Results 21 to 30 of about 2,925,762 (288)
Unraveling the Allosteric Cross-Talk Between Coactivator Peptide and Ligand Binding Site in Glucocorticoid Receptor [PDF]
, 2021 Glucocorticoid receptor (GR) is a nuclear receptor that controls critical biological processes by regulating thetranscription of specific genes. There is a known allosteric cross-talk between the ligand and coregulator bindingsites within the GR ligand ...
Giuseppina, La Sala +5 more
core +1 more source
Pharmaceutics, 2021 Dual-targeting therapeutics by coadministration of allosteric and orthosteric drugs is drawing increased attention as a revolutionary strategy for overcoming the drug-resistance problems.
Yuran Qiu +6 more
doaj +1 more source
The catalytic effects of active site conformational change in the allosteric activation of imidazole glycerol phosphate synthase [PDF]
, 2023 Imidazole glycerol phosphate synthase (IGPS) is a heterodimeric class-I glutamine amidotransferase (GAT) that hydrolyzes glutamine. Ammonia is produced and transferred to a second active site where it reacts with N1-(5\u27- phosphoribosyl)-formimino-5 ...
Juan V., Alegre-Requena +2 more
core +2 more sources
Scientific Reports, 2023 Cancer has been viewed as one of the deadliest diseases worldwide. Among various types of cancer, breast cancer is the most common type of cancer in women.
Nisarg Rana +5 more
doaj +1 more source
Pharmaceutics, 2022 The acquisition of penicillin-binding protein (PBP) 2a in resistant strains of Staphylococcus aureus allows for the continuous production of cell walls even after the inactivation of intrinsic PBPs. Thus, the discovery of novel therapeutics with enhanced
Jamiu Olaseni Aribisala, Saheed Sabiu
doaj +1 more source
An Extracellular Pore‑Targeting Peptide Defines a Designable Allosteric Site in TRPV2. [PDF]
Adv Sci (Weinh)Structure‐guided peptide engineering yields Depiv2, a highly potent and subtype‐selective TRPV2 inhibitor that binds to the extracellular pore and remodels it into a closed, non‐conductive state. Depiv2 suppresses pathological cardiac hypertrophy, establishing the TRPV2 outer pore as a designable interface for selective peptide modulation.
Zhu A +7 more
europepmc +2 more sources
The Allosteric Binding Sites of Sulfotransferase 1A1 [PDF]
Drug Metabolism and Disposition, 2015 Human sulfotransferases (SULTs) comprise a small, 13-member enzyme family that regulates the activities of thousands of compounds-endogenous metabolites, drugs, and other xenobiotics. SULTs transfer the sulfuryl-moiety (-SO3) from a nucleotide donor, PAPS (3'-phosphoadenosine 5'-phosphosulfate), to the hydroxyls and primary amines of acceptors. SULT1A1,
Ian, Cook +3 more
openaire +2 more sources
Allo-network drugs: Extension of the allosteric drug concept to protein-protein interaction and signaling networks [PDF]
, 2013 Allosteric drugs are usually more specific and have fewer side effects than orthosteric drugs targeting the same protein. Here, we overview the current knowledge on allosteric signal transmission from the network point of view, and show that most ...
Csermely, Péter +3 more
core +2 more sources
Cells, 2022 The pregnane X receptor (PXR, NR1I2) is a xenobiotic-activated transcription factor with high levels of expression in the liver. It not only plays a key role in drug metabolism and elimination, but also promotes tumor growth, drug resistance, and ...
Rajamanikkam Kamaraj +3 more
doaj +1 more source
Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I [PDF]
, 2012 Background: Chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive (Ph+) acute lymphatic leukemia (Ph + ALL) are caused by the t(9;22), which fuses BCR to ABL resulting in deregulated ABL-tyrosine kinase activity.
Ruimi, Nili +18 more
core +2 more sources