Results 1 to 10 of about 114,356 (118)
Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators
Molecules, 2023 Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent agonists, allosteric activating PAMs and neutral or silent allosteric modulators are compounds capable of modulating the nicotinic receptor by interacting at allosteric ...
Laura Braconi +2 more
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PASSer2.0: Accurate Prediction of Protein Allosteric Sites Through Automated Machine Learning
Frontiers in Molecular Biosciences, 2022 Allostery is a fundamental process in regulating protein activities. The discovery, design, and development of allosteric drugs demand better identification of allosteric sites.
Hao Tian, Peng Tao, Sian Xiao
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Uncovering an allosteric mode of action for a selective inhibitor of human Bloom syndrome protein
eLife, 2021 BLM (Bloom syndrome protein) is a RECQ-family helicase involved in the dissolution of complex DNA structures and repair intermediates. Synthetic lethality analysis implicates BLM as a promising target in a range of cancers with defects in the DNA damage ...
Xiangrong Chen +13 more
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Structure-Activity Relationships of Benzothiazole-Based Hsp90 C-Terminal-Domain Inhibitors
Pharmaceutics, 2021 Heat shock protein 90 (Hsp90) is a chaperone responsible for the maturation of many cancer-related proteins, and is therefore an important target for the design of new anticancer agents.
Jaka Dernovšek +6 more
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Angiotensinogen and the Modulation of Blood Pressure
Frontiers in Cardiovascular Medicine, 2021 The angiotensin peptides that control blood pressure are released from the non-inhibitory plasma serpin, angiotensinogen, on cleavage of its extended N-terminal tail by the specific aspartyl-protease, renin. Angiotensinogen had previously been assumed to
Zimei Shu +4 more
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Biomolecules, 2022 The peroxisome proliferator-activated receptor gamma (PPARγ) is a nuclear receptor and controls a number of gene expressions. The ligand binding domain (LBD) of PPARγ is large and involves two binding sites: orthosteric and allosteric binding sites ...
Suliman Almahmoud, Haizhen A. Zhong
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Biomolecules, 2022 Hsp90 is a promising target for the development of novel agents for cancer treatment. The N-terminal Hsp90 inhibitors have several therapeutic limitations, the most important of which is the induction of heat shock response, which can be circumvented by ...
Živa Zajec +3 more
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The protein kinase CK1: Inhibition, activation, and possible allosteric modulation
Frontiers in Molecular Biosciences, 2022 Protein kinases play a vital role in biology and deregulation of kinases is implicated in numerous diseases ranging from cancer to neurodegenerative diseases, making them a major target class for the pharmaceutical industry.
Yashoda Krishna Sunkari +2 more
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Molecules, 2021 CagA is a major virulence factor of Helicobacter pylori. H. pylori CagA is geographically subclassified into East Asian CagA and Western CagA, which are characterized by the presence of a EPIYA-D or EPIYA-C segment.
Quan Wang +3 more
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The Impact of the Secondary Binding Pocket on the Pharmacology of Class A GPCRs
Frontiers in Pharmacology, 2022 G-protein coupled receptors (GPCRs) are considered important therapeutic targets due to their pathophysiological significance and pharmacological relevance. Class A receptors represent the largest group of GPCRs that gives the highest number of validated
Attila Egyed +2 more
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