Results 121 to 130 of about 79,838 (161)
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Searching for new allosteric sites in enzymes
Current Opinion in Structural Biology, 2004The discovery of new allosteric sites generates opportunities for the identification of novel pharmaceuticals and increases our understanding of basic biological processes. Increasingly, allosteric sites are being discovered in various families of proteins by several methods, paving the way for the development of entirely new classes of drugs with a ...
Jeanne A, Hardy, James A, Wells
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Correlation Between Allosteric and Orthosteric Sites
2019Correlation between an allosteric site and its orthosteric site refers to the phenomenon that perturbations like ligand binding, mutation, or posttranslational modifications at the allosteric site leverage variation in the orthosteric site. Understanding this kind of correlation not only helps to disclose how information is transmitted in allosteric ...
Weilin, Zhang, Juan, Xie, Luhua, Lai
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Active site directed effectors of allosteric enzymes
Biochimica et Biophysica Acta (BBA) - Enzymology, 1975This communication introduces the concept of an active site directed effector, in terms of the two state model of Monod et al. (Monod, J., Wyman, J. and Changeux, J.-P. (1965) J. Mol. Biol. 12, 88-118), a consideration made necessary by the observation that the activity of a number of enzymes of the control type is modulated by effector molecules whose
G D, Smith, D V, Roberts, P W, Kuchel
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Advances in NMR Methods to Identify Allosteric Sites and Allosteric Ligands
2019NMR allows assessment of protein structure in solution. Unlike conventional X-ray crystallography that provides snapshots of protein conformations, all conformational states are simultaneously accessible to analysis by NMR. This is a significant advantage for discovery and characterization of allosteric effects.
Hazem, Abdelkarim +3 more
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Hidden allosteric sites and De-Novo drug design
Expert Opinion on Drug Discovery, 2021Hidden allosteric sites are not visible in apo-crystal structures, but they may be visible in holo-structures when a certain ligand binds and maintains the ligand intended conformation. Several computational and experimental techniques have been used to investigate these hidden sites but identifying them remains a challenge.This review provides a ...
Ashfaq Ur, Rehman +6 more
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Discovery of hidden allosteric sites as novel targets for allosteric drug design
Drug Discovery Today, 2018Hidden allosteric sites, as a novel type of allosteric site, are invisible in ligand-unbound (apo) crystal structures, but can emerge in ligand-bound (holo) crystal structures when a specific ligand binds to, and stabilizes, a unique conformation favored by the ligand. However, the identification of these sites is a significant challenge.
Shaoyong, Lu +3 more
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Fishing for allosteric sites on GABAA receptors
Biochemical Pharmacology, 2004GABA(A) receptors have structural and functional homology with a super-family of cys-loop ligand-gated ion channel receptors including the nicotinic acetylcholine receptors. Amino acid residues involved in ligand-binding pockets are homologous among super-family members, leading to the multiple-loop model of binding sites situated at subunit interfaces,
Richard W, Olsen +4 more
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Characteristics of Allosteric Proteins, Sites, and Modulators
2019Allostery is considered one of the most direct and efficient ways to regulate biological macromolecule functions. Allostery is increasingly receiving attention in the field of drug discovery because of the unique advantages of allosteric modulators such as high selectivity and low toxicity.
Xinheng, He +3 more
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Allosteric Binding Sites on Muscarinic Acetylcholine Receptors
Molecular Pharmacology, 2005In this issue of Molecular Pharmacology, Tränkle et al. (p. 1597) present new findings regarding the existence of a second allosteric site on the M2 muscarinic acetylcholine receptor (M2 mAChR). The M2 mAChR is a prototypic class A G protein-coupled receptor (GPCR) that has proven to be a very useful model system to study the molecular mechanisms ...
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Characterization of the CHK1 Allosteric Inhibitor Binding Site
Biochemistry, 2009Checkpoint kinase 1 (CHK1) is a key element in the DNA damage response pathway and plays a crucial role in the S-G(2)-phase checkpoint. Inhibiting CHK1 is a therapeutic strategy involving abrogation of the G2/M mitotic checkpoint defense of tumor cells toward lethal damage induced by DNA-directed chemotherapeutic agents.
Darin, Vanderpool +14 more
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