A technology, in which sets of reactions for solution or solid-phase synthesis, is used to create molecular libraries for analysis of compounds on a large scale.
Methods used for the chemical synthesis of compounds. Included under this heading are laboratory methods used to synthesize a variety of chemicals and drugs.
Inorganic or organic derivatives of phosphinic acid, H2PO(OH). They include phosphinates and phosphinic acid esters.
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.
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.
Methodologies used for the isolation, identification, detection, and quantitation of chemical substances.
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.
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.
Organic chemistry methodology that mimics the modular nature of various biosynthetic processes. It uses highly reliable and selective reactions designed to "click" i.e., rapidly join small modular units together in high yield, without offensive byproducts. In combination with COMBINATORIAL CHEMISTRY TECHNIQUES, it is used for the synthesis of new compounds and combinatorial libraries.
Thin strands of transparent material, usually glass, that are used for transmitting light waves over long distances.
That portion of the electromagnetic spectrum in the visible, ultraviolet, and infrared range.
Nucleus of the spinal tract of the trigeminal nerve. It is divided cytoarchitectonically into three parts: oralis, caudalis (TRIGEMINAL CAUDAL NUCLEUS), and interpolaris.
The technology of transmitting light over long distances through strands of glass or other transparent material.
Exclusive legal rights or privileges applied to inventions, plants, etc.
Differential thermal analysis in which the sample compartment of the apparatus is a differential calorimeter, allowing an exact measure of the heat of transition independent of the specific heat, thermal conductivity, and other variables of the sample.
The deliberate and methodical practice of finding new applications for existing drugs.
Carbohydrates consisting of between two (DISACCHARIDES) and ten MONOSACCHARIDES connected by either an alpha- or beta-glycosidic link. They are found throughout nature in both the free and bound form.
The largest class of organic compounds, including STARCH; GLYCOGEN; CELLULOSE; POLYSACCHARIDES; and simple MONOSACCHARIDES. Carbohydrates are composed of carbon, hydrogen, and oxygen in a ratio of Cn(H2O)n.
The sequence of carbohydrates within POLYSACCHARIDES; GLYCOPROTEINS; and GLYCOLIPIDS.
The characteristic 3-dimensional shape of a carbohydrate.
Cellular processes in biosynthesis (anabolism) and degradation (catabolism) of CARBOHYDRATES.
Facilities providing diagnostic, therapeutic, and palliative services for patients with severe chronic pain. These may be free-standing clinics or hospital-based and serve ambulatory or inpatient populations. The approach is usually multidisciplinary. These clinics are often referred to as "acute pain services". (From Br Med Bull 1991 Jul;47(3):762-85)
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
Lists of persons or organizations, systematically arranged, usually in alphabetic or classed order, giving address, affiliations, etc., for individuals, and giving address, officers, functions, and similar data for organizations. (ALA Glossary of Library and Information Science, 1983)
A publication issued at stated, more or less regular, intervals.
A quantitative measure of the frequency on average with which articles in a journal have been cited in a given period of time.
Directory signs or listings of designated areas within or without a facility.
The homogeneous mixtures formed by the mixing of a solid, liquid, or gaseous substance (solute) with a liquid (the solvent), from which the dissolved substances can be recovered by physical processes. (From Grant & Hackh's Chemical Dictionary, 5th ed)
"The business or profession of the commercial production and issuance of literature" (Webster's 3d). It includes the publisher, publication processes, editing and editors. Production may be by conventional printing methods or by electronic publishing.
A class of devices combining electrical and mechanical components that have at least one of the dimensions in the micrometer range (between 1 micron and 1 millimeter). They include sensors, actuators, microducts, and micropumps.
Methods of creating machines and devices.
An interdisciplinary field in materials science, ENGINEERING, and BIOLOGY, studying the use of biological principles for synthesis or fabrication of BIOMIMETIC MATERIALS.
A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.
Property, such as patents, trademarks, and copyright, that results from creative effort. The Patent and Copyright Clause (Art. 1, Sec. 8, cl. 8) of the United States Constitution provides for promoting the progress of science and useful arts by securing for limited times to authors and inventors, the exclusive right to their respective writings and discoveries. (From Black's Law Dictionary, 5th ed, p1014)
Rapid methods of measuring the effects of an agent in a biological or chemical assay. The assay usually involves some form of automation or a way to conduct multiple assays at the same time using sample arrays.
The misinterpretation of a real external, sensory experience.
The resistance that a gaseous or liquid system offers to flow when it is subjected to shear stress. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
A procedure consisting of a sequence of algebraic formulas and/or logical steps to calculate or determine a given task.
In statistics, a technique for numerically approximating the solution of a mathematical problem by studying the distribution of some random variable, often generated by a computer. The name alludes to the randomness characteristic of the games of chance played at the gambling casinos in Monte Carlo. (From Random House Unabridged Dictionary, 2d ed, 1993)
Computer-based representation of physical systems and phenomena such as chemical processes.
A plant species of the family CUCURBITACEAE that is a source of TRICHOSANTHIN (a ribosomal inhibitory protein).
Sequential operating programs and data which instruct the functioning of a digital computer.
Processes that incorporate some element of randomness, used particularly to refer to a time series of random variables.
A field of biology concerned with the development of techniques for the collection and manipulation of biological data, and the use of such data to make biological discoveries or predictions. This field encompasses all computational methods and theories for solving biological problems including manipulation of models and datasets.
Microdevices that combine microfluidics technology with electrical and/or mechanical functions for analyzing very small fluid volumes. They consist of microchannels etched into substrates made of silicon, glass, or polymer using processes similar to photolithography. The test fluids in the channels can then interact with different elements such as electrodes, photodetectors, chemical sensors, pumps, and valves.
The study of fluid channels and chambers of tiny dimensions of tens to hundreds of micrometers and volumes of nanoliters or picoliters. This is of interest in biological MICROCIRCULATION and used in MICROCHEMISTRY and INVESTIGATIVE TECHNIQUES.
Methods utilizing the principles of MICROFLUIDICS for sample handling, reagent mixing, and separation and detection of specific components in fluids.
Systems for the delivery of drugs to target sites of pharmacological actions. Technologies employed include those concerning drug preparation, route of administration, site targeting, metabolism, and toxicity.
An international agreement of the World Medical Association which offers guidelines for conducting experiments using human subjects. It was adopted in 1962 and revised by the 18th World Medical Assembly at Helsinki, Finland in 1964. Subsequent revisions were made in 1975, 1983, 1989, and 1996. (From Encyclopedia of Bioethics, rev ed, 1995)

A multiplasmid approach to preparing large libraries of polyketides. (1/942)

A three-plasmid system for heterologous expression of 6-deoxyerythronolide B synthase (DEBS) has been developed to facilitate combinatorial biosynthesis of polyketides made by type I modular polyketide synthases (PKSs). The eryA PKS genes encoding the three DEBS subunits were individually cloned into three compatible Streptomyces vectors carrying mutually selectable antibiotic resistance markers. A strain of Streptomyces lividans transformed with all three plasmids produced 6-deoxyerythronolide B at a level similar to that of a strain transformed with a single plasmid containing all three genes. The utility of this system in combinatorial biosynthesis was demonstrated through production of a library of modified polyketide macrolactones by using versions of each plasmid constructed to contain defined mutations. Combinations of these vector sets were introduced into S. lividans, resulting in strains producing a wide range of 6-deoxyerythronolide B analogs. This method can be extended to any modular PKS and has the potential to produce thousands of novel natural products, including ones derived from further modification of the PKS products by tailoring enzymes.  (+info)

Modelling G-protein-coupled receptors for drug design. (2/942)

The G-protein coupled receptors form a large and diverse multi-gene superfamily with many important physiological functions. As such, they have become important targets in pharmaceutical research. Molecular modelling and site-directed mutagenesis have played an important role in our increasing understanding of the structural basis of drug action at these receptors. Aspects of this understanding, how these techniques can be used within a drug-design programme, and remaining challenges for the future are reviewed.  (+info)

A combinatorial approach to producing sterically stabilized (Stealth) immunoliposomal drugs. (3/942)

We have developed a method for producing sterically stabilized immunoliposomal drugs (SIL) readily applicable to a 'mix and match' combinatorial approach for the simple manufacture of a variety of ligand-targeted liposomal drugs. Ligands coupled to the terminus of polyethylene glycol (PEG) in micelles formed from PEG-lipid derivatives (mPEG2000-DSPE) could be transferred into preformed, drug-containing liposomes from the micelles in a temperature- and time-dependent manner. Antibody densities up to 100 microg antibody/micromol of phospholipid, and up to 3 mol% of mPEG2000-DSPE, could be simultaneously transferred from the ligand-coupled micelles into the liposomal outer monolayer with negligible drug leakage from liposomes during transfer and good stability in human plasma. Transfer of anti-CD19 into SIL resulted in a three-fold increase in binding of these liposomes to CD19+ human B cell lymphoma cells.  (+info)

Phagotopes derived by antibody screening of phage-displayed random peptide libraries vary in immunoreactivity: studies using an exemplary monoclonal antibody, CII-C1, to type II collagen. (4/942)

Antibody screening of phage-displayed random peptide libraries to identify mimotopes of conformational epitopes is promising. However, because interpretations can be difficult, an exemplary system has been used in the present study to investigate whether variation in the peptide sequences of selected phagotopes corresponded with variation in immunoreactivity. The phagotopes, derived using a well-characterized monoclonal antibody, CII-C1, to a known conformational epitope on type II collagen, C1, were tested by direct and inhibition ELISA for reactivity with CII-C1. A multiple sequence alignment algorithm, PILEUP, was used to sort the peptides expressed by the phagotopes into clusters. A model was prepared of the C1 epitope on type II collagen. The 12 selected phagotopes reacted with CII-C1 by both direct ELISA (titres from < 100-11 200) and inhibition ELISA (20-100% inhibition); the reactivity varied according to the peptide sequence and assay format. The differences in reactivity between the phagotopes were mostly in accord with the alignment, by PILEUP, of the peptide sequences. The finding that the phagotopes functionally mimicked the C1 epitope on collagen was validated in that amino acids RRL at the amino terminal of many of the peptides were topographically demonstrable on the model of the C1 epitope. Notably, one phagotope that expressed the widely divergent peptide C-IAPKRHNSA-C also mimicked the C1 epitope, as judged by reactivity in each of the assays used: these included cross-inhibition of CII-C1 reactivity with each of the other phagotopes and inhibition by a synthetic peptide corresponding to that expressed by the most frequently selected phagotope, RRLPFGSQM. Thus, it has been demonstrated that multiple phage-displayed peptides can mimic the same epitope and that observed immunoreactivity of selected phagotopes with the selecting mAb can depend on the primary sequence of the expressed peptide and also on the assay format used.  (+info)

Fibroblast growth factor receptor signalling is dictated by specific heparan sulphate saccharides. (5/942)

Signalling by fibroblast growth factors (FGFs) through FGF receptors (FGFRs) depends on the cell-surface polysaccharide heparan sulphate (HS) [1] [2]. HS has an ordered domain structure of highly diverse saccharide motifs that present unique displays of sulphate, carboxyl and hydroxyl groups [3]. These motifs interact with many proteins, particularly growth factors. HS binds both to FGFs [4] [5] [6] and FGFRs [7], and probably activates signalling by facilitating ligand-induced receptor dimerisation [8] [9]. Nevertheless, the extent to which specific HS saccharide sequences play a regulatory role has not been established. By screening a library of structurally diverse HS decasaccharides in bioassays of FGF signalling mediated by three different FGFR isoforms, we found that saccharides showed specificity for both ligands and receptors; some saccharides selectively activated FGF signalling through different FGFR isoforms, others acted as negative regulators. We conclude that HS saccharides play critical roles in dictating the specificity of ligand-receptor interactions in FGFR signalling. Controlled alterations in HS structures [10] would provide a mechanism for regulation of cellular responsiveness to growth factors that bind HS.  (+info)

Combinatorial catalysis: identification of potent chiral catalysts through fluorescent bead signaling. (6/942)

Simultaneous labeling of beads with a fluorescent sensor and a unique catalyst allows chemists to identify the most active catalyst within a mixture. This approach is a valuable addition to the protocols available in the growing field of combinatorial catalysis.  (+info)

A loop-mimetic inhibitor of the HCV-NS3 protease derived from a minibody. (7/942)

We have been interested for some time in establishing a strategy for deriving lead compounds from macromolecule ligands such as minibody variants. A minibody is a minimized antibody variable domain whose two loops are amenable to combinatorial mutagenesis. This approach can be especially useful when dealing with 'difficult' targets. One such target is the NS3 protease of hepatitis C virus (HCV), a human pathogen that is believed to infect about 100 million individuals worldwide and for which an effective therapy is not yet available. Based on known inhibitor specificity (residues P6-P1) of NS3 protease, we screened a number of minibodies from our collection and we were able to identify a competitive inhibitor of this enzyme. We thus validated an aspect of recognition by HCV NS3 protease, namely that an acid anchor is necessary for inhibitor activity. In addition, the characterization of the minibody inhibitor led to the synthesis of a constrained hexapeptide mimicking the bioactive loop of the parent macromolecule. The cyclic peptide is a lead compound prone to rapid optimization through solid phase combinatorial chemistry. We therefore confirmed that the potential of turning a protein ligand into a low molecular weight active compound for lead discovery is achievable and can complement more traditional drug discovery approaches.  (+info)

Oligonucleotide-conjugated beads for transdominant genetic experiments. (8/942)

Transdominant genetics using expression libraries can identify proteins and peptides that affect cell division. In conjunction with these libraries, oligo-nucleotide-conjugated beads and flow cytometry were used to test a strategy that potentially expands the range of such genetic studies. The experimental approach involved creation of tagged expression libraries, introduction of these libraries into cells, growth of the cultured cells for several generations and recovery on oligonucleotide-conjugated beads of sequences that encode growth-modulatory proteins or peptides. Experiments in Saccharomyces cerevisiae demonstrating the feasibility of the strategy are presented.  (+info)

387501517 - EP 0983983 A3 2000-07-05 - Combinatorial synthesis and analysis of organometallic compounds and catalysts - [origin: EP0978499A2] Methodologies for the synthesis, screening and characterisation of organometallic compounds and catalysts (eg homogenous catalysts), including combinatorial synthesis, screening and characterisation of libraries of supported and unsupported organometallic compounds and catalysts (eg homogenous catalysts). The methods can be applied to the preparation and screening of large numbers of organometallic compounds which can be used not only as catalysts (eg homogeneous catalysts), but also as additives and therapeutic agents.[origin: EP0978499A2] Methodologies for the synthesis, screening and characterisation of organometallic compounds and catalysts (eg homogenous catalysts), including combinatorial synthesis, screening and characterisation of libraries of supported and unsupported organometallic compounds and catalysts (eg homogenous catalysts). The methods can be
Dynamic combinatorial chemistry utilises reversible reactions to set up a dynamic library of molecules, with the library composition determined by the thermodynamic stability of each library member. Upon addition of a protein template, any library members which bind to the template are stabilised and amplified. Analysis of the library composition enables the identification of molecules which bind to the template protein. The suitability of two enzyme catalysed reactions catalysed by N-acetylneuraminic acid aldolase and subtilisin® Carlsberg was investigated for use in the synthesis of a DCL. A 173 component dynamic combinatorial library was successfully synthesised using these reactions with the resulting library screened against two protein template molecules, wheat germ agglutinin and Div1B. Several methods were investigated for the simplification of DCL analysis including the immobilisation of protein template molecules and the segregation of DCL proteins using semi-permiable membranes, ...
Download free Solid-Phase Organic Syntheses, Volume 2: Solid-Phase Palladium Chemistry (Wiley Series on Solid-Phase Organic Syntheses) ePub eBook
Combinatorial Chemistry & High Throughput Screening (CCHTS) publishes full length original research articles and reviews dealing with various topics related to chemical biology (High Throughput Screening, Combinatorial Chemistry, Chemoinformatics, Laboratory Automation and Compound management) in advancing drug discovery research.
Since oxidative cellular damage contributes to the development of cancers, heart disease and ageing, the synthesis of antioxidative agents which are able to either prevent or mitigate oxidative stress to cells is an important area of investigation. Combinatorial chemistry has had a profound impact on the discovery and optimisation of potential lead compounds, especially in the medicinal field. This review details recent examples of combinatorial chemistry dealing with the synthesis of novel antioxidants with an emphasis on solid phase compound synthesis and parallel library synthesis.. Full text not available from this repository.. ...
Combinatorial Chemistry & High Throughput Screening (CCHTS) publishes full length original research articles and reviews dealing with various topic...
Trusted information for laboratory scientists about Combinatorial Chemistry lab products and techniques on SelectScience, including reagents, reactors and standards.
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Bentham Science Publishers would like to invite you to submit your research paper for publishing in the Journal of Combinatorial Chemistr ...
The goal of this thesis was to develop a method for efficiently synthesizing a large suite of asymmetric oligoester ion channel-forming compounds. A solid-phase organic synthesis (SPOS) approach on Wang resin was used to generate the ion channel candidates. A follow-on goal is to survey the compounds produced to uncover structure-related controls on ion transport activity. Two classes of building blocks were used to generate the oligoesters - head groups and cores. The core building blocks were three omega-hydroxy acid derivatives six, eight and twelve carbons in length and the alcohol protected as a tetrahydropyranyl ether. The head group building blocks were either a glutaric acid monoester derivative of varying lipophilicity (12 to 16 carbon long alkyl tail) or a beta-hydroxy acid derivative; these building blocks used a tert-butyldimethylsilyl ether for alcohol protection. Optimized conditions for building block coupling, deprotection, and product cleavage were first established by the ...
Establishing synthesis methods for a target material constitutes a grand challenge in materials research, which is compounded with use-inspired specifications on the format of the material. Solar photochemistry using thin film materials is a promising technology for which many complex materials are being proposed, and the present work describes application of combinatorial methods to explore the synthesis of predicted La-Bi-Cu oxysulfide photocathodes, in particular alloys of LaCuOS and BiCuOS. The variation in concentration of three cations and two anions in thin film materials, and crystallization thereof, is achieved by a combination of reactive sputtering and thermal processes including reactive annealing and rapid thermal processing. Composition and structural characterization establish composition-processing-structure relationships that highlight the breadth of processing conditions required for synthesis of LaCuOS and BiCuOS. The relative irreducibility of La oxides and limited diffusion ...
TentaGel® Macrobeads are highlighted by extraordinary large particle diameters and high capacities based on the TentaGel® technology and designed for single bead synthesis and single bead analysis ...
Multicomponent reactions are flexible reactions for the rapid generation of complex molecules with often biologically relevant scaffold structures. Combined with the ease of parallelization and the exploratory power with regard to chemical space, multicomponent reactions have attracted significant attention
Title:Tandem Multicomponent Reactions Toward the Design and Synthesis of Novel Antibacterial and Cytotoxic Motifs. VOLUME: 20 ISSUE: 11. Author(s):Mohammad H. Semreen, Raafat El-Awady, Raed Abu-Odeh, Maha Saber-Ayad, Raed A. Al-Qawasmeh, Salem Chouaib, Wolfgang Voelter and Taleb H. Al-Tel. Affiliation:Sharjah Institute for Medical Research, University of Sharjah, P.O.Box 27272, Sharjah, UAE.. Keywords:Imidazopyridines, Ugi reaction, multicomponent reaction, Groebke-Blackburn reaction, antibacterial, hospital resistant strains, anticancer.. Abstract:The synthesis of polysubstituted imidazopyridines and imidazopyrazines through the orthogonal union of Groebke-Blackburn and Ugi reactions is described. These motifs were produced efficiently in a tandem operation without intermediate isolation. The synthesized scaffolds were biologically evaluated and found to posses potent anticancer and antibacterial activities. Importantly, some of these motifs (e.g. compound 5) were found to possess specific ...
International Scholarly Research Notices is a peer-reviewed, Open Access journal covering a wide range of subjects in science, technology, and medicine. The journals Editorial Board as well as its Table of Contents are divided into 108 subject areas that are covered within the journals scope.
The designing, synthesizing and screening of one-bead-one-compound (OBOC) combinatorial chemistry libraries against a single target ligand has been well developed. Recently, novel cholesterol/peptide hybrid combinatorial One-Bead-One-Compound (OBOC) combinatorial libraries have been developed and synthesized with self folding capabilities. The library design strategy was based on a similar pentamer and hexamer self-folding branched tricylic libraries previously developed. The cholic acid on the side chain of the carboxyl lysine is believed to interact with fixed hydrophobic amino acids at the amino-termini (position 5) of the twin branched L-amino acid arms and self-fold into a tricyclic molecule. The newly synthesized library has arginine (R) and Lysine (K) down-proportioned to 10 % for each position to decrease the probability of positive charge nonspecific binding. Thirty L-, D-, and unnatural amino acids were used in each position as building blocks. Hydrophobicity was fixed at position 5 ...
An apparatus for high-throughput combinatorial syntheses of organic molecules including a reaction vessel for containing a combinatorial-chemistry synthetic reaction, a liquid dispenser for dispensing the liquid, a liquid aspirator and an adjustment mechanism. The reaction vessel includes an ingress aperture allowing a liquid to enter into an interior of the vessel and an egress aperture for aspirating the liquid from the vessel. The liquid dispenser dispenses liquid through the ingress aperture. The liquid aspirator aspirates liquid through the egress aperture and includes a rotor for carrying the vessel and orbiting the vessel about an axis of rotation. The rotor is oriented generally in a horizontal plane and includes an adjustment mechanism for adjusting the angle of the vessel relative to the horizontal plane in response to the centrifugal force generated by orbiting the vessel about the axis of rotation. A method of combinatorial synthesis of organic molecules is also disclosed.
Systems and methods for providing in situ, controllably variable concentrations of one, two or more chemical components on a substrate to produce an integrated materials chip. The component concentrations can vary linearly, quadratically or according to any other reasonable power law with one or two location coordinates. In one embodiment, a source and a mask with fixed or varying aperture widths and fixed or varying aperture spacings are used to produce the desired concentration envelope. In another embodiment, a mask with one or more movable apertures or openings provides a chemical component flux that varies with location on the substrate, in one or two dimensions. In another embodiment, flow of the chemical components through nuzzle slits provides the desired concentrations. An ion beam source, a sputtering source, a laser ablation source, a molecular beam source, a chemical vapor deposition source and/or an evaporative source can provide the chemical component(s) to be deposited on the substrate.
Diversity-oriented synthesis yields a new drug lead for treatment of chagas disease.: A phenotypic high-throughput screen using ∼100,000 compounds prepared usin
N-Acylsulfonamides usually react with nucleophiles by acyl transfer and C-N bond fission. However, the hydrolysis of N-acyl -sultams is a sulfonyl transfer reaction that occurs with S-N fission and opening of the four-membered ring. Similar to other -sultams, the N-acyl derivatives are at least 106-fold more reactive than N-acyl sulfonamides. 3-Oxo--sultams are both -lactams and -sultams but also hydrolyze with preferential S-N bond fission.. ...
TentaGel® resins are grafted copolymers consisting of a low crosslinked polystyrene matrix on which polyethylene glycol (PEG or POE) is grafted. The PEG spacer is attached to the matrix via an ethyl ether group which increases stability towards acid treatment and minimizes PEG-leaching. As PEG is a chameleon type polymer with hydrophobic and hydrophilic properties, the graft copolymer shows modified physico chemical properties which are highly dominated by the PEG moiety (and no longer by the polystyrene matrix). These graft copolymers are pressure stable and can be used in batch processes as well as under continuous flow conditions. The PEG spacer is in the range of MW 3000 Da. This resin is synthesized from TentaGel® amine and the base labile 4-(hydroxymethyl)benzoic acid linker. It is a versatile support for the immobilization of carboxylic acids. The resulting ester bond is stable to strong acids but is cleaved by nucleophiles like amines, hydrazine or alkoxides. ...
Isogenica, Cambridge UK and Imperial College London secure funding from UKs Technology Strategy Board to develop gene library synthesis for synthetic
A novel bacteriophage lambda vector system was used to express in Escherichia coli a combinatorial library of Fab fragments of the mouse antibody repertoire. The system allows rapid and easy identification of monoclonal Fab fragments in a form suitable for genetic manipulation. It was possible to generate, in 2 weeks, large numbers of monoclonal Fab fragments against a transition state analog hapten. The methods described may supersede present-day hybridoma technology and facilitate the production of catalytic and other antibodies.. ...
AIM AND OBJECTIVE: The importance of acridine core structure and other heterocycles containing its framework is well known, as they are found in numerous compounds with a variety of biological effects. Pyridine is also an important solvent and heterocyclic nucleus for the design and synthesis of novel molecules with biological properties. It occurs in several natural compounds which are used as a precursor in agrochemicals and pharmaceuticals. The utility of nanostructured metal salts because of their small size and high surface area as catalysts in organic synthesis has drawn special attention due to their better properties such as slower reaction rate, reusability of the catalyst, and higher yields of products compared to the bulk size ...
Bentham Science Publishers would like to invite you to submit your research paper for publishing in the Journal of Combinatorial Chemistr ...
PharmaSeq, Inc., is a private company located near Princeton, NJ. Its business is in developing an ultra-small microtransponder tagging platform that has broad applications for the tagging and tracking of objects used in the consumer goods, industrial goods, life sciences and eventually clinical diagnostics industries.
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A versatile copper(i)-catalyzed cascade multicomponent reaction strategy between readily available (Z)-3-iodoacrylic acids, terminal alkynes, and primary amines is reported, leading to a great diversity of complex heterocyclic backbones based on biorelevant indole/lactam scaffolds.
The use of cyclic peptides in one-bead-one-compound libraries is limited by difficulties in sequencing hit compounds. Lacking a free N-terminal amine, such peptides cannot be sequenced by the Edman degradation approach, and complex fragmentation patterns are obtained by tandem mass spectrometry. To overcome this problem, we designed an alternative approach introducing a methionine residue within the macrocycle and as a linker to allow simultaneous ring-opening and release from the resin upon treatment with cyanogen bromide. The methionine linker was inverted relative to the peptide chain to allow the synthesis of cyclic peptides anchored by a lysine side chain and to avoid the presence of two C-terminal homoserine lactones on the released linear peptides. After MALDI-TOF MS/MS analysis, the peptides released from a single bead were sequenced manually and with a de novo sequencing software. The strategy described herein is compatible with commonly used amino acids and allows sequencing of cyclic ...
Dynamic covalent chemistry (DCvC) is a synthetic strategy employed by chemists to make complex supramolecular assemblies from discrete molecular building blocks. DCvC has allowed access to complex assemblies such as covalent organic frameworks, molecular knots, polymers, and novel macrocycles. Not to be confused with dynamic combinatorial chemistry, DCvC concerns only covalent bonding interactions. As such, it only encompasses a subset of supramolecular chemistries. The underlying idea is that rapid equilibration allows the coexistence of a variety of different species among which molecules can be selected with desired chemical, pharmaceutical and biological properties. For instance, the addition of a proper template will shift the equilibrium toward the component that forms the complex of higher stability (thermodynamic template effect). After the new equilibrium is established, the reaction conditions are modified to stop equilibration. The optimal binder for the template is then extracted ...
The Chemical Biology Thematic Group is engaged in a diverse range of research topics which span structural biology, enzymology, nucleic acid research, signalling pathways, single molecule biophysics, and biophysical chemistry of living tissues. Among the themes which unite the research being performed in this group is trying to learn new chemistry and physics from biological systems. We have projects relating to pharmaceutically relevant enzymes such as those involved in drug metabolism and antibiotic resistance; development of therapeutic agents in the control of inflammation, cancer and viral infections; the chemical biology of NO; quantification of bioenergetic markers of metabolism; self-assembly mechanisms of the HIV-1 virion capsid; liposome microarray systems to address membrane protein dynamics and recognition; studies on reactive oxygen species translocation across the aqueous/lipid membrane interface; RNAi/antisense technologies; dynamic combinatorial chemistry; protein dynamics and ...
Related Articles. Structure-Based Design of Inhibitors of the Aspartic Protease Endothiapepsin by Exploiting Dynamic Combinatorial Chemistry.. Angew Chem Int Ed Engl. 2014 Feb 14 ...
The blood-brain barrier (BBB) is a biological barrier that protects the brain from neurotoxic agents and regulates the influx and efflux of molecules required for its correct function. This stringent regulation hampers the passage of brain parenchyma-targeting drugs across the BBB. BBB shuttles have been proposed as a way to overcome this hurdle because these peptides can not only cross the BBB but also carry molecules which would otherwise be unable to cross the barrier unaided. Here we developed a new high-throughput screening methodology to identify new peptide BBB shuttles in a broadly unexplored chemical space. By introducing d-amino acids, this approach screens only protease-resistant peptides. This methodology combines combinatorial chemistry for peptide library synthesis, in vitro models mimicking the BBB for library evaluation and state-of-the-art mass spectrometry techniques to identify those peptides able to cross the in vitro assays. BBB shuttle synthesis was performed by the ...
TY - JOUR. T1 - Inactivation of Bacterial DD-Peptidase by β-Sultams. AU - Llinás, Antonio. AU - Ahmed, Naveed. AU - Cordaro, Massimiliano. AU - Laws, Andrew P.. AU - Frère, Jean Marie. AU - Delmarcelle, Michael. AU - Silvaggi, Nicholas R.. AU - Kelly, Judith A.. AU - Page, Michael I.. PY - 2005/5/31. Y1 - 2005/5/31. N2 - N-Acyl-β-sultams are time-dependent, irreversible active site-directed inhibitors of Streptomyces R61 DD-peptidase. The rate of inactivation is first order with respect to β-sultam concentration, and the second-order rate constants show a dependence on pH similar to that for the hydrolysis of a substrate. Inactivation is due to the formation of a stable 1:1 enzyme-inhibitor complex as a result of the active site serine being sulfonylated by the β-sultam as shown by ESI-MS analysis and by X-ray crystallography. A striking feature of the sulfonyl enzyme is that the inhibitor is not bound to the oxyanion hole but interacts extensively with the roof of the active site where ...
SAN DIEGO-- Ligand Pharmaceuticals Incorporated (NASDAQ: LGND) today announced that it has agreed to divest and sell its combinatorial chemical library and associated proprietary technology to Venenum Biodesign, LLC, an affiliate of Medical Diagnostic Laboratories, LLC, members of Genesis Biotechnology Group (GBG), for $1.8 million. Under the terms of the agreement, Ligand will receive $1 million at the close of the transaction, $800,000 over the next two years and 10% of all revenues from third party collaborations for three years. The combinatorial chemistry asset, which Ligand obtained in the acquisition of Pharmacopeia in December 2008, comprises an encoded combinatorial library collection (ECLiPS) and an ultra-high throughput screening platform. While this screening technology was valuable in the discovery of multiple drug candidates for many of our existing collaborations, it is no longer required in the service of those collaborations and going forward it is not a priority for our ...
Fingerprint Dive into the research topics of Acyl vs Sulfonyl Transfer in N-Acyl β-Sultams and 3-Oxo-β-sultams. Together they form a unique fingerprint. ...
Hepatitis C virus (HCV) poses a major health threat to the world. The recent development of direct-acting antivirals (DAAs) against HCV has markedly improved the response rate of HCV and reduced the side effects in comparison to the interferon-based therapy. Despite this therapeutic advance, there is still a need to develop new inhibitors that target different stages of the HCV life cycle because of various limitations of the current regimens. In this study, we performed a quantitative high throughput screening of the Molecular Libraries Small Molecule Repository (MLSMR) of ∼350,000 chemicals for novel HCV inhibitors using our previously developed cell-based HCV infection assay. Following confirmation and structural clustering analysis, we narrowed down to 158 compounds from the initial ∼3000 molecules that showed inhibitory activity for further structural and functional analyses. We were able to assign the majority of these compounds to specific stage(s) in the HCV life cycle. Three of them ...
This focus review documents the developments in polymer synthesis that involve multicomponent reactions (MCRs) and related sequential reaction systems. Postpolymerization modification and step-growth polymerization reactions based on MCRs and sequential reactions such as the Kabachnik-Fields three-component reaction (KF-3CR) are described. Welcoming more participants in a polymer synthesis; recent years, multicomponent reactions (MCRs) have been gradually integrated into synthetic polymer chemistry, which led to a new synthetic toolbox for a range of interdisciplinary applications. In this focus review, this new trend in polymer chemistry has been summarized with including contributions from the author.
This paper reports the synthesis and screening of a combinatorial peptide library for new affinity ligands for glycosylated haemoglobin (HbA(1c)), which is an important indicator of diabetes control. The new ligands are suitable for large-scale synthesis and overcome the disadvantages of antibodies (unstable and expensive to produce etc.), while remaining as efficient as antibodies in binding to the analyte. The library consisted of 262 144 hexapeptides synthesised using the one-bead-one-compound technique. The hexapeptides attached onto beads were screened with glycosylated haemoglobin HbA(1c). The structures of the peptides exhibiting high affinity were characterised by Edman microsequencing. Computer modelling simulation of one of the lead sequences has shown that this class of ligand has a high affinity and specificity for glycosylated haemoglobin. (C) 1998 Elsevier Science S.A. All rights reserved.. ...
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TY - JOUR. T1 - Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M1 positive allosteric modulators. AU - Yang, Feng V.. AU - Shipe, William D.. AU - Bunda, Jaime L.. AU - Nolt, M. Brad. AU - Wisnoski, David D.. AU - Zhao, Zhijian. AU - Barrow, James C.. AU - Ray, William J.. AU - Ma, Lei. AU - Wittmann, Marion. AU - Seager, Matthew A.. AU - Koeplinger, Kenneth A.. AU - Hartman, George D.. AU - Lindsley, Craig W.. PY - 2010/1/15. Y1 - 2010/1/15. N2 - An iterative analog library synthesis approach was employed in the exploration of a quinolone carboxylic acid series of selective M1 positive allosteric modulators, and strategies for improving potency and plasma free fraction were identified.. AB - An iterative analog library synthesis approach was employed in the exploration of a quinolone carboxylic acid series of selective M1 positive allosteric modulators, and strategies for improving potency and plasma free fraction were identified.. KW - M. KW - Positive allosteric ...
Two different methods are available for synthesizing random peptide libraries. The first technique is known as Split and Mix method which consists of three basic steps: splitting, coupling and mixing. Firstly, resin beads are split in a number of aliquots that equals the number of building blocks to be utilized in the synthesis (splitting). Then, to each resin aliquot one building block is coupled and the reactions are driven to completion (coupling). Following this step, beads are randomly and thoroughly mixed (mixing) and then re-splitted in the same number of aliquots, achieving a set of homogeneous and equimolar collections of compounds. Repetitive execution of these basic steps for n times will thus produce a rapid increase of newly generated molecules, while bead number remains constant. Resin beads encounter one reactant at a time, no more than one compound per bead can be generated (one-bead one-compound-OBOC-library). As reactions are driven to completion, all peptides are generated ...
International trade is stepping into the age of digitally enabled trade, driven by cross-border data flows and interoperability. Concerns for cybersecurity, privacy, and digital sovereignty have prompted the widespread implementation of trade policies regulating cross-border data flows. At present, there is a deficit of information characterizing such policies and analyzing their role in the global economy. We address this deficit through a quantitative analysis of trade in services that seeks both to categorize data-related trade policies and to evaluate the extent to which they are similar to other restrictive measures. We propose a mixture-based clustering pipeline to group trade restrictiveness data and a method for quantifying the difference between the cross-border data flow regulations and other traditional regulations. Our analysis reveals that a significant localization effect among data flow restrictions and that, while highly restrictive data flow policies generally do not overlap with other
As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials are peer reviewed and may be re-organized for online delivery, but are not copy-edited or typeset. Technical support issues arising from supporting information (other than missing files) should be addressed to the authors. ...
Perspectives, compilations, and reviews of modern drug discovery methods:. Bunin, B. A.; Bajorath, J.; Morales, G.; Siesel, B. Cheminformatics: Theory, Practice, and Products 2006, Springer-Verlag, manuscript in press, A summary of the theory and features of the available modern cheminformatics tools.. Bunin, B. A. Increasing the Efficiency of Small Molecule Drug Discovery (In response to an interview with Chris Lipinski on current challenges) Drug Discovery Today 2003, 8, 18, 823-826.. Bunin, B. A.; Dener, J. M.; Livingston, D. A. Application of Combinatorial and Parallel Synthesis to Medicinal Chemistry Annu. Rep. Med. Chem. 1999, 34, 267-286.. Bunin, B. A. The Combinatorial Index 1998, pp. 1-322, Academic Press, An exhaustive compilation on methods for the combinatorial synthesis of small molecules widely used by synthetic chemists.. Morales, G. A.; Bunin, B. A. Guest Editors, Comb. Chem. & HTS., 2004, 7, 5. 397-529. Morales, G. A.; Bunin, B. A. Editors, Methods Enzymol., 2003, 369, ...
The selection, acquisition, and use of high‐quality small molecule libraries for screening is an essential aspect of drug discovery and chemical biology programs
DNA-encoded chemical libraries (DEL) is a technology for the synthesis and screening on unprecedented scale of collections of small molecule compounds. DEL is used in medicinal chemistry to bridge the fields of combinatorial chemistry and molecular biology. The aim of DEL technology is to accelerate the drug discovery process and in particular early phase discovery activities such as target validation and hit identification. DEL technology involves the conjugation of chemical compounds or building blocks to short DNA fragments that serve as identification bar codes and in some cases also direct and control the chemical synthesis. The technique enables the mass creation and interrogation of libraries via affinity selection, typically on an immobilized protein target. A homogeneous method for screening DNA-encoded libraries has recently been developed which uses water-in-oil emulsion technology to isolate, count and identify individual ligand-target complexes in a single-tube approach. In contrast ...
Search for Identifying A Library Member By Means Of A Tag, Label, Or Other Readable Or Detectable Entity Associated With The Library Member (e.g., Decoding Process, Etc.) Patents and Patent Applications (Class 506/4) Filed with the USPTO
Combinatorial synthesis is an efficient tool that can be used to discover new materials. It allows one to systemically study a large number of materials simultaneously as their physical properties change with the varying chemical composition. Using this technique, we study various multifunctional electronic materials. Different designs of libraries, such as discrete libraries and composition spreads, are fabricated and characterized in order to rapidly map composition-structure-property relationships in a variety of systems. We have made gas sensor device libraries to optimize the performance of gas sensing materials. We have utilized the combinatorial pulsed laser deposition (PLD) flange for fabricating the discrete device library of doped SnO2 thin films. Several libraries were made with different amounts of dopants such as In2O3, WO3, ZnO, Pt, and Pd. After exposing the whole library to chloroform, formaldehyde, and benzene gases, the compositions most sensitive to these gases were found. We ...
The Group of Nanomaterials and Microsystems has established as its main research goal the synergy between basic research in Nanoscience and Nanotechnology with the technological development of new tools to prepare and characterize materials at the nanoscale. The GNaM is one of the few groups in Europe working in nanocalorimetry of low dimensional systems and in the combinatorial synthesis and characterization of thin layers prepared by physical vapour deposition (PVD). Our group has also a wide experience in the study of transformation kinetics associated to nucleation and growth processes. Simultaneously, the group has developed and patented a high throughput analysis methodology based on membrane-based microchips to the study of phase transformations in thin films. The innovative and efficient synergy between synthesis and thermal characterization tools has brought the GNaM to an international recognition in the area of Nanoscience and Nanotechnology. Our team is formed by Javier Rodr guez Viejo,
UOP LLC, a Honeywell Company, Ford Motor Company, and Striatus, Inc., collaborated with Professor Craig Jensen of the University of Hawaii and Professor Vidvuds Ozolins of University of California, Los Angeles on a multi-year cost-shared program to discover novel complex metal hydrides for hydrogen storage. This innovative program combined sophisticated molecular modeling with high throughput combinatorial experiments to maximize the probability of identifying commercially relevant, economical hydrogen storage materials with broad application. A set of tools was developed to pursue the medium throughput (MT) and high throughput (HT) combinatorial exploratory investigation of novel complex metal hydrides for hydrogen storage. The assay programs consisted of monitoring hydrogen evolution as a function of temperature. This project also incorporated theoretical methods to help select candidate materials families for testing. The Virtual High Throughput Screening served as a virtual laboratory, calculating
Autori: Oprea, Tudor I.; Zamora, Ismael; Ungell, Anna-Lena. Editorial: Journal of Combinatorial Chemistry, 4, p.258-266, 2002.. Rezumat:. ChemGPS, the chem. global positioning system, is a tool that combines rules (equiv. to dimensions) and objects (chem. structures) to provide a consistent chem. space map (Oprea, T. I.; Gottfries, J. J. Comb. Chem. 2001, 3, 157-166.). Rules included, initially, general properties such as size, lipophilicity, and hydrogen bond capacity, while objects include „satellites, intentionally placed outside the druglike space, as well as „core objects, mostly orally available drugs. ChemGPS mols. (objects) were used in conjunction with the VolSurf (http://www.moldiscovery.com) descriptors (rules), which are relevant for ADME (absorption, distribution, metab., and excretion) properties. The combination of ChemGPS and VolSurf, GPSVS, was investigated with respect to the biopharmaceutics classification system, which is recommended by the Food and Drug Administration ...
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Autor: Müller, Oliver et al.; Genre: Zeitschriftenartikel; Im Druck veröffentlicht: 2004; Keywords: bioorganic chemistry • combinatorial chemistry • library screening • medicinal chemistry • signal transduction; Titel: Identification of potent Ras signaling inhibitors by pathway-selective phenotype-based screening
article {Drake:2002:1386-2073:201, title = Optimisation of Polystyrene Resin-supported Pt Catalysts in Room Temperature, Solvent-less, Oct-l-ene Hydrosilylation using Methyldichlorosilane, journal = Combinatorial Chemistry & High Throughput Screening, parent_itemid = infobike://ben/cchts, publishercode =ben, year = 2002, volume = 5, number = 3, publication date =2002-05-01T00:00:00, pages = 201-209, itemtype = ARTICLE, issn = 1386-2073, url = https://www.ingentaconnect.com/content/ben/cchts/2002/00000005/00000003/art00003, doi = doi:10.2174/1386207024607293, keyword = pt catalyst, solid phase peptide synthesis, solid support, polystyrene resin-support, author = Drake, R. and Dunn, R. and Sherrington, D.C. and Thomson, S.J., abstract = Six precursor resins with systematic variation of porous parameters were prepared by suspension polymerisation using specific compositions of divinylbenzene, styrene vinylbenzyl chloride (VBC) and 2- ethylhexan-l-ol (a porogen). ...
I think that the reason for this lack of interest in solubility measurements relates to the way synthetic organic chemists have learned to think about their workflows. Generally, the researcher sets up an experiment with the intention of preparing and isolating a specific compound. The role of the solvent is usually just to solubilize the reactants - it is then commonly evaporated for chromatographic purification of the product. Even in combinatorial chemistry experiments where products are not purified for a rough screening, the expectation is that compounds of interest will be purified and characterized at some point ...
Malaria is responsible for 300 million cases a year, resulting in 1 million deaths. From a military perspective, maintaining bases in regions where the disease is endemic puts troops at risk for infection. Whether for civilian or military populations,the fact remains that insecticide tolerant mosquitoes, drug resistant parasites and lack of effective vaccines necessitate new approaches to combating this scourge. Emerging information about the genetics of these organisms, primarily through advances inwhole-genome and expression analysis, provides a knowledge base to investigate new opportunities for disease prevention. Genetic approaches are complemented by technological advances in high-throughput screening and combinatorial chemistry that, together,enable a means to synthesize and rapidly screen prospective drug leads. In this Phase I proposal, Agave BioSystems proposes to develop a validated protocol for the isolation of shikimate pathway genes from P. falciparum, the causative agent of ...
Location: Montr al, Quebec, Canada. Daniel Chelsky, PhD, is the chief scientific officer at Caprion, a company using mass spectrometry and multiparametric flow cytometry to discover and validate biomarkers of disease and drug efficacy, drug mechanism of action and new targets for disease intervention. Previously he served as president of BioSignal, Inc., a subsidiary of PerkinElmer focused on G-protein coupled receptor related research and reagents.. He has also held positions as senior director of biology at Pharmacopeia, a combinatorial chemistry company, director of drug discovery at Onyx Pharmaceuticals, and principal investigator at DuPont Merck Pharmaceuticals. He received his PhD at the University of Oregon and was an American Cancer Society fellow at the University of California, Berkeley.. ...
A variety of proven techniques, such as filtration, dialysis, liquid/liquid extraction and Solid Phase Extraction (SPE), are routinely adopted in todaylj analytical laboratories to resolve the vast array of sample preparation demands. SPE has established itself as one of the most popular and flexible tools within the analytical laboratory; providing effective, efficient sample concentration and purification prior to HPLC, LC/MS, GC or GC/MS and adaptation to automated techniques such as combinatory chemistry. The resultant SPE product range provides unparalleled performances and satisfies the clients demand for Recovery, Reliability and Reproducibility ...
Chapter 1: Combinatorial Materials Science: Measures of Success (Michael J. Fasolka and Eric J. Amis). Chapter 2: Experimental Design in High Throughput Systems (James N. Cawse).. Chapter 3: Polymeric Discrete Libraries for High-Throughput Materials Science: Conventional and Microfluidic Library Fabrication and Synthesis (Kathryn L. Beers and Brandon M. Vogel).. Chapter 4: Strategies in the Use of Atomic Force Microscopy as a Multiplexed Readout Tool of Chip-Scale Protein Motifs (Jeremy R. Kenseth, Karen M. Kwarta, Jeremy D. Driskell, and Marc D. Porter, John D. Neill and Julia F. Ridpath).. Chapter 5: Informatics Methods for Combinatorial Materials Science (Changwon Suh, Krishna Rajana, Brandon M. Vogel, Balaji Narasimhan, and Surya K. Mallapragada).. Chapter 6: Combinatorial Approaches and Molecular Evolution of Homogeneous Catalysts (L. Keith Woo).. Chapter 7: Biomaterials Informatics (Nicole K. Harris, Joachim Kohn, W.J. Welsh, and Doyle Knight).. Chapter 8: Combinatorial Methods and their ...
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An efficient method to synthesize positional scanning synthetic combinatorial libraries (PS-SCLs) for studying the specificity of protein kinases is presented. Isokinetic ratios for pentafluorophenyl esters were determined iteratively using a new approach incorporating high performance liquid chromatography (HPLC) quantification and statistical experimental design. In the development process a large amount of work was put in to find efficient ways of screening for new isokinetic mixtures and to optimize the process of PS-SCL synthesis. The newly developed methods for the screening of isokinetic mixtures could be used for the screening of other interesting mixtures, but more importantly, the isokinetic ratios determined for the preactivated pentafluorophenyl esters were incorporated into a new efficient protocol. This straightforward protocol allows for a convenient synthesis of high quality PS-SCLs regardless of previous experience in solid phase synthesis.
Real-time reaction monitoring based on a combination of thin-layer chromatography (TLC) and compact mass spectrometry (CMS) is a simple and quick way for chemists to overcome synthetic challenges and optimize chemical reactions in the modern laboratory. Peptides of pharmaceutical interest can be readily synthesized following a rapid, continuous solution-phase synthesis strategy based on Fmoc protected amino acid building blocks. A simple model for such a reaction is the growing of analogues of the acyl carrier protein (ACP), a component of the fatty acid synthesis pathway.. ...
Diffusion ordered spectroscopy (DOSY) NMR experiments have been used to characterize a dynamic combinatorial library of helical strands and grid-type metallosupramolecular architectures. The technique allows the deconvolution of very similar chemical structures differing only by their hydrodynamic radius. Moreover, the occurrence of springlike, extension-contraction conformational motions in helical strands can be revealed as a function of the temperature. ...
Sorrento Therapeutics, Inc. (OTC Bulletin Board: SRNE) today announced that it has completed the construction of an extensive library of full-length, fully human monoclonal antibodies
Deubiquitinases (DUBs) have been proposed as therapeutic targets in cancer due to their ability to alter degradation rates of known oncoproteins. However, previous efforts to develop potent and selective DUB inhibitors have been largely unsuccessful. In this work, we develop a target class drug discovery platform targeting DUBs, which incorporates small molecule libraries, enzyme libraries, and a suite of structural and functional activity assays. Using this platform, we demonstrate one of the first examples of potent and selective DUB inhibitor development, targeting USP7 (chapter II). We then use our potent USP7 inhibitors (chapter III) as well as our annotated DUB-wide small molecule library (chapter IV) in a series of cellular assays to identify novel biological function of USP7 (chapter III) and USP10 (chapter IV). Finally, we describe our efforts to improve and expand our current target class library in order to continue to identify novel DUB inhibitors and DUB biology. ...
We present LoFT, a tool for focused combinatorial library design. LoFT provides a set of algorithms, constructing a focused library from a chemical fragment space under optimization of multiple design criteria. A weighted multiobjective scoring function based on physicochemical descriptors is employ …
One of the first steps towards elucidating the biological function of a putative transcriptional regulator is to ascertain its preferred DNA-binding sequences. This may be rapidly and effectively achieved through the application of a combinatorial approach, one involving very large numbers of randomized oligonucleotides and reiterative selection and amplification steps to enrich for high-affinity nucleic acid-binding sequences. Previously, we had developed the novel combinatorial approach Restriction Endonuclease Protection, Selection and Amplification (REPSA), which relies not on the physical separation of ligand-nucleic acid complexes but instead selects on the basis of ligand-dependent inhibition of enzymatic template inactivation, specifically cleavage by type IIS restriction endonucleases. Thus, no prior knowledge of the ligand is required for REPSA, making it more amenable for discovery purposes. Here we describe using REPSA, massively parallel sequencing, and bioinformatics to identify the
ACS Short Course Computational Chemistry and Computer-Assisted Drug Design: Practical Approaches 230th ACS National Meeting Washington Convention Center, Washington, DC Friday-Saturday, August 26-27, 2005 This introductory level course is designed for organic chemists, pharmaceutical chemists, and biochemists who are interested in learning more about computational and combinatorial methods, or scientists who need to develop a working knowledge of the fundamentals and need to understand the concepts and terminology of this rapidly developing area. Program Overview of Computational Chemistry and Computer-Assisted Drug Design Molecular Mechanics: Background, Development, Concepts, Force Fields Conformational Searching Molecular Dynamics Simulations: Background, Development, Concepts, and Applications Protein Structure Prediction Overview of Quantum Chemistry Methods and Its Application to Drug Design DNA and Protein Sequence and Structure Analysis Drug Design Methods and Pharmacophore Design QSAR ...
Good methods must be reliable, well-tested, and honed to minimize the time and expense required to achieve the desired results. CPNC provides a continuously growing and evolving set of protocols that allows researchers to benefit from the experience of other researchers around the world. The core manual provides a comprehensive set of protocols that have been compiled, revised, and streamlined over the last 6 years. Quarterly updates provide new protocols in emerging areas of research as well as continued advances and new applications for fundamental methods. The book is designed to grow and change with the field of nucleic acid chemistry. Fundamental nucleoside chemistry methods include sugar-base condensation, phosphorylation, and nucleoside protection. Methods for oligonucleotide synthesis include H-phosphonate and phosphoramidite approaches, solid-phase and solution-phase synthesis, large-scale synthesis, synthesis for modified and unmodified oligonucleotides, conjugation of ...
MALT1 inhibitors are promising therapeutic agents for B-cell lymphomas dependent on constitutive or aberrant signaling pathways. However, a potential limitation for signal transduction targeted therapies is the occurrence of feedback mechanisms that enable escape from the full impact of such drugs. Here, we used a functional genomics screen in ABC-DLBCL cells treated with a small molecule irreversible inhibitor of MALT1 to identify genes that might confer resistance or enhance the activity of MALT1 inhibition. We find that loss of BCR and PI3K activating proteins enhanced sensitivity, while loss of negative regulators of these pathways (e.g. TRAF2, TNFAIP3) promoted resistance. These findings were validated by knockdown of individual genes and a combinatorial drug screen focused on BCR and PI3K pathway targeting drugs. Among these, the most potent combinatorial effect was observed with PI3Kd inhibitors against ABC-DLBCLs in vitro and in vivo, but which led to an adaptive increase in p-S6 and ...
Mark Wheelis Biology is in the midst of what can only be described as a revolution. It began in the mid-1970s with the development of recombinant DNA technology. Slowly at first but with increasing speed, related technologies have been developed that have dramatically expanded the experimental capabilities of modern research biologists and that are rapidly being adopted in such areas of applied biology as drug development. These new technologies include genomics, proteomics, microarray technology, high-throughput screening techniques, combinatorial methods in both chemistry and biology, site-specific mutagenesis, knock-out mice, and many others.[1] Collectively, these technologies are referred to as genomic sciences, or the new biology.. This technology will have great power both for peaceful and hostile uses. Peaceful applications will include a wide range of new therapeutic agents of much greater specificity and safety than are currently available; hostile applications could include a wide ...
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One of the most important roles mathematics plays in the world is that of reducing complex problems to simple algorithms that either someone of a computer could follow to a desired solution. In many, many real world applications, the object is to find the least expensive, or the most environmentally safe, or the fastest solution from a huge number of possible solutions. There are certain optimization problems that become unmanageable using combinatorial methods as number of objects becomes large. For example, finding an optimal solution to the Traveling Salesman Problem (TSP) optimization problem could be an incredibly difficult task, often practically impossible. Because when you increase the number of cities, you need to search through an enormous number of possible solutions in order to find the optimal one. In this case because we cant realistically expect to find the optimal one within a sensible length of time, we have to settle for something that is close enough. Simulated Annealing ...
These techniques are complemented by laboratory methods from combinatorial chemistry, molecular biology and functional genomics ... statistical analysis and chemoinformatic techniques, a recent and innovative international concept registered under the name " ...
A Powerful New Technique for Identifying Privileged Molecular Fragments with Useful Applications in Combinatorial Chemistry". ... RECAP (Retrosynthetic Combinatorial Analysis Procedure) uses SMARTS to define bond types. RECAP is a molecule editor which ... Methods and Principles in Medicinal Chemistry. pp. 271-285. doi:10.1002/3527603743.ch11. ISBN 9783527307531. Lyne, Paul D.; ... Lewell, Xiao Qing; Judd, Duncan B.; Watson, Stephen P.; Hann, Michael M. (1998). "RECAPRetrosynthetic Combinatorial Analysis ...
A Powerful New Technique for Identifying Privileged Molecular Fragments with Useful Applications in Combinatorial Chemistry". ... Lewell, Xiao Qing; Judd, Duncan B.; Watson, Stephen P.; Hann, Michael M. (1998). "RECAP-Retrosynthetic Combinatorial Analysis ... Molecular structure input on the web The Chemical Structure Editor: Bridging Chemistry and Cheminformatics. ... Methods and Principles in Medicinal Chemistry. pp. 271-285. doi:10.1002/3527603743.ch11. ISBN 9783527307531. ...
"Perspective articles on the utility and application of solution-phase combinatorial". Journal of Combinatorial Chemistry. 2 (2 ... Reaction may be monitored: The purification process is controlled Traditional purity techniques may be employed Can be used in ... Used primarily in the synthesis of medicinal drugs, solution-phase combinatorial chemistry allows for the creation of large ... Carlisle, Steven J. , Marsh, Andrew, Smith, S.C. (2001). "High-loading scavenger resins for combinatorial chemistry". ...
DEL is used in medicinal chemistry to bridge the fields of combinatorial chemistry and molecular biology. The aim of DEL ... The technique enables the mass creation and interrogation of libraries via affinity selection, typically on an immobilized ... Combinatorial Chemistry 20 years on.., Drug DiscovToday 7; 1-4. Brenner S, Lerner RA (June 1992). "Encoded combinatorial ... Genetic manipulation of combinatorial chemistry libraries for small-molecule evolution". PLOS Biology. 2 (7): E174. doi:10.1371 ...
"For outstanding achievement in creative chemistry." Eli Lilly Award in Biological Chemistry, ACS (1993). "For fundamental ... DOS pathways and new techniques for small-molecule screening provided many new, potentially disruptive insights into biology. ... combinatorial synthesis and the so-called Build/Couple/Pair strategy of modular chemical synthesis. ... Chemistry departments have changed their names to include the term chemical biology and new journals have been introduced (Cell ...
... she developed combinatorial chemistry and molecular graphics techniques and was involved in the development of software ... She was the only woman to be a chemistry/zoology major in her year. From 1958 to 1960 she worked as a pharmacology assistant at ... Editorially, she has worked on Perspectives in Drug Design and Discovery, QSAR: Annual Reports in Computational Chemistry, ... She has also significantly contributed to the development of compound collections and combinatorial libraries which ...
The advent of combinatorial chemistry has enabled medicinal chemists to synthesize and identify large numbers of potential ... Micellar electrokinetic chromatography (MEKC) is a chromatography technique used in analytical chemistry. It is a modification ... Simms, P.J.; Jeffries, C.T.; Huang, Y.; Zhang, L.; Arrhenius, T.; Nadzan, A.M. (2001). "Analysis of Combinatorial Chemistry ... In MEKC, however, techniques must be used to extend the elution range to separate strongly retained analytes. Elution ranges ...
... chemistry). Operations research provides techniques for solving practical problems in engineering, business, and other fields ... Discrete geometry and combinatorial geometry are about combinatorial properties of discrete collections of geometrical objects ... Operations research techniques include linear programming and other areas of optimization, queuing theory, scheduling theory, ... ISBN 978-0-13-045803-2. Kenneth H. Rosen; John G. Michaels (2000). Hand Book of Discrete and Combinatorial Mathematics. CRC ...
... is a combinatorial chemistry technique in molecular biology for producing oligonucleotides of either single-stranded DNA or RNA ... Combinatorial Chemistry & High Throughput Screening. 9 (8): 619-32. doi:10.2174/138620706778249695. PMID 17017882. Daniels DA, ... The technique has been used to evolve aptamers of extremely high binding affinity to a variety of target ligands, including ... Clinical uses of the technique are suggested by aptamers that bind tumor markers, GFP-related fluorophores, and a VEGF-binding ...
Similar to combinatorial chemistry, compounds are produced by biosynthesis rather than organic chemistry. This process was ... Combinatorial biology techniques generally begin with large numbers of peptides, which are generated and screened by physically ... In biotechnology, combinatorial biology is the creation of a large number of compounds (usually proteins or peptides) through ... Combinatorial biology allows the generation and selection of the large number of ligands for high-throughput screening. ...
Quite a few of available ones are already described Materials science has applied the techniques of combinatorial chemistry to ... formerly Journal of Combinatorial Chemistry) Combinatorial Chemistry Review Molecular Diversity Combinatorial Chemistry and ... The methods used in combinatorial chemistry are applied outside chemistry, too. Combinatorial chemistry had been invented by ... "The concealed side of the history of combinatorial chemistry" IUPAC's "Glossary of Terms Used in Combinatorial Chemistry" ACS ...
... or from historic chemical compound collections or libraries created through combinatorial chemistry. While a number of ... approaches toward the identification and development of hits exist, the most successful techniques are based on chemical and ... Medicinal chemistry and pharmaceutical chemistry are disciplines at the intersection of chemistry, especially synthetic organic ... Royal Society of Chemistry. doi:10.1039/9781782621836. ISBN 978-1-78262-419-6. Roland Barret (2018). Medicinal Chemistry: ...
Several analytical techniques have been applied to the analysis of protein-directed DCL. These include HPLC, mass spectrometry ... Protein-directed dynamic combinatorial chemistry. In Dynamic combinatorial chemistry: in drug discovery, bioinorganic chemistry ... Center for Dynamic Combinatorial Chemistry[citation needed] University of Cambridge: Dynamic Combinatorial Chemistry. ... Bridge from supramolecular chemistry to adaptive chemistry. Constitutional Dynamic Chemistry. Topics in Current Chemistry. 322 ...
"Combinatorial chemistry in the agrosciences". Bioorganic & Medicinal Chemistry. 17 (12): 4035-46. doi:10.1016/j.bmc.2009.03.027 ... "Screening technique uncovers five new plant activator compounds". Phys.org. Retrieved 2014-02-11. Noutoshi Y, Okazaki M, Kida T ... The sources of new molecules employ natural products, competitors, universities, chemical vendors, combinatorial chemistry ... Techniques such as fragment-based design, virtual screening and genome sequencing have helped generate drug leads. Published ...
... the application of high throughput and combinatorial approaches and biophysical chemistry, which focuses on the development and ... application of physicochemical techniques to biological systems. Chemical Physics/Physical Chemistry is the fundamental study ... The Materials Chemistry group is one of the largest materials chemistry groups in the UK. Areas of strength include the design ... "RAE 2008: chemistry results". The Guardian. 18 December 2008. Retrieved 7 March 2019. "History of Chemistry - Is this going to ...
Protein-directed dynamic combinatorial chemistry". In Miller BL (ed.). Dynamic combinatorial chemistry: in drug discovery, ... Nuclear magnetic resonance spectroscopy is the primary technique for determining chemical structures of natural products. NMR ... selection of different binders from the same uridine-based dynamic combinatorial library". Journal of Combinatorial Chemistry. ... Despite the rise of combinatorial chemistry as an integral part of lead discovery process, natural products still play a major ...
... protein-directed dynamic combinatorial chemistry and organic synthesis/medicinal chemistry. Most clinically used antibiotics ... Techniques involved in this interdisciplinary research include proteomics, X-ray crystallography, nuclear magnetic resonance ( ... In 1998, he became professor of Chemistry, and in 2011 he was appointed the Head of Organic Chemistry at the Department of ... Chris Schofield is a professor of organic chemistry at the University of Oxford, Department of Chemistry and a Fellow of ...
Journal of Combinatorial Chemistry, 7, 921-928, 2005. B.M. Vogel and S.K. Mallapragada, "The Synthesis of Polyanhydrides", in ... "Polyanhydride Synthesis Techniques." Wyatt Technology Corp. http://www.lightscattering.com/literature/polyanhydride.pdf[ ... These classes are determined by examining their R groups (the chemistry of the molecule between the anhydride bonds). Aliphatic ...
Physical chemistry and chemical physics: Chemistry investigated via physical methods like laser techniques, scanning tunneling ... Examples are molecular docking, protein-protein docking, drug design, combinatorial chemistry. The fitting of shape and ... Theoretical chemistry is the branch of chemistry which develops theoretical generalizations that are part of the theoretical ... Theoretical chemistry unites principles and concepts common to all branches of chemistry. Within the framework of theoretical ...
Some more narrow interpretations include combinatorial chemistry, Process Modeling, materials property databases, materials ... This lack of big data has led to growing effort in developing machine learning techniques that utilize data extremely data sets ...
Nasir M (1999). "Fluorescence Polarization: An Analytical Tool for Immunoassay and Drug Discovery". Combinatorial Chemistry & ... Despite originating as a method for direct interaction studies, the technique has been adopted by high-throughput screening ( ... Jameson D (2003). "Fluorescence Polarization: Past, Present and Future". Combinatorial Chemistry & High Throughput Screening. 6 ... Eremin SA, Smith DS (May 2003). "Fluorescence polarization immunoassays for pesticides". Combinatorial Chemistry & High ...
The method of choice is generally phosphoramidite chemistry, developed in the 1980s. Combinatorial chemistry Noncovalent solid- ... Solid-phase synthesis is a common technique for peptide synthesis. Usually, peptides are synthesised from the carbonyl group ... Solid-Phase Combinatorial Chemistry, see [1] N-(pyrimidin-2-yl)amino acid amides in drug research, see Full article. ... More recently, this method has also been used in combinatorial chemistry and other synthetic applications. The process was ...
The CombiMatrix microarray ("CombiMatrix" refers to combinatorial chemistry on a matrix array) was born and received US patents ... CombiMatrix performs genetic testing utilizing a variety of advanced cytogenomic techniques, including chromosomal microarray ...
Combinatorial chemistry Congener Conformation activity relationship Quantitative structure-activity relationship Pharmacophore ... Medicinal chemists use the techniques of chemical synthesis to insert new chemical groups into the biomedical compound and test ... Environmental Toxicology and Chemistry. 5 (6): 503-509. doi:10.1002/etc.5620050601. Alexander, Martin; Lustigman (1966). " ...
... is one of the most powerful spectroscopic techniques in analytical chemistry. It is an important tool for the studies of host- ... and by doing so hope to gain further insight into the combinatorial outcome of these many, small, non-covalent forces that are ... Host-guest chemistry is a branch of supramolecular chemistry in which a host molecule forms a chemical compound with a guest ... In supramolecular chemistry, host-guest chemistry describes complexes that are composed of two or more molecules or ions that ...
Druglikeness Protein-directed dynamic combinatorial chemistry Lipinski's rule of five Price AJ, Howard S, Cons BD (November ... FBLD is a technique being used in research for discovering novel potent inhibitors. This methodology could help to design ... Many biophysical techniques have been applied to address this issue. In particular, ligand-observe nuclear magnetic resonance ( ... Topics in Current Chemistry. 317. pp. 1-32. doi:10.1007/128_2011_180. ISBN 978-3-642-27539-5. PMID 21695633. Edward Zartler; ...
in chemistry and physics at Chinese University of Hong Kong in 1969. She earned a Ph.D. in inorganic and physical chemistry at ... Structural studies involve synchrotron X-ray and neutron diffraction techniques. In 2000, Wong-Ng became a fellow of the ... and high throughput combinatorial approach for novel materials discovery and property optimization for energy conversion ... Wong-Ng was a research associate and lecturer in the chemistry department at University of Toronto. From 1981 to 1985, she was ...
Ernesto Julio Calvo, Professor of Physical Chemistry, University of Buenos Aires: A study of self-assembled proteins at ... John Stembridge, Professor of Mathematics, University of Michigan: Combinatorial aspects of root systems and Weyl characters. ... New query and search techniques for the Internet. Jennette Williams, Photographer, New York City; Instructor in Photography, ... Robert J. Hamers, Evan P. Helfaer Professor of Chemistry, University of Wisconsin-Madison: Studies in molecular electronics. ...
FISH is a very general technique. The differences between the various FISH techniques are usually due to variations in the ... For miRNA detection, the probes use proprietary chemistry for specific detection of miRNA and cover the entire miRNA sequence. ... Three primary fluorophores are able to generate a total of 7 readily detectable emission spectra as a result of combinatorial ... This technique is used routinely in telomere length research. Flow-FISH[edit]. Flow-FISH uses flow cytometry to perform FISH ...
She along with her husband, Frédéric Joliot-Curie, was awarded the Nobel Prize for Chemistry in 1935.[173][174] ... Melanie Klein (1882-1960): Austrian-born British psychoanalyst who devised novel therapeutic techniques for children that ... combinatorial game theory and coding theory. He is best known for the invention of the cellular automaton called Conway's Game ... Creations of Fire: Chemistry's Lively History from Alchemy to the Atomic Age. New York: Plenum, 1995. Print. "But Nobel, both ...
"Journal of Biological Chemistry. 286 (10): 7737-7743. doi:10.1074/jbc.C110.209288. PMC 3048661. PMID 21257745.. ... Berlec, Aleš (2012-09-01). "Novel techniques and findings in the study of plant microbiota: Search for plant probiotics". Plant ... This combinatorial approach enables a systems-level understanding of microbial contributions to human biology.[27] But also ... "Identifying gut microbe-host phenotype relationships using combinatorial communities in gnotobiotic mice". Sci. Transl. Med. 6 ...
This technique can be used to obtain the power of a positive real number b for any irrational exponent. The function fb(x) = bx ... Combinatorial interpretationEdit. See also: Exponentiation over sets. For nonnegative integers n and m, the value of nm is the ... Exponentiation is used extensively in many fields, including economics, biology, chemistry, physics, and computer science, with ...
"The Journal of Biological Chemistry. 280 (5): 3946-53. doi:10.1074/jbc.M407876200. PMC 2947832. PMID 15556947.. ... Prospects as a therapeutic techniqueEdit. This section needs to be updated. Please update this article to reflect recent events ... providing a combinatorial therapeutic approach with chemotherapy.[155] Another potential RNAi-based treatment is to inhibit ... Such techniques take advantage of the stable and heritable RNAi phenotype in plant stocks. Cotton seeds are rich in dietary ...
In combination with combinatorial chemistry, high-throughput screening, and building chemical libraries, click chemistry has ... These techniques represent a part of the field of chemical biology, in which click chemistry plays a fundamental role by ... Metal-free click chemistry review. *Click Chemistry - a Chem Soc Rev themed issue highlighting the latest applications of click ... Now limitations emerge from the chemistry of the probe to its target. In order for this technique to be useful in biological ...
"The Journal of Biological Chemistry. 285 (25): 19637-19646. doi:10.1074/jbc.M110.117382. PMC 2885242 . PMID 20400508.. ... Rosetta Antibody is a novel antibody FV region structure prediction server, which incorporates sophisticated techniques to ... "Immunoglobulin purification by affinity chromatography using protein A mimetic ligands prepared by combinatorial chemical ... "Bioconjugate Chemistry. 27 (5): 1390-1399. doi:10.1021/acs.bioconjchem.6b00164. PMC 4916912 . PMID 27064381.. ...
Recently, a technique using non-mutagenic LED lights[60] have been developed for macro-photography.[61] The technique uses an ... "The Journal of Biological Chemistry. 279 (13): 13044-53. doi:10.1074/jbc.M312846200. PMID 14722062.. ... "Transgenic strategies for combinatorial expression of fluorescent proteins in the nervous system". Nature. 450 (7166): 56-62. ... Scientists Roger Y. Tsien, Osamu Shimomura, and Martin Chalfie were awarded the 2008 Nobel Prize in Chemistry on 10 October ...
Applications in chemistry, geology and astrobiology[edit]. Main articles: Biosignature, Biomolecule, and Biomarker (petroleum) ... The field of biomarker research is also expanding to include a combinatorial approach to identifying biomarkers from multi-omic ... Trends in Analytical Chemistry. 100: 7-14. doi:10.1016/j.trac.2017.12.015.. ...
The Royal Society of Chemistry. pp. 1-18. doi:10.1039/9781847551658. ISBN 978-0-85404-306-4. .. ... Natural fluorescence (Many optical dosimetry techniques, such as fluorescence spectroscopy, depend on fluorescence.)[14] ... 1 and combinatorial phototherapy with dual photothermal and photodynamic therapeutic mechanisms that may be appropriate for ... The Journal of Physical Chemistry B. 109 (18): 8570-8573. doi:10.1021/jp051163i. PMID 16852012.. CS1 maint: Multiple names: ...
Clue to chemistry of heredity found The New York Times June 1953. First American newspaper coverage of the discovery of the DNA ... These techniques, especially multiple sequence alignment, are used in studying phylogenetic relationships and protein function. ... They are mostly single stranded DNA sequences isolated from a large pool of random DNA sequences through a combinatorial ... Beckman KB, Ames BN (August 1997). "Oxidative decay of DNA". The Journal of Biological Chemistry. 272 (32): 19633-36. doi: ...
Optical detection includes fluorescence-based techniques, chemiluminescence-based techniques, and surface plasmon resonance ( ... Surface chemistry of polymers can also be modified for specific applications. The most common polymers used in bio-MEMS include ... Using ECM microarrays to optimize combinatorial effects of collagen, laminin, and fibronectin on stem cells is more ... Conventional micromachining techniques such as wet etching, dry etching, deep reactive ion etching, sputtering, anodic bonding ...
This technique could be useful for the treatment of malignant tumors as it is non-invasive and specific. A molecular logic gate ... In another XOR logic gate system the chemistry is based on the pseudorotaxane [5] depicted in scheme 3. In organic solution the ... field has advanced from simple logic systems based on a single chemical or physical input to molecules capable of combinatorial ... specific concentration threshold of each input must be reached to achieve a fluorescent output in accordance with combinatorial ...
Laboratories devoted to activities such as high-throughput screening, combinatorial chemistry, automated clinical and ... "Clinical Chemistry 46, No. 5, 2000, pgs. 246-250" (PDF). Archived (PDF) from the original on 2011-06-07. Retrieved 2009-02-20. ... of the American Association for Clinical Chemistry,[5][6] which later evolved into an area committee of the Clinical and ... Laboratory techniques. *Laboratory equipment. *Robotics. *Laboratory robots. Hidden categories: *All articles with dead ...
... most recently to the field of dynamic combinatorial chemistry at the forefront of supramolecular chemistry". - ... especially his development and application of techniques for the computation of molecular wave-functions and properties". [114] ... "In recognition of his leading work in inorganic chemistry, particularly his major impact on the chemistry of transition metals ... "In recognition of his many notable contributions to organic chemistry, especially to the chemistry of natural products of ...
Ghosh D, Papavassiliou AG (2005). "Transcription factor therapeutics: long-shot or lodestone". Current Medicinal Chemistry. 12 ... This technique relies on chemical fixation of chromatin with formaldehyde, followed by co-precipitation of DNA and the ... the combinatorial use of a subset of the approximately 2000 human transcription factors easily accounts for the unique ...
A Practical Combinatorial Auction Design". In Combinatorial Auctions, Edited by Cramton, P., Shoham, Y., and Steinberg, R. MIT ... Due to the influence of Milgrom and Shannon's paper and related research by Milgrom and others, these techniques, now often ... In their 1987 paper, Holmstrom and Milgrom introduced new techniques for studying multidimensional agency problems. The key ... In Combinatorial Auctions. MIT press: 17-40. CiteSeerX 10.1.1.120.7158. doi:10.7551/mitpress/9780262033428.003.0002. ISBN ...
... for which they won the 1952 Nobel Prize in Chemistry.[6] They established the principles and basic techniques of partition ... "Pure and Applied Chemistry. 65 (4): 819-872. doi:10.1351/pac199365040819.. *^ Manish T. "How does column chromatography work?" ... simulated moving bed technique was proposed. In the simulated moving bed technique instead of moving the bed, the sample inlet ... Techniques by physical state of mobile phase[edit]. Gas chromatography[edit]. Further information: Gas chromatography ...
"The Journal of Biological Chemistry. 280 (5): 3946-53. doi:10.1074/jbc.M407876200. PMC 2947832. PMID 15556947.. ... Such techniques take advantage of the stable and heritable RNAi phenotype in plant stocks. Cotton seeds are rich in dietary ... providing a combinatorial therapeutic approach with chemotherapy.[155] Another potential RNAi-based treatment is to inhibit ... Prospects as a Therapeutic TechniqueEdit. Clinical Phase I and II studies of siRNA therapies conducted between 2015 and 2017 ...
Role of imaging techniques in the diagnosis of dementia. „Br J Radiol". 80 (Spec No 2), s. S71-7, 2007 Dec. DOI: 10.1259/bjr/ ... Journal of Biological Chemistry". 277 (45), s. 42881-42890, 2002. DOI: 10.1074/jbc.M206593200. PMID: 12167652. ... Identification of Candidate IgG Antibody Biomarkers for Alzheimer's Disease Through Screening of Synthetic Combinatorial ... Report from SNM: PET imaging of brain chemistry bolsters characterization of dementias. „Diagnostic Imaging", June 16, 2009. ...
One of the most basic techniques of molecular biology to study protein function is molecular cloning. In this technique, DNA ... Click chemistry. *Combinatorial chemistry. *Biosynthesis. *Computational chemistry *Mathematical chemistry. *Theoretical ... The PCR technique can be used to introduce restriction enzyme sites to ends of DNA molecules, or to mutate particular bases of ... High-throughput technique ("-omics"). DNA microarray. Mass spectrometry. Lab-on-a-chip. ...
This brute force approach is still successful and has even been extended by combinatorial chemistry approaches that quickly ... In a complementary technique, peptide mass fingerprinting involves digestion of the native and modified protein with a protease ... "The Journal of Biological Chemistry. 279 (28): 29493-500. doi:10.1074/jbc.M403187200. PMC 3491871 . PMID 15102853.. ... Medicinal Chemistry and Drug Design (PDF). InTech. pp. 357-371. ISBN 978-953-51-0513-8.. ...
Combinatorial problems[edit]. First results to these problems were obtained by Leonard Adleman (NASA JPL) ... Nayebi, Aran (2009). "Fast matrix multiplication techniques based on the Adleman-Lipton model". arXiv:0912.0750.. ... Cruz, R. P. G.; Withers, J. B.; Li, Y. (2004). "Dinucleotide Junction Cleavage Versatility of 8-17 Deoxyribozyme". Chemistry & ... Adleman, L. M. (1994). "Molecular computation of solutions to combinatorial problems". Science. 266 (5187): 1021-1024. Bibcode: ...
This technique can be used to obtain the power of a positive real number b for any irrational exponent. The function fb(x) = bx ... Combinatorial interpretation. For nonnegative integers n and m, the power nm is the number of functions from a set of m ... Exponentiation is used extensively in many fields, including economics, biology, chemistry, physics, and computer science, with ... Alternatively, the combinatorial interpretation of b0 is the number of empty tuples of elements from a set with b elements; ...
"Enhancement of Combinatorial Chemistry by Microwave-Assisted Organic Synthesis". Combinatorial Chemistry & High Throughput ... Oberhofer, M.; Scharmann, A. (1993). Techniques and Management of Personnel Thermoluminescence Dosimetry Services. Current ... "Royal Society of Chemistry. Consultado o 27 de setembro de 2010.. *↑ 10,0 10,1 Lynch, Charles T. (1974). CRC Handbook of ... Royal Society of Chemistry: 125. ISBN 9780851863382. ISSN 0305-9987.. *↑ 69,0 69,1 "Cesium Atoms at Work". Time Service ...
Marc L. Mansfield (1988, applied polymer chemistry and physics). For his outstanding theoretical studies of the structure and ... For his refinement of mathematical techniques in low Reynolds number hydrodynamics, and for his development of novel computer ... subtle design of the most efficient algorithms known for many fundamental problems related to graphs and other combinatorial ... For his development and application of innovative field techniques for studying active faults to identify and date ...
D. Andrica, I. Tomescu, On an integer sequence related to a product of trigonometric functions and its combinatorial relevance ... A Method of Analysis of Contact Multipoles and its Realization by Computer Technique, International Symposium "Computational ... Math., 19(1988), 5-16; reprinted in: Applications of graphs in physics and chemistry, North-Holland, 1989. ... Combinatorial methods in the theory of finite automata, in Gr.C. Moisil (ed.), Logique, Automatique, Informatique, Ed. ...
In Chemistry self-replication studies are typically about how a specific set of molecules can act together to replicate each ... The guidelines recommend that researchers use several specific techniques for preventing mechanical replicators from getting ... Moulin, Giuseppone (2011). "Dynamic Combinatorial Self-Replicating Systems". Springer. doi:10.1007/128_2011_198. Wikisource: ... other within the set (often part of Systems chemistry field). Memetics studies ideas and how they propagate in human culture. ...
Units and Symbols in Physical Chemistry (2nd ed.). Oxford: International Union of Pure and Applied Chemistry, Commission on ... Electron emission techniques such as X-ray photoelectron spectroscopy (XPS) and Auger electron spectroscopy (AES), which ... Myers, Richard (2003). The Basics of Chemistry. Greenwood Press. p. 85. ISBN 978-0-313-31664-7. . OCLC 50164580.. ... Zumdahl, Steven S. (2002). Introductory Chemistry: A Foundation (5th ed.). Houghton Mifflin. ISBN 978-0-618-34342-3. . OCLC ...
Combinatorial Chemistry Techniques* * Humans * Neoplasms / immunology* * Signal Transduction* * T-Lymphocytes / immunology* ... Combinatorial antigen recognition with balanced signaling promotes selective tumor eradication by engineered T cells Nat ...
Combinatorial Chemistry Techniques. Genetic Vectors. Immunoglobulin Fab Fragments / biosynthesis*, immunology. Peptide Library* ... In this paper, we describe an elegant and simple method for constructing large combinatorial Fab libraries for display on the ...
Several analytical techniques have been applied to the analysis of protein-directed DCL. These include HPLC, mass spectrometry ... Protein-directed dynamic combinatorial chemistry. In Dynamic combinatorial chemistry: in drug discovery, bioinorganic chemistry ... Center for Dynamic Combinatorial Chemistry[citation needed] University of Cambridge: Dynamic Combinatorial Chemistry. ... Bridge from supramolecular chemistry to adaptive chemistry. Constitutional Dynamic Chemistry. Topics in Current Chemistry. 322 ...
Combinatorial Chemistry Techniques* * Organ Specificity * Peptide Library* * Receptors, Cell Surface / chemistry Substances * ... New Approaches for Cell-Specific Targeting: Identification of Cell-Selective Peptides From Combinatorial Libraries Curr Opin ...
These techniques are complemented by laboratory methods from combinatorial chemistry, molecular biology and functional genomics ... statistical analysis and chemoinformatic techniques, a recent and innovative international concept registered under the name " ...
To this end, Analysis and Purification Methods in Combinatorial Chemistry describes various analytical techniques and systems ... Quality measurement, control, and improvement in combinatorial chemistry. Combinatorial chemistry has developed rapidly in the ... combinatorial chemistry, medicinal chemistry, organic chemistry, biotechnology, biochemistry, or biophysics. About the Author. ... Analysis and Purification Methods in Combinatorial Chemistry. Bing Yan (Editor). ISBN: 978-0-471-53197-5 January 2004 480 Pages ...
Combinatorial chemistry is increasingly being used by pharmaceutical companies in their search for new drugs. ... Combinatorial chemistry is a group of techniques for synthesising large arrays of related chemicals. These can be easily ... Combinatorial chemistry is a group of techniques for synthesising large arrays of related chemicals. These can be easily ... Combinatorial chemistry is a group of techniques for synthesising large arrays of related chemicals. These can be easily ...
Combinatorial Chemistry, Chemoinformatics, Laboratory Automation and Compound management) in advancing drug discovery research. ... Combinatorial Chemistry & High Throughput Screening (CCHTS) publishes full length original research articles and reviews ... Screening GLP-1 Receptor Ligands from Natural Products in Herbs through High-Content Technique. , 2019; 22(7): 445 - 454. ... Combinatorial Chemistry & High Throughput Screening. Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry ...
5.1.1 The design of combinatorial syntheses 147. 5.1.2 The general techniques used in combinatorial synthesis 148 ... "Medicinal Chemistry is certainly a text I would chose to teach from for undergraduates. It fills a unique niche in the market ... Medicinal Chemistry: An Introduction, Second Edition provides a comprehensive, balanced introduction to this evolving and ... Written in an accessible style, Medicinal Chemistry: An Introduction, Second Edition carefully explains fundamental principles ...
Combinatorial chemistry is one of these techniques. Currently, the technique is very time consuming. A need in the art exists ... Drug Development Through Combinatorial Chemistry. Combinatorial chemistry is the synthesis of large numbers of compounds that ... Using the combinatorial chemistry technique, one typically begins with a molecule or compound known to be useful. The substance ... The intent of combinatorial chemistry efforts includes: 1) lead generation, 2) lead optimization, and 3) combinatorial mixtures ...
Analytical Techniques in Combinatorial Chemistry (Hardback) Edited by Swartz, Michael E. *RRP: $419.00 ... Where? Books » Category » Technology, Engineering & Agriculture » Industrial Chemistry & Manufacturing Technologies » ... This title describes the chromatographic and spectroscopic techniques used to generate chemical and molecular diversity in ...
Combinatorial biosynthesis; Plant cell based chemistry; Bacterial and viral cell based chemistry; Chemistry of cellular ... New high throughput screening techniques; Small molecular array fabrication; Chemical genomics; Chemical and biological ... Current Chemical Biology aims to publish full-length and mini reviews on exciting new developments at the chemistry-biology ... Science at Chemistry-Biology Interface (Chemical informatics; Macromolecular catalysts and receptors; Enzymatic synthesis; ...
Bioorganic Chemistry, and Materials Science - Author: Miller, Benjamin L. - Price: 81,70€ ... Effective techniques for applying Dynamic Combinatorial Chemistry. In a relatively short period, Dynamic Combinatorial ... Dynamic Combinatorial Chemistry : In Drug Discovery, Bioorganic Chemistry, and Materials Science. 81,70€ ... Dynamic Combinatorial Chemistry. In Drug Discovery, Bioorganic Chemistry, and Materials Science. Edited by. Benjamin L. Miller ...
Novel Techniques in Combinatorial Chemistry. p. 371. Reviews. p. 372. Author Index. p. 375. ...
Combinatorial chemistry; Graph theory in chemistry; Prediction of drug toxicity; Property prediction; Molecular mechanics and ... Bioimaging ( Image processing in medicine and biological sciences; Measurements techniques; Mass spectrometry; Numerical( ... Mathematical chemistry and chemical graphs; In silico environmental toxicology; Computer-assisted chemical engineering; ... Techniques for gene expression analysis; Modeling and simulation of biomarkers) ...
Combinatorial chemistry; Graph theory in chemistry; Prediction of drug toxicity; Property prediction; Molecular mechanics and ... Biotechnology is defined as the industrial use of living organisms or biological techniques developed through basic research. ... Bioimaging ( Image processing in medicine and biological sciences; Measurements techniques; Mass spectrometry; Numerical( ... Mathematical chemistry and chemical graphs; In silico environmental toxicology; Computer-assisted chemical engineering; ...
... which are adapted for combinatorial chemistry. Any of the embodiments of the invention may be used either alone or taken in ... The array, array cover, and the stage may be modified as required for a variety of synthesis and/or analysis techniques. The ... screening and/or characterization of combinatorial libraries. The invention relates to an array, which permits various high- ... Combinatorial Chemistry Process. The invention also relates to a combinatorial chemistry process, used for the synthesis of ...
Methods to allow the clean preparation of oligosaccharides were investigated using techniques that do not require conventional ... Combinatorial Chemistry Techniques / methods*. Glycosides / chemistry. Glycosylation. Iodine / chemistry. Molecular Sequence ... Title: Organic & biomolecular chemistry Volume: 1 ISSN: 1477-0520 ISO Abbreviation: Org. Biomol. Chem. Publication Date: 2003 ... Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, UK CB2 1EW.. ...
Combinatorial Chemistry and New Drugs An innovative technique that quickly produces large numbers of structurally related ...
Combinatorial Chemistry, Chemoinformatics, Laboratory Automation and Compound management) in advancing drug discovery research. ... Combinatorial Chemistry & High Throughput Screening (CCHTS) publishes full length original research articles and reviews ... Machine learning techniques for high-throughput structure and function analysis for proteomics and genomics. Guest Editor(s): ... Combinatorial Chemistry & High Throughput Screening. Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry ...
Transducer Techniques, LLC. Transducer Techniques manufactures a complete line of Load Cells,... ... Combinatorial Chemistry. Comprehensive information on combinatorial chemistry and high.... Explore All Collections in Your City ...
Method and system for inhibiting cross-contamination in fluids of combinatorial chemistry device. ... Bead Manipulation Techniques. US20110118132 *. 25 Jan 2011. 19 May 2011. Advanced Liquid Logic, Inc.. Enzymatic Assays Using ... Bead manipulation techniques. US9091649. 8 Nov 2010. 28 Jul 2015. Advanced Liquid Logic, Inc.. Integrated droplet actuator for ... Techniques and droplet actuator designs for reducing bubble formation. US9816133. 8 Oct 2013. 14 Nov 2017. cole Polytechnique. ...
Another problem with combinatorial chemistry, says Harren Jhoti of Astex, is that over time, the compounds it produced were ... But now they are making a comeback in the form of novel twists on combinatorial techniques. ... The enthusiasm for combinatorial chemistry also diverted attention away from compounds derived from natural products. Once a ... As a result, much effort is now being focused on using combinatorial chemistry and high-throughput screening more appropriately ...
Buy the Paperback Book Combinatorial Chemistry by Hicham Fenniri at Indigo.ca, Canadas largest bookstore. + Get Free Shipping ... It is written at a level easily accessible to novices and will enable readers to use combinatorial techniques to the best ... Combinatorial Chemistry is a genuine practical guide covering all the major areas of combinatorial chemistry from an ... Being one of the most powerful of modern technologies, combinatorial chemistry has had implications to many areas of chemistry ...
Novel Bioinformatics and Systems Biology approaches and techniques in Pharmaceutical and Biochemical Sciences Guest Editor(s): ... Combinatorial Chemistry & High Throughput Screening Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry ... Combinatorial Chemistry & High Throughput Screening, Volume 21, Number 3. Guest Editor(s): Luciana Scotti, Jahan Ghasemi, ... Combinatorial Chemistry & High Throughput Screening. Science Citation Index ExpandedTM, Journal Citation Reports/Science ...
Stochastic Processes; Protein Engineering; Algorithms; Proteins; Combinatorial Chemistry Techniques; Probability, Databases: ... Here, we study four common search techniques: Monte Carlo (MC) and Monte Carlo plus quench (MCQ); genetic algorithms (GA); self ...
Combinatorial chemistry; Graph theory in chemistry; Prediction of drug toxicity; Property prediction; Molecular mechanics and ... Bioimaging ( Image processing in medicine and biological sciences; Measurements techniques; Mass spectrometry; Numerical( ... Techniques for gene expression analysis; Modeling and simulation of biomarkers) Advanced biocomputation technologies ( ... Mathematical chemistry and chemical graphs; In silico environmental toxicology; Computer-assisted chemical engineering; ...
... and combinatorial chemistry to generate large numbers of candidate drug structures. SPECIAL REQUIREMENTS Patent Coverage. Since ... and computational techniques to allow the determination of three-dimensional structure; advances in screening technology to ... molecular structure determined through biophysical techniques as a prelude to drug discovery studies . These aspects are ...
Combinatorial Chemistry Combinatorial chemistry [1] is a technology for creating a multitude of different compounds by reacting ... Combinatorial Chemistry. Combinatorial chemistry is a sophisticated set of techniques used to synthesize, purify, analyze, and ... Combinatorial Chemistry. Combinatorial chemistry is a technology for creating a multitude of different compounds by reacting ... Spending most of his care… Green Chemistry , Green chemistry is also known as environmentally benign chemistry, or sustainable ...
These include isolation and assay, combinatorial chemistry and bioassay-guided fractionation. Bioassay guided fractionation ... eluted fractions are tested for bioactivity and active fractions are examined by various analytic techniques, viz. thin layer ... involves the separation of bioactive phytochemicals from a mixture of compounds using various analytic techniques based on ...
  • In this paper, we describe an elegant and simple method for constructing large combinatorial Fab libraries for display on the surface of Saccharomyces cerevisiae, from modestly sized, and easily constructed, heavy and light chain libraries. (biomedsearch.com)
  • employed transesterification to generate dynamic combinatorial libraries. (wikipedia.org)
  • However, their subsequent investigations identified that both the disulfide and hydrazone covalent bonds exhibit effective component exchange processes and so present a reliable means of generating dynamic combinatorial libraries capable of thermodynamic templation. (wikipedia.org)
  • Workstation, apparatuses and methods for the high-throughput synthesis, screening and/or characterization of combinatorial libraries. (google.com)
  • Combinatorial Chemistry and the Synthesis of Compound Libraries / Matthias Mentel -- 6. (princeton.edu)
  • Adaptive Combinatorial Design of Focused Compound Libraries / Andreas Schutter -- 9. (princeton.edu)
  • The essence of combinatorial chemistry or techniques involving "molecular diversity" is to generate enormous populations of molecules and to exploit appropriate screening techniques to isolate active components contained in these libraries. (worldcat.org)
  • Combinatorial chemistry, also known as combichem, is a technique used in drug discovery to create libraries of structurally related compounds. (selectscience.net)
  • Identification of Technetium-99m Binding Peptides Using Combinatorial Cellulose-Bound Peptide Libraries," J. Am. Chem. (patentgenius.com)
  • Combinatorial Libraries: Studies in Molecular Recognition and the Quest for New Catalysts," Liebigs Ann. (patentgenius.com)
  • Early practitioners coined the term `combinatorial chemistry` to describe the synthesis of large libraries with diverse chemical structures screened in mass for potential biological activity. (environmental-expert.com)
  • Libraries can comprise compound mixtures, or separate, single substances, depending on the synthetic strategy, which are described as combinatorial. (docplayer.net)
  • Methods and Techniques of Combinatorial Synthesis 4.1 Synthetic Strategies towards Combinatorial Libraries Split-Pool Synthesis towards Combinatorial Libraries In the first step, the resin beads, each of which is coupled with a single building block, are split into multiple, equally sized portions in separate reaction vessels. (docplayer.net)
  • Advantages of this method: - few reaction vessels needed - only one single compound is bound to each resin bead in a library Currently, split-pool synthesis is the most popular method for the synthesis of large combinatorial libraries of compound mixtures. (docplayer.net)
  • 5 4.1.2 Parallel Synthesis towards Combinatorial Libraries Compounds are synthesized in parallel using ordered arrays (collections of separate single substances) of spatially separated reaction vessels. (docplayer.net)
  • Topics include (1) the generation of continuous gradient techniques for fabricating combinatorial libraries of film thickness, temperature, surface chemistry and polymer blend composition, (2) high-throughput measurement techniques for assessing the mechanical properties and adhesion of surfaces, interfaces and films, and (3) microfluidic approaches to synthesizing and analyzing libraries of interfacially-active polymer species. (springer.com)
  • Topics include chemical and electrophoretic techniques for rapid sample preconcentration and separation, screening processes for proteins from libraries of compounds, protein folding and dynamics, and more. (routledge.com)
  • Method of generating combinatorial libraries of polypeptides containing the β-peptide residues and libraries formed thereby are disclosed. (freepatentsonline.com)
  • Known as combinatorial peptide ligand libraries, these new methodologies are one of the hottest topics related to the study of proteomics and have applications in medical diagnostics, food quality, and plant analysis. (bookdepository.com)
  • Low-abundance protein access by combinatorial peptide libraries 5. (bookdepository.com)
  • Other applications of combinatorial peptide libraries 8. (bookdepository.com)
  • Analytical & Bioanalytical Chemistry, February 2014 'Boschetti and Righetti introduce the new technique of combinatorial peptide ligand libraries for identifying low-abundance peptide fragments. (bookdepository.com)
  • The simplest form a combinatorial peptide library is parallel library in which each peptide is synthesized in individual reaction chambers resulting in well characterized libraries. (scientistsolutions.com)
  • A wide range of techniques are now available for generating gene libraries with different characteristics. (openwetware.org)
  • Today, many combinatorial libraries as well as several systems for automation are available. (mpg.de)
  • In this review we will discuss several concepts of combinatorial libraries and provide information as what to expect from these depending on the given context. (mpg.de)
  • Medicinal Chemistry: An Introduction, Second Edition provides a comprehensive, balanced introduction to this evolving and multidisciplinary area of research. (wiley.com)
  • Written in an accessible style, Medicinal Chemistry: An Introduction, Second Edition carefully explains fundamental principles, assuming little in the way of prior knowledge. (wiley.com)
  • At St Andrews, students are able to build their fundamental training in chemistry into specialised areas including medicinal chemistry, materials, molecular biology, nanotechnology, catalysis and surface science. (st-andrews.ac.uk)
  • Journal of Medicinal Chemistry , 53 15: 5536-5548. (edu.au)
  • 2 pany HEALTH AND MEDICINE · 'Medicinal Chemistry,' Paul S. Anderson, Bristol-Myers Squibb Com- · 'Bioprocessing,' James R. Swartz, Stanford University There were also breakout sessions in which participants in the workshop expressed their views about the various topics. (nap.edu)
  • The library[further explanation needed] of these reversibly interconverting building blocks is called a dynamic combinatorial library (DCL). (wikipedia.org)
  • By modern definition, dynamic combinatorial chemistry is generally considered to be a method of facilitating the generation of new chemical species by the reversible linkage of simple building blocks, under thermodynamic control. (wikipedia.org)
  • first proposed the concept of dynamic combinatorial chemistry. (wikipedia.org)
  • In a relatively short period, Dynamic Combinatorial Chemistry (DCC) has grown from proof-of-concept experiments in a few isolated labs to a broad conceptual framework with applications to an exceptional range of problems in molecular recognition, lead compound identification, catalyst design, nanotechnology, polymer science, and others. (ellibs.com)
  • It's a variation, in its way, of another one of those techniques called Dynamic Combinatorial Chemistry . (sciencemag.org)
  • Dynamic Combinatorial Chemistry is a new method with great potential for the development of new synthetic receptors, the discovery of new ligands for proteins and for studying the folding of extended molecules. (europa.eu)
  • In addition, the involvement of the biotech company Astex, who have an active interest in dynamic combinatorial chemistry, will be mutually beneficial: Astex will be informed of the latest developments in the field, while the students will be exposed to the industrial perspective on Science in general and Dynamic Combinatorial Chemistry in particular. (europa.eu)
  • Through the combined and synergistic efforts of all participants we will deliver a new generation of highly trained researchers that will help to consolidate Europeas leading role in Dynamic Combinatorial Chemistry and develop this new and highly promising technique to its full potential. (europa.eu)
  • The field of combinatorial chemistry extends over a broad range of disciplines, from synthetic organic chemistry to biochemistry, from material sciences to cell biology. (worldcat.org)
  • The same suite of techniques, slightly adapted, is now available to those working in the field of combinatorial chemistry. (springer.com)
  • The company published numerous examples of it, but I don't know if any of these compounds ever got anywhere (and indeed, I'm not at all sure that their current clinical candidate was discovered by this technique). (sciencemag.org)
  • Combinatorial chemistry is a technology for creating a multitude of different compounds by reacting different combinations of interchangeable chemical "building blocks. (encyclopedia.com)
  • Combinatorial chemistry allows the rapid synthesis and testing of many related compounds, greatly speeding the pace of drug discovery. (encyclopedia.com)
  • By using a moderately sized collection of side groups, placing them onto a "scaffold" molecule that is more complex than benzene (such as cholesterol, which has three six-carbon rings and a five-carbon ring), and by using additional levels of side groups, combinatorial chemists can synthesize vast numbers of distinct but related compounds. (encyclopedia.com)
  • The large number of possible new drug targets has already outgrown the number of existing compounds that could potentially serve as drug candidates and the field of chemistry has limitation when it comes to synthesising new drug structures. (ispub.com)
  • This technique makes and tests large quantities of chemical compounds simultaneously to find those with certain desired properties. (studentscholarships.org)
  • Combinatorial chemistry allows chemists to produce thousands of compounds more quickly and less expensively than was formerly possible. (studentscholarships.org)
  • Furthermore, analytical chemists develop techniques and study the relationships and interactions among the parts of compounds. (studentscholarships.org)
  • Organic chemists study the chemistry of the vast number of carbon compounds that make up all living things. (studentscholarships.org)
  • Newman said the advent of new drug discovery techniques such as combinatorial chemistry in the 1990s diverted many drug company resources away from a rich source of new drug compounds. (reuters.com)
  • The technique allows for the rapid combination of many different but similar compounds - basically industrializing the role of the chemist. (reuters.com)
  • Parallel Synthesis is a technique widely used by researchers to speed the discovery of new compounds and screen for optimal process conditions. (environmental-expert.com)
  • Combinatorial synthesis as a novel high-throughput method enables the rapid production of thousand times more compounds than conventional serial organic synthesis allows. (docplayer.net)
  • In this automated chemistry lab, the scientists make, analyse and purify tens of thousands of compounds for biological testing. (abpischools.org.uk)
  • This principle is known to select the most thermodynamically stable product from an equilibrating mixture of a number of components, a concept commonly utilised in synthetic chemistry to direct the control of reaction selectivity. (wikipedia.org)
  • Although the work of Busch helped to establish the template method as a powerful synthetic route to stable macrocyclic structures, this approach remained exclusively within the domain of inorganic chemistry until the early 1990s, when Sanders et al. (wikipedia.org)
  • This methodology combines information from several fields, such as X-ray crystallography and/or NMR, molecular modelling, synthetic organic chemistry, QSAR, and biological assays [ 6 ]. (hindawi.com)
  • Although the industrial revolution and the development of organic chemistry resulted in a preference for synthetic products, World Health Organisation (WHO) reports that between 70% and 95% of citizens in a majority of developing countries still rely on traditional medicine as their primary source of medication 3 . (ispub.com)
  • The scientific aims are to further develop the underlying chemistry and the theory behind complex equilibrium systems and to deliver new functional molecules in the form of inhibitors of proteins, enantioselective synthetic receptors or catalysts. (europa.eu)
  • The hope is to generalize the notion of synthetic organic chemistry to graph grammars, and create a stronger underlying formalism that would allow us to make useful tools and think of new problems and applications that can be solved by thinking of them in a “chemical†fashion. (lambda-the-ultimate.org)
  • What kinds of problems do people in synthetic organic chemistry think about? (lambda-the-ultimate.org)
  • The last 60 or so years of chemistry has developed to give us synthetic routes to millions of molecules. (lambda-the-ultimate.org)
  • These factors include, but are not limited to, isolation techniques, such as spectroscopic, chromatographic, biosynthetic, and synthetic methods, and the fact that these isolates can now be obtained by synthetic or combinatorial chemistry and molecular modeling [ 3 , 4 , 5 ]. (mdpi.com)
  • The value of this approach in combinatorial synthesis is clearly obvious as many different synthetic conditions can be investigated simultaneously and the biological activity of the products concurrently ascertained. (chromatography-online.org)
  • Being one of the most powerful of modern technologies, combinatorial chemistry has had implications to many areas of chemistry andbiology and the current approaches to drug, catalyst, receptor, and materials development and discovery are all included in this volume. (indigo.ca)
  • We present an overview of research conducted at the National Institute of Standards and Technology aimed at developing and applying combinatorial and high-throughput measurement approaches to polymer surfaces, interfaces and thin films. (springer.com)
  • Combinatorial chemistry is most often used to synthesize "small molecules," in contrast to macromolecules such as DNA, RNA, proteins, and polysaccharides, which are polymers containing long chains of monomer subunits. (encyclopedia.com)
  • It summarizes breakthroughs in the theory and instrumentation of electrospray mass spectrometry in pharmaceutical and biomedical applications, provides practical examples for the characterization of peptides, proteins, and glycoproteins, includes applications in proteomics, combinatorial chemistry, and drug characterization. (routledge.com)
  • Protein assays are the techniques used to study proteins such as for detecting proteins, for isolating and purifying proteins, and for characterizing the structure and function of proteins, often requiring that the protein first be purified. (reportsnreports.com)
  • The application of combinatorial strategies to protein engineering therefore requires, above all else, the construction of a library of variant proteins. (openwetware.org)
  • Much of the appeal of directed evolution of proteins lies in the fact that the coding information is held in a molecular medium which is straightforward to amplify, read, and manipulate, while the functional molecule, the protein, has a rich chemistry that provides a wide range of possible activities. (openwetware.org)
  • Phage display is a laboratory technique for the study of protein-protein, protein-peptide, and protein-DNA interactions that uses bacteriophages (viruses that infect bacteria) to connect proteins with the genetic information that encodes them. (wikipedia.org)
  • These techniques are complemented by laboratory methods from combinatorial chemistry, molecular biology and functional genomics. (wikipedia.org)
  • Methods to allow the clean preparation of oligosaccharides were investigated using techniques that do not require conventional column chromatography or an aqueous work-up. (biomedsearch.com)
  • Bringing together a group of respected experts, this overview explains how chemists can apply DCC and fragment-based library methods to lead generation for drug discovery and molecular recognition in bioorganic chemistry and materials science. (ellibs.com)
  • The invention also relates to a variety of methods for synthesis, screening, and characterization, which are adapted for combinatorial chemistry. (google.com)
  • Dr. Fodor's group also developed sensitive techniques to read these arrays, using fluorescent labeling methods and confocal laser scanning. (aacc.org)
  • Volume 5 in this series spans a variety of topics including terpene synthesis, amino acid synthesis, and combinatorial methods for generation of structural diversity. (elsevier.com)
  • Three of the major asymmetric methods are discussed and grouped according to the chemistry involved. (elsevier.com)
  • A review of the combinatorial chemistry methods currently available for lead discovery in pharmaceutical research is provided in this chapter, as well as discussions on the methods based on natural products and an overview of the complexity building techniques. (elsevier.com)
  • Geysen s multipin apparatus (1984) and Houghten s tea-bag system (1985) are methods for multiple (parallel) synthesis of peptides, based on the techniques of solid-phase peptide synthesis according to Merrifield (presented 1963) Birth of Comb. (docplayer.net)
  • Meredith JC, Karim A, Amis EJ (2002) Combinatorial methods for investigations in polymer materials science. (springer.com)
  • Vera Go is using combinatorial chemistry methods developed by Kit Lam to identify new treatments for cytomegalovirus - or CMV. (ucdavis.edu)
  • Presentation and discussion of a research based topic in the field of modern methods in (bio)organic synthesis and analysis, like solid phase reactions, combinatorial chemistry, microreaction technique, hyphenated analysis techniques (HPLC-MS) or special metal-, organo- or photocatalytic reactions. (uni-regensburg.de)
  • The aim is to provide an up to date resource to allow groups interested in using directed evolution to identify the most appropriate methods for their purposes and to guide those moving on from initial experiments to more ambitious targets in the selection of library construction techniques. (openwetware.org)
  • Although this approach was arguably utilised in the work of Fischer and Werner as early as the 19th century, their respective studies of carbohydrate and coordination chemistry were restricted to rudimentary speculation, requiring the rationale of modern thermodynamics. (wikipedia.org)
  • This approach comprises different techniques, of which the most used are quantitative structure activity relationship (QSAR), molecular similarity/diversity technique, and combinatorial chemistry. (hindawi.com)
  • The training programme will integrate different disciplines ranging from inorganic chemistry and computational chemistry to protein chemistry and nanotechnology. (europa.eu)
  • Additionally, the complementary techniques of computational chemistry and cheminformatics have been used to successfully leverage research information. (ccl.net)
  • Provide state-of-the-art techniques to lead generation and optimization processes (analytics, including physicochemical measurements, combinatorial and computational chemistry, separation techniques). (theladders.com)
  • Computational chemistry of polyatomic reaction kinetics and dynamics: the quest for an accurate CH5 potential energy surface. (neurotransmitter.net)
  • The School has several groups carrying out research in core areas of organic synthesis and molecular inorganic chemistry. (st-andrews.ac.uk)
  • Our research program utilizes organic synthesis and coordination chemistry to make polymers and organized assemblies. (umich.edu)
  • The standard proteomics techniques of mass spectrometry, 2D electrophoresis and chromatography are deliberately given brief treatment only as prefractionation tools in favor of new methodologies. (bookdepository.com)
  • The research interests of the members of the Chemical Physics Thematic Research Group are diverse, with groups focusing on high-end laser and NMR spectroscopies, kinetics and modelling of atmospheric chemical reactions, experimental and theoretical biophysical chemistry, polymers at interfaces, and statistical and quantum mechanics. (mcgill.ca)
  • Since the early 1990s, combinatorial chemistry has attracted the attention of many companies. (docplayer.net)
  • biophysical chemistry, which focuses on the development and application of physicochemical techniques to biological systems. (st-andrews.ac.uk)
  • The Chemical Biology Thematic Research Group is engaged in a diverse range of research topics, which span structural biology, enzymology, nucleic acid research, signalling pathways, single-molecule biophysics, and biophysical chemistry of living tissues. (mcgill.ca)
  • In the field of biophysical chemistry, single molecule spectroscopy is being used to probe enzyme function as well as DNA recombination and repair. (mcgill.ca)
  • The main topic of this 39th Mosbacher Colloquium is concerned with techniques of protein engineering, examples of application, and the analysis and determination of protein structure, their stability and flexibility. (worldcat.org)
  • Directed molecular evolution and combinatorial methodologies are playing an increasingly important role in the field of protein engineering. (openwetware.org)
  • It is for these reasons that 'design by statistics' or combinatorial strategies for protein engineering are appealing. (openwetware.org)
  • In this technique, a gene encoding a protein of interest is inserted into a phage coat protein gene, causing the phage to "display" the protein on its outside while containing the gene for the protein on its inside, resulting in a connection between genotype and phenotype. (wikipedia.org)
  • It was not until supramolecular chemistry revealed early concepts of molecular recognition, complementarity and self-organisation that chemists could begin to employ strategies for the rational design and synthesis of macromolecular targets. (wikipedia.org)
  • Developments in technology and the use of computers have allowed chemists and materials scientists to practice new, more efficient techniques, such as combinatorial chemistry. (studentscholarships.org)
  • Constraint technology proposes a novel set of techniques and tools for efficiently solving (hard) combinatorial problems. (uu.se)
  • Note that constraint technology is complementary to linear programming (a common technique in operations research): this course will be of particular interest to students with such a background. (uu.se)
  • In addition to its importance as an application area, this is important to nanotechnology as a source of new component parts, which may be applied in either parallel or sequential techniques for constructing new structures. (foresight.org)
  • Current Chemical Biology aims to publish full-length and mini reviews on exciting new developments at the chemistry-biology interface, covering topics relating to Chemical Synthesis, Science at Chemistry-Biology Interface and Chemical Mechanisms of Biological Systems. (ingentaconnect.com)
  • Biotechnology is defined as the industrial use of living organisms or biological techniques developed through basic research. (iaria.org)
  • Concisely stated, a genetic algorithm (or GA for short) is a programming technique that mimics biological evolution as a problem-solving strategy. (talkorigins.org)
  • Among the themes that unite the research being performed in this group is the attempt to learn new chemistry and physics from biological systems. (mcgill.ca)
  • The book is written for university and industry scientists starting proteomic studies of complex matrices (e.g., biological fluids, biopsies, recalcitrant plant tissues, foodstuff, and beverage analysis), researchers doing wet chemistry, and graduate-level students in the areas of analytical and biochemistry, biology, and genetics. (bookdepository.com)
  • The Department of Chemistry and Biochemistry offers majors leading to a Bachelor of Science or a Bachelor of Arts Degree. (csudh.edu)
  • Contact the Department of Chemistry and Biochemistry for further information. (csudh.edu)
  • Drug research has been greatly transformed by the 'omics revolution' and advances in computational tools, combinatorial chemistry, and high throughput screening techniques (HTS). (princeton.edu)
  • Research on the chemistry of living things spurs advances in medicine, agriculture, food processing, and other fields. (studentscholarships.org)
  • Advances in technology are making massive data sets common in many scientific disciplines, such as astronomy, medical imaging, bio-informatics, combinatorial chemistry, remote sensing, and physics. (umn.edu)
  • Our recent advances in image correlation spectroscopic techniques now allow researchers to precisely follow the macromolecular dynamics in living cells. (mcgill.ca)
  • Significant advances in the technique of thin layer chromatography have been few and far between over the last decade but, nevertheless, progress continues, albeit at a reduced rate. (chromatography-online.org)
  • Describe the structural elucidation of morphine.I & II) (2008 Pattern) CHEMISTRY OF MEDICINAL NATURAL PRODUCTS Time : 3 Hours] Instructions to the candidates: 1) 2) 3) [Max.T. Answers to the two sections should be written in separate answer books.Pharmacy (Sem. (scribd.com)
  • of Questions :8] [Total No.112 M. . Shikimic acid Pathway.I Q1) Describe the chemistry and structural elucidation of Caffeine. (scribd.com)
  • Dr. Fodor and his colleagues were the first to develop and describe microarray technologies and combinatorial chemistry synthesis. (aacc.org)
  • 1253-1256 22May98] describe a new technique for cutting large numbers of nanotubes into segments with controllable lengths. (imm.org)
  • Pore size distribution, volume percent porosity, BET surface area, and strength measurements are compared for different processing techniques against standard reticulates. (mrs.org)
  • Beers KL, Douglas JF, Amis EJ, Karim A (2003) Combinatorial measurements of crystallization growth rate and morphology in thin films of isotactic polystyrene. (springer.com)
  • When undertaking combinatorial chemistry consider reagents, buffers, resins and standards. (selectscience.net)
  • B): In a combinatorial synthesis, different building blocks of type A (A1-An) are treated simultaneously with different building blocks of type B (B1-Bn) according to combinatorial principles, i.e. each starting material A reacts separately with all reagents B resulting in a combinatorial library A1-nB1-n. (docplayer.net)
  • Through combinatorial chemistry, scientists can make and test millions, billions, or even quadrillions (10 15 ) of guesses about which chemical compound might have a desirable function, such as the ability to bind to a specific molecule, or to serve as a drug. (encyclopedia.com)
  • Discussing strategies to determine the structure and machanisms of numerous compound classics, this book covers new chemical and elctrophoretic techniques for rapid sample preconcentration and separation. (routledge.com)
  • While these separation techniques offer high-performance compound isolation, time-consuming preliminary experiments and the use of large amounts of silica gel are required. (intechopen.com)
  • Solid-phase techniques are one solution to provide great advantages with respect to compound separation and have also proven to be effective for automated synthesis and combinatorial chemistry. (intechopen.com)
  • The study shows that a practical method, bacterial enzymatic combinatorial chemistry (BECC), can be used to generate functionally diverse molecules that can potentially be used as adjuvants. (asm.org)
  • Organic chemistry methodology that mimics the modular nature of various biosynthetic processes. (bioportfolio.com)
  • This technique will be very helpful in probing the sequence of conformations important in the operation of molecular machines, particularly when high flexibility may make unexpected structures accessible, as in biopolymer systems. (foresight.org)
  • Most structural techniques provide averaged information or information about a single predominant conformational state. (stanford.edu)
  • Presented by IRB Barcelona PhD students and postdocs , the course will cover 12 hot scientific topics, ranging from cell and molecular biology to structural and computational biology, and chemistry. (irbbarcelona.org)
  • High throughput screening and combinatorial chemistry have been used to rapidly identify and optimize leads for these targets. (ccl.net)
  • Students use genetic analysis and molecular biology techniques to investigate chromosome organization, chromatin structure, functional genomics, and mechanisms of differential gene expression. (jhu.edu)
  • It is directed at researchers and professionals in vibrational spectroscopy, analytical chemistry, materials science, biomedicine, food science and combinatorial chemistry. (whsmith.co.uk)
  • International Journal of Environmental Analytical Chemistry "…excellent. (routledge.com)
  • Abstract DESCRIPTION (provided by applicant): The long-term objective of the proposed research is to provide computer-based tools to aid in the high-throughput screening of drug candidates, derived from combinatorial chemistry and similar techniques. (sbir.gov)
  • Rawls writes that "DNA is an ideal molecule to investigate using combinational chemistry" and all of the labs involved have used combinational techniques to select their catalysts. (foresight.org)
  • Acid catalysts in industrial hydrocarbon chemistry. (neurotransmitter.net)
  • Fluorescence Polarization and Time-Resolved Fluorescence Resonance Energy Transfer Techniques for PI3K Assays / Haiching Ma -- 11. (princeton.edu)
  • Smith and Winter were awarded a half share of the 2018 Nobel Prize in chemistry for their contribution to developing phage display. (wikipedia.org)
  • This application of an enzyme system in a cell-free reactor also allows a wider variety of potential substrates than in vivo techniques, including substrates, intermediates, and products that would be toxic to intact cells. (foresight.org)
  • Chemistry is a vibrant and exciting central science that interfaces with biology, physics, mathematics, medicine and geology, and St Andrews offers appropriate modules highlighting the importance of these interfaces. (st-andrews.ac.uk)
  • Community college transfers should have completed one year of general chemistry, one year of calculus and one year of physics. (csudh.edu)
  • Comprehensive information on combinatorial chemistry and high. (dirjournal.com)
  • That is why expectations were high when two much-hyped technologies-combinatorial chemistry and high-throughput screening-appeared on the scene in the 1990s. (economist.com)
  • Combinatorial Chemistry & High Throughput Screening Journal was launched in 1998. (benthamscience.com)
  • Combinatorial Chemistry & High Throughput Screening is a pivotal journal in the field of drug discovery. (eurekaselect.com)
  • With the advent of spectrometers operating at very high magnetic fields (up to 21.1 T, i.e. 900 MHz proton resonance frequency) it has become an extremely sensitive technique, so that it is now standard practice to couple NMR with high pressure liquid chromatography (HPLC). (springer.com)
  • Meier MAR, Schubert US (2005) Integration of MALDI-TOFMS as high-throughput screening tool into the workflow of combinatorial polymer research. (springer.com)
  • Sehgal A, Karim A, Stafford CF, Fasolka MJ (2003) Techniques for combinatorial and high-throughput microscopy: part 1: gradient specimen fabrication for polymer thin films research. (springer.com)
  • Lucas LA, DeLongchamp DM, Vogel BM, Lin EK, Fasolka MJ, Fischer DA, McCulloch I, Heeney M, Jabbour GE (2007) Combinatorial screening of the effect of temperature on the microstructure and mobility of a high performance polythiophene semiconductor. (springer.com)
  • We are reduced by infected credits, high-quality properties, and a combinatorial actorshortname that indicates much about the page and too at all about the confidence. (motoequip.com)
  • Rated in the top four UK Chemistry departments in the most recent Research Excellence Framework (see Times Higher Education analysis of REF 2014), we are internationally recognised for the breadth, creativity and high quality of our research. (bristol.ac.uk)
  • Combinatorial chemistry (CC) combined with high throughput screening (HTS) technique is an efficient method of synthesizing and screening large number of molecules rapidly. (scientistsolutions.com)
  • Despite the adoption of new techniques like combinatorial chemistry and high through-put screening that have greatly improved the productivity of drug discovery, the average R&D investment required to bring a new drug to market has more than doubled in the past decade, rising from $230MM to $500MM or more. (bain.com)
  • High school students should include two years of algebra, one year of geometry and a one-year course in chemistry in their high school preparation. (csudh.edu)
  • Combinatorial chemistry is increasingly being used by pharmaceutical companies in their search for new drugs. (rsc.org)
  • In the area of atmospheric chemistry, the chemical transformation of the atmosphere is being modelled both experimentally and theoretically to understand how these processes are currently affecting and driving climate change. (mcgill.ca)
  • This procedure is quite unique and is an excellent illustration of the extension of an ongoing and established technique to a challenging modern chemical problem. (chromatography-online.org)
  • current contents are listed at the journal website ) , Chemistry - A European Journal , and Chemical Communications . (neurotransmitter.net)
  • Robots that can do the same chemical reaction over and over again but using different starting materials are often used for this type of routine chemistry. (abpischools.org.uk)