminate between its subtypes and prompts some re-evaluation of the activities of compounds which may now be regarded as nonselective for the receptor subtypes in this class. (nih.gov)
Each receptor shows a differential pattern of tissue expression and is activated by structurally diverse compounds including endogenous long-chain fatty acids. (sigmaaldrich.com)
This study attempts to perceive the mode of binding of dithionitrobenzoic acid (DTNB), and its structurally related compounds on PDI enzyme. (biomedcentral.com)
Two decades later, the prostaglandins were deduced to be a family of related compounds that contain 20-carbon polyunsaturated fatty acids with a cyclopentane ring, as depicted below. (medscape.com)

Ligand-binding characteristics and related structural features of the expressed goldfish kainate receptors: identification of a conserved disulfide bond and three residues important for ligand binding. (aspetjournals.org)
Evaluation of the active site residues of the CYP7B1 model and validation of the active site architecture were performed via molecular docking experiments: the docking of the substrates 25-hydroxycholesterol and 27-hydroxycholesterol and the inhibitor 3α-Adiol identified structurally and functionally important residues. (nih.gov)
Mutational analysis of CYP7B1 amino acid mutations related to hereditary spastic paraplegia type 5 considered phosphorylation, ligand/substrate binding and the structural roles of mutated amino acid residues, with R112, T297 and S363 mutations expected to have a direct impact on ligand binding, while mutations involving R417 would indirectly affect ligand binding as a result of impairment in catalytic function. (nih.gov)
In aspartate peptidases, Asp residues are ligands of an activated water molecule in all examples where catalytic residues have been identified. (nih.gov)
X-ray crystallography of human PPAR isoforms has revealed important residues responsible for ligand binding, heterodimerisation and co-factor interactions. (sigmaaldrich.com)
These sites are highly enriched in prolines and charged residues and are strikingly similar to other ligand-independent ribosome stalling motifs. (dgohara.me)

Wnts bind Frizzled receptors and forms complex with low-density lipoprotein receptor-related protein (LRP5 or LRP6) which results in the stabilization of intracellular beta-catenin levels. (biolegend.com)
The B7 family consists of structurally related cell-surface protein ligands, which bind to receptors on lymphocytes that regulate immune responses. (bio-connect.nl)
The catalytic core of the [FeFe]-hydrogenase (HydA), termed the H-cluster, exists as a [4Fe-4S] subcluster linked by a cysteine thiolate to a modified 2Fe subcluster with unique non-protein ligands. (rcsb.org)
A family of structurally related cell-surface receptors that signal through an intrinsic PROTEIN-TYROSINE KINASE. (bvsalud.org)
Sphingosine-1-phosphate and lysophosphatidic acid (LPA) are ligands for two related families of G protein-coupled receptors, the S1P and LPA receptors, respectively. (biomedcentral.com)
It is structurally related to the activating ligands, in that it is a secreted protein with a single epidermal growth factor (EGF) domain. (ox.ac.uk)
Interferon pathway-related cytokines/chemokines, including interleukin (IL) 18, macrophage inflammatory protein 3α, and IL-33, were elevated, but tumor necrosis factor-α, IL-6, CXCL8 (formerly IL-8), and cytokines acting through C-C chemokine receptor 2 and CCR5 were lower among case-patients than controls. (cdc.gov)
Another reported that IL-10, C-X-C motif chemokine ligand 10 (CXCL-10, formerly IFN-γ inducible protein 10) and CC chemokine ligand 2 (CCL2, formerly monocyte chemoattractant protein 1) levels were higher in patients with high viral loads ( 12 ), but patients with severe disease had higher levels of CXCL10 and CCL2 than did patients with less-severe cases. (cdc.gov)

The family of selectins consists of three structurally and functionally related molecules. (biovendor.com)
While the ligands for E- and L-selectins with primary binding activity have not been identified so far, the functionally most important ligand for P-selectin has been identified. (biovendor.com)
Structurally and functionally, the glycine receptor is most closely related to the GABAA receptor . (axonmedchem.com)

These data lend further evidence in support of a model of glutamate receptor topology with three transmembrane segments and reveal several general structural features of the extracellular ligand-binding domain of the kainate receptors. (aspetjournals.org)
Ephrin-A ligands are structurally related to the extracellular domains of the transmembrane Ephrin-B ligands. (cellgs.com)

Low-molecular-weight kainate receptors from nonmammalian vertebrate brain belong structurally to the ionotropic glutamate receptor superfamily. (aspetjournals.org)
Structurally related to the TNF superfamily, CTRPs have roles in immunity and metabolism. (rndsystems.com)
Peroxisome proliferator activated receptors (PPARs) are members of the nuclear hormone receptor superfamily of ligand-activated transcription factors that are related to retinoid, steroid and thyroid hormone receptors. (sigmaaldrich.com)
The TNFSF consists of 19 structurally related ligands, each binding to one or more of the 29 members of the TNF receptor superfamily. (apogenix.com)

The GDNF family ligands (GFLs) function through a glycosyl-phosphatidylinositol-(GPI) anchored coreceptor, GDNF family receptor alpha (GFRα), and rearranged during transfection (RET), a well-known receptor tyrosine kinase involved in kidney development, spermatogonial stem cell maintenance, and the development and maintenance of the sympathetic, parasympathetic, and enteric nervous systems [ 1 , 2 ]. (medsci.org)

The endogenous ligands of NPY receptors are a family of structurally related peptides, including NPY, peptide YY (PYY), and pancreatic polypeptide (PP). Increased activity of NPY and its receptors, Y1R, Y2R, and Y5R has been found in the brain in many forms of experimental obesity. (neuromics.com)

2) A deletion mutant lacking the originally proposed second-transmembrane domain was efficiently expressed and retains the overall ligand-binding properties of wild-type GFKAR alpha, strongly indicating that this region is not a transmembrane domain. (aspetjournals.org)
Wnts are ligand for seven-pass transmembrane receptors of the frizzled family. (biolegend.com)
c-Met and receptor originated from nantes (RON) are structurally related transmembrane phosphotyrosine kinase receptors. (oncotarget.com)
The biological activities of the FGFs are mediated by a family if type I transmembrane tyrosine kinases which undergo dimerization and autophosphorylation after ligand binding. (prospecbio.com)
Glutamic acid in the third transmembrane domain of the S1P receptors is a general selectivity switch regulating response to S1P over the closely related phospholipids, LPA. (biomedcentral.com)

State Key Laboratory for Oncogenes and Related Genes, Key Laboratory of Gastroenterology & Hepatology, Ministry of Health. (medsci.org)
Four distinct genes encoding closely related FGF receptors, FGFR-1to -4 are known. (prospecbio.com)

All ligands showed favorable interactions and most of them seemed to bind to hydrophobic amino acids Ala34, Trp36, Cys37, Cys40, His39, Thr68 and Phe80. (biomedcentral.com)
Computational modelling of the interactions between these ligands and both wild type and mutant S1P 4 receptors showed excellent agreement with experimental data, therefore confirming the fundamental role of this residue in ligand recognition by S1P receptors. (biomedcentral.com)

The preference for short-chain LPA species indicates a length restriction different from the closely related S1P 1 receptor. (biomedcentral.com)
Phylogenetic analysis of the Edg family of receptors indicates that S1P 4 is more closely related to other S1P receptors than receptors which respond to LPA. (biomedcentral.com)

Interestingly we found that number of docked clusters with each ligand varies in the range of five to eight and conveys that the binding specificity of each inhibitor varies for PDI. (biomedcentral.com)
Experimental characterisation confirmed that replacement of glutamic acid with glutamine in S1P 1 changed ligand specificity from S1P to LPA, and the reciprocal mutation in LPA 1 resulted in recognition of both LPA and S1P [ 7 ]. (biomedcentral.com)

Currently, the family consists of four structurally related secreted ligands (Rspo 1-4), all containing furin-like and thrombospondin structural domains. (reliatech.de)

Among the top features of competitive integrin antagonists is certainly to take up the ligand binding pocket and induce a conformational transformation that is like the conformational transformation induced by an all natural ligand. (bioinf.org)
Probable ligand for integrin in the brain. (nih.gov)

Importantly, Mfsd2a transported structurally related acylcarnitines but not a lysolipid without a negative charge, demonstrating the necessity of a negative charged headgroup interaction with Lys436 for transport. (neurosciencenews.com)
The interaction of trimeric TNFSF ligands with their specific cell surface receptors leads to clustering of these receptors, followed by intracellular signal transduction. (apogenix.com)

This is attributed to the relatively easy synthetic procedure of the ligands and interesting structural features such as helicity, water clusters and porosity that the coordination complexes possess. (sun.ac.za)
The Edg receptor family is classified into two clusters based on ligand selectivity: S1P 1/2/3/4/5 (formerly Edg1/5/3/6/8) specifically respond to S1P whilst LPA 1/2/3 (formerly Edg2/4/7) respond to LPA [ 5 ]. (biomedcentral.com)

Mutations in the DSL (Delta, Serrate, Lag2) Notch (N) ligand Delta-like (Dll) 3 cause skeletal abnormalities in spondylocostal dysostosis, which is consistent with a critical role for N signaling during somitogenesis. (rupress.org)
Aberrant expression and activities of c-Met and RON in cancer are attributed to various mechanisms including increased expression of their ligands or receptors and by activating mutations [ 4 , 15 ]. (oncotarget.com)

Different putative ligand structures have been identified for which the selectins show high affinity. (biovendor.com)
We conducted series of potentiometric titrations, in non-coordinating medium at seawater ionic strength (0.7 M NaClO 4 ) over a range of metal:ligand molar ratios, to study complexation of the siderophore desferrioxamine B (DFOB) with Mg and Ca, for which it has the highest affinity among the major seasalt cations. (frontiersin.org)
Besides high affinity and long tumor retention, the DOTA-conjugated ligand PSMA-617 has low kidney uptake, making it an excellent choice for therapeutic application. (snmjournals.org)
Flare Free Energy Perturbation (FEP) offers a quantitative method to reliably calculate relative binding affinity, enabling accurate ranking of molecules in a congeneric ligand series. (cresset-group.com)
Right here we survey the id of many structurally related substances that were in a position to prevent publicity of ligand-induced binding site (LIBS) epitope following the addition of VLA-4-particular ligand lower binding affinity of VLA-4-particular ligand and stop VLA-4/VCAM-1-reliant cell adhesion. (bioinf.org)
EXPERIMENTAL Techniques Components The VLA-4-particular ligand (22 -24) 4-((～12 nm) and above the for physiologically turned on VLA-4 (high affinity condition ～1-2 nm) (22). (bioinf.org)

Ligand docking studies and biochemical assays identified Lys436 as a key residue for transport. (neurosciencenews.com)
When the level of estrogen receptor (ER)-β mRNA in tumors, determined by reverse transcription-PCR, was assessed according to either ER status or PR status alone, determined by ligand binding assays, the level of ER-β mRNA was significantly lower in PR+ tumors compared with PR−tumors ( P = 0.036), and no association with ER status was found. (aacrjournals.org)
The cases were selected for ER and PR status as determined by ligand binding assays. (aacrjournals.org)

We performed molecular docking simulation with six different inhibitors (ligand), which includes DTNB, NSC695265, thionitrobenzoic acid, 2-nitro-5-thiocyanobenzoic acid, 2-nitro-5-sulfo-sulfonyl-benzoic acid and NSC517871 into the redox-active site [C37-G38-H39-C40] of the PDI enzyme and the activity was inferred by redox inhibitory models. (biomedcentral.com)
A recent addition to the list of immune checkpoint inhibitors is the CD95 ligand (CD95L). (apogenix.com)

For other types of ligands, e.g. longer nucleotides and peptides, a manually drawn representation of the molecule may be provided. (guidetopharmacology.org)

Thus, the higher efficiency of ligand 1 over ligand 2 in Pd/L-catalyzed Suzuki arylation of aryl chlorides can be ascribed to the ability of ligand 1 to generate and stabilize mono-phosphine P,O-chelating Pd/L intermediates, which appear to be most suitable for Suzuki arylation reactions involving certain substrates and conditions. (unboundmedicine.com)

1] Novel animal-health drug targets from ligand-gated chloride channels. (axonmedchem.com)

Due to a common structural element, the amino-terminal lectin-like domain, the selectins are able to bind to carbohydrate ligands. (biovendor.com)

Because all of the identified substances are structurally related used or presently marketed medications this Piperlongumine result Piperlongumine starts a variety of therapeutic opportunities for VLA-4-related pathologies. (bioinf.org)
Because these substances are used or presently marketed medications (17 -19) that are known to Piperlongumine have immunosuppressive properties (20) this influence on VLA-4 ligand binding offers a plausible description for the system of immunosuppression (21). (bioinf.org)

Dual Piperidine-Based Histamine H and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain. (iasp-pain.org)

It was shown that glycoproteins represent the biological relevant ligands for selectins. (biovendor.com)

Activation of T and B lymphocytes is initiated by engagement of cell-surface, antigen-specific T cell or B cell receptors, but additional signals delivered simultaneously by B7 ligands determine the ultimate immune response. (bio-connect.nl)

In this study, two previously cloned goldfish kainate receptor subunits (GFKAR alpha and GFKAR beta) were transiently expressed in human embryonic kidney 293 cells, and their ligand-binding properties and some associated structural features were characterized, resulting in the following findings. (aspetjournals.org)

In a series of 16 new ligands, mainly based on the piperidine core, we selected three lead structures (, , and ) for further biological evaluation. (iasp-pain.org)

3] Structure and Function of the Glycine Receptor and Related Nicotinicoid Receptors. (axonmedchem.com)

The reaction of ligand 1 with Pd(dba)(2) affords the complex LPd(dba) (14, L = 1). (unboundmedicine.com)
The NMR spectroscopic and X-ray crystallographic data of complex 14 establish that ligand 1 functions as a P,O-chelating ligand in complex 14. (unboundmedicine.com)
Br)}(2) with ligand 2 affords the bis-phosphine complex L(2)Pd(4-(t)()Bu-C(6)H(4))(Br) (13, L = 2). (unboundmedicine.com)
The NMR spectroscopic data of complex 13 establish that ligand 2 in complex 13 functions as a nonchelating ligand. (unboundmedicine.com)
In the second part, the synthesized ligands were reacted with a variety of transition metal salts to yield fifteen novel coordination polymers and one discrete complex. (sun.ac.za)

Importantly, increasing numbers of novel reports suggest that the GFRα-mediated signaling pathway acts as an oncogenic promoter related to tumor proliferation, invasion, and metastasis as well as treatment resistance. (medsci.org)
Therefore, it seems more promising that a radioactive PSMA ligand, which is directly internalized into tumor cells, will be effective in delivering high doses for systemic endoradiotherapy. (snmjournals.org)

Nonetheless, marine microbes doubtlessly make unique ligands to regulate the bioavailability or, in some cases, the toxicity of various metals. (frontiersin.org)

The C-terminal ligand-binding domain (regions E/F) is the site of ligand docking and has the most diversity between the pharmacologically distinct subtypes. (sigmaaldrich.com)
Structurally distinct PPREs are recognized by PPARα, δ and γ. (sigmaaldrich.com)

ENGLISH ABSTRACT: The number of coordination complexes utilizing bis-pyridyl diamide ligands has increased significantly over the past decade. (sun.ac.za)
We have crystallized a reported polycarboxyl-ate containing the ligand, 5-[(4-carb-oxy-benz-yl)-oxy]isophthalic acid (CIA), which has the advantage of being flexible and has conformational freedom allowing it to conform to the coordination environment of transition metal ions. (iucr.org)

Specifically, at clinically attainable serum concentrations, telmisartan is unique among these drugs in its ability to structurally interact with and activate the PPARg receptor, a ligand-activated transcription factor that regulates lipid metabolism and insulin sensitivity. (medicalnewstoday.com)

Book antibody epitopes termed ligand-induced binding site (LIBS) epitopes are open because of this conformational transformation (12 -15). (bioinf.org)
The binding of ligand triggers a series of events which result in conformational changes involving recruitment of coactivators and dissociation of corepressors. (sigmaaldrich.com)

TNFSF ligands naturally exist as homo-trimers with three receptor binding sites. (apogenix.com)

PPARs have a highly conserved DNA binding domain (region C) and a diverse ligand-independent activation domain (region A/B) which can confer constitutive activity on the receptor. (sigmaaldrich.com)
We tested whether mutation of this "ligand selectivity" residue to glutamine could confer LPA-responsiveness to the related S1P receptor, S1P 4 . (biomedcentral.com)

FeVTAML(=O), TAML = tetra-amido macrocyclic ligand, is formed by the reaction of [FeIII(TAML)(H2O)](PPh4) with 2-5 equivalents of meta-chloroperbenzoic acid at -60 ˚C in n-butyronitrile. (wikipedia.org)
Such comparisons cannot be meaningfully interpreted unless the side-reaction coefficient (SRC) of the model ligand in seawater is thoroughly evaluated. (frontiersin.org)

In contrast, the structurally related ligand 2-(2'-dicyclohexylphosphinophenyl)-1,3-dioxolane (ligand 2) was found to be less efficient under similar conditions. (unboundmedicine.com)
1, 2, 4] Short bones arise from the same precursors but are not necessarily structurally similar to long bones, often taking on unique shapes (eg, carpal bones). (medscape.com)

Manipulation of the signals delivered by B7 ligands has shown potential in the treatment of autoimmunity, inflammatory diseases and cancer. (bio-connect.nl)
Nephrotic syndrome is neither a single gested that IL-1 has a significant role in the disease nor even a heterogeneous group of immunopathogenesis of proteinuria [ 7 ] and related diseases. (who.int)

Electrochemical techniques like adsorptive cathodic stripping voltammetry with competitive ligand equilibration (ACSV-CLE) can determine total concentrations of marine organic ligands and their conditional binding constants for specific metals, but cannot identify them. (frontiersin.org)
A complementary approach is to compare known properties of natural ligands, particularly their conditional binding constants, with those of model organic ligands, measured under suitable conditions. (frontiersin.org)
Binding of a ligand leads to internalization via clathrin-coated pits ( 3 ) and prolonged retention in the cell. (snmjournals.org)
In this study, the relationship of ER-β mRNA expression to ER and PR status, as determined by ligand binding analysis, was investigated. (aacrjournals.org)
The receptors are activated upon binding of specific ligands which include EPIDERMAL GROWTH FACTORS, and NEUREGULINS. (bvsalud.org)
PPAR-RXR heterodimers can also be activated by ligand binding to either receptor partner independently. (sigmaaldrich.com)
Mouse and human cDNA clones encoding the ligand-binding IL-10 receptor (IL-10 R) have been isolated. (bio-techne.com)

Levels of endocannabinoid ligands (AEA, NAGly, and 2-AG) change significantly in rodent brain with the estrous cycle and show sex differences, suggesting a preparatory role for mating [ 10 ]. (hindawi.com)

Our findings suggest that statistically important differences exist in the effectiveness of angiotensin-receptor blockers when used for the prevention of diabetes-related macrovascular disease, and that a class effect for these agents may not be assumed when used for this purpose in clinical practice,' writes Dr. Tony Antoniou, Department of Family and Community Medicine, St. Michael's Hospital, Toronto, with coauthors. (medicalnewstoday.com)

Benchmarking experiments can be used to gain confidence that your system is prepared correctly, confirming the predictivity of the method on the target and ligand series of interest. (cresset-group.com)

The TAM receptor and ligand expression was evaluated in LMS cell lines and 358 sarcoma samples by either gene expression or immunohistochemistry. (nature.com)

Chemicals and Drugs7

Analytical, Diagnostic and Therapeutic Techniques and Equipment1

Phenomena and Processes4

Information Science2

Proteins11

Receptors are structurally similar2

Compounds12

Residues6

Protein8

Functionally3

Extracellular2

Superfamily4

Receptor tyrosi1

Endogenous1

Transmembrane5

Genes2

Interactions2

Closely related2

Specificity2

Consists1

Integrin2

Interaction2

Clusters2

Mutations2

Affinity6

Assays3

Inhibitors2

Peptides1

Stabilize1

Targets1

Bind1

Substances2

Histamine1

Glycoproteins1

Immune response1

Structural features1

Structures1

Glycine1

Complex5

Tumor2

Regulate1

Distinct2

Coordination2

Transcription1

Conformational2

Naturally1

Confer2

Reaction2

Similar2

Diseases2

Binding7

Significantly1

Important1

Series1

Cell1