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Stapled Peptide
A stapled peptide is a short peptide, typically in an alpha-helical conformation, that is constrained by a synthetic brace ("staple"). The staple is formed by a covalent linkage between two amino acid side-chains, forming a peptide macrocycle. Staples, generally speaking, refer to a covalent linkage of two previously independent entities. Peptides with multiple, tandem staples are sometimes referred to as stitched peptides. Among other applications, peptide stapling is notably used to enhance the pharmacologic performance of peptides. Introduction The two primary classes of therapeutics are small molecules and Biopharmaceutical, protein therapeutics. The Drug design, design of small molecule inhibitors of Protein–protein interaction, protein-protein interactions has been impeded by issues such as the general lack of small-molecule starting points for drug design, the typical flatness of the interface, the difficulty of distinguishing real from artifactual binding, and the size and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ring-closing Metathesis
Ring-closing metathesis (RCM) is a widely used variation of olefin metathesis in organic chemistry for the synthesis of various unsaturated rings via the intramolecular metathesis of two terminal alkenes, which forms the cycloalkene as the ''E-'' or ''Z-'' isomers and volatile ethylene.Carey, F. A.; Sunburg, R. J. Reactions Involving Transition Metals. ''Advanced Organic Chemistry: Reaction and Synthesis'', 5th Ed.; Part B; Springer: New York, 2010, pp. 761-767.Monfette, S.; Fogg, D. E. (2009). "Equilibrium Ring-Closing Metathesis". ''Chem. Rev.'' 109 (8): 3783-3816. . The most commonly synthesized ring sizes are between 5-7 atoms;Deiters, A.; Martin, S. F. (2004). “Synthesis of Oxygen- and Nitrogen-Containing Heterocycles by Ring-Closing Metathesis”. ''Chem. Rev.'' 104 (5): 2199-2238. . however, reported syntheses include 45- up to 90- membered macroheterocycles.Cain, M. F.; Forrest, W. P.; Peryshkov, R. V.; Schrock, R. R. Muller, P. (2013). “Synthesis of a TREN in Whic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peptidomimetic
A peptidomimetic is a small protein-like chain designed to mimic a peptide. They typically arise either from modification of an existing peptide, or by designing similar systems that mimic peptides, such as peptoids and Beta-peptide, β-peptides. Irrespective of the approach, the altered chemical structure is designed to advantageously adjust the molecular properties such as stability or biological activity. This can have a role in the development of drug-like compounds from existing peptides. Peptidomimetics can be prepared by cyclization of linear peptides or coupling of stable unnatural amino acids. These modifications involve changes to the peptide that will not occur naturally (such as altered backbones and the incorporation of nonnatural amino acids). Unnatural amino acids can be generated from their native analogs via modifications such as amine alkylation, side chain substitution, structural bond extension cyclization, and isosteric replacements within the amino acid backb ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peptide Synthesis
In organic chemistry, peptide synthesis is the production of peptides, compounds where multiple amino acids are linked via amide bonds, also known as peptide bonds. Peptides are chemically synthesized by the condensation reaction of the carboxyl group of one amino acid to the amino group of another. Protecting group strategies are usually necessary to prevent undesirable side reactions with the various amino acid side chains. Chemical peptide synthesis most commonly starts at the carboxyl end of the peptide (C-terminus), and proceeds toward the amino-terminus (N-terminus). Protein biosynthesis (long peptides) in living organisms occurs in the opposite direction. The chemical synthesis of peptides can be carried out using classical solution-phase techniques, although these have been replaced in most research and development settings by solid-phase methods (see below). Solution-phase synthesis retains its usefulness in large-scale production of peptides for industrial purposes how ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Non-proteinogenic Amino Acids
In biochemistry, non-coded or non-proteinogenic amino acids are distinct from the 22 proteinogenic amino acids (21 in eukaryotesplus formylmethionine in eukaryotes with prokaryote organelles like mitochondria) which are naturally encoded in the genome of organisms for the assembly of proteins. However, over 140 non-proteinogenic amino acids occur naturally in proteins and thousands more may occur in nature or be synthesized in the laboratory. Chemically synthesized amino acids can be called unnatural amino acids. Unnatural amino acids can be synthetically prepared from their native analogs via modifications such as amine alkylation, side chain substitution, structural bond extension cyclization, and isosteric replacements within the amino acid backbone. Many non-proteinogenic amino acids are important: * intermediates in biosynthesis, * in post-translational formation of proteins, * in a physiological role (e.g. components of bacterial cell walls, neurotransmitters and toxins), * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Druggability
Druggability is a term used in drug discovery to describe a biological target (such as a protein) that is known to or is predicted to bind with high affinity to a drug. Furthermore, by definition, the binding of the drug to a druggable target must alter the function of the target with a therapeutic benefit to the patient. The concept of druggability is most often restricted to small molecules (low molecular weight organic substances) but also has been extended to include biologic medical products such as therapeutic monoclonal antibodies. Drug discovery comprises a number of stages that lead from a biological hypothesis to an approved drug. Target identification is typically the starting point of the modern drug discovery process. Candidate targets may be selected based on a variety of experimental criteria. These criteria may include disease linkage (mutations in the protein are known to cause a disease), mechanistic rationale (for example, the protein is part of a regula ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Beta-peptide
Beta-peptides (β-peptides) are peptides derived from β-amino acids, in which the amino group is attached to the β-carbon (i.e. the carbon two atoms away from the carboxylate group). The parent β-amino acid is β-alanine (H2NCH2CH2CO2H), a common natural substance, but most examples feature substituents in place of one or more C-H bonds. β-peptides usually do not occur in nature. β-peptide-based antibiotics are being explored as ways of evading antibiotic resistance. Early studies in this field were published in 1996 by the group of Dieter Seebach and that of Samuel Gellman. Structure As there are two carbons available for substitution, β-amino acids have four sites (chirality included; as opposed to two in α-amino acids) for attaching the organic residue group. Accordingly, two main types β-amino acids exist differing by which carbon the residue is attached to: ones with the organic residue (R) next to the amine are called β3 and those with position next to the carbon ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as |
Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small pilot studies, and subsequently conduct progressively larger scale comparative studies. Clinical trials can vary i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gregory L
Gregory may refer to: People and fictional characters * Gregory (given name), including a list of people and fictional characters with the given name * Gregory (surname), a surname Places Australia *Gregory, Queensland, a town in the Shire of Burke **Electoral district of Gregory, Queensland, Australia *Gregory, Western Australia. United States *Gregory, South Dakota *Gregory, Tennessee *Gregory, Texas Outer space *Gregory (lunar crater) *Gregory (crater on Venus) Other uses * "Gregory" (''The Americans''), the third episode of the first season of the television series ''The Americans'' See also * Greg (other) * Greggory * Gregoire (other) * Gregor (other) * Gregores (other) * Gregorian (other) * Gregory County (other) * Gregory Highway, Queensland * Gregory National Park, Northern Territory * Gregory River in the Shire of Burke, Queensland * Justice Gregory (other) Justice Gregory may refer to: * George G ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Helen Blackwell
Helen E. Blackwell (born 1972) is an American organic chemist and chemical biologist. She is a professor at the University of Wisconsin–Madison. Education Blackwell is a native of Shaker Heights, Ohio and was educated as an undergraduate at Oberlin College, receiving a Bachelor of Arts degree in chemistry in 1994. She received a Ph.D. in organic chemistry from the California Institute of Technology in 1999 working with Robert Grubbs. Career and research Nearing the end of her doctoral education in 1999, Blackwell gained an interest in biology and joined Stuart Schreiber's lab at Harvard University. At the time, the lab was focusing on animal models, but Blackwell decided to work with plants. During her research, Blackwell identified several small-molecule sirtuin inhibitors in ''Arabidopsis'' plants. Blackwell's research utilizes chemical probes—synthesized using solution-phase and solid-phase synthesis, and combinatorial chemistry—to better understand bacterial communic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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