Allosteric modulation of G protein-coupled receptor signaling
G protein-coupled receptors (GPCRs), the largest family of transmembrane proteins,
regulate a wide array of physiological processes in response to extracellular signals …
regulate a wide array of physiological processes in response to extracellular signals …
Fine tuning muscarinic acetylcholine receptor signaling through allostery and bias
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug
targets for neurological diseases, in particular for Alzheimer's disease and schizophrenia …
targets for neurological diseases, in particular for Alzheimer's disease and schizophrenia …
Structure, function and drug discovery of GPCR signaling
L Cheng, F Xia, Z Li, C Shen, Z Yang, H Hou… - Molecular …, 2023 - Springer
G protein-coupled receptors (GPCRs) are versatile and vital proteins involved in a wide
array of physiological processes and responses, such as sensory perception (eg, vision …
array of physiological processes and responses, such as sensory perception (eg, vision …
Drug design targeting the muscarinic receptors and the implications in central nervous system disorders
There is substantial evidence that cholinergic system function impairment plays a significant
role in many central nervous system (CNS) disorders. During the past three decades …
role in many central nervous system (CNS) disorders. During the past three decades …
Impact of allosteric modulation in drug discovery: innovation in emerging chemical modalities
B Han, FG Salituro, MJ Blanco - ACS Medicinal Chemistry Letters, 2020 - ACS Publications
Recent years have seen an unprecedented level of innovation in allosteric drug discovery
and development, with multiple drug candidates advancing into clinical studies. From early …
and development, with multiple drug candidates advancing into clinical studies. From early …
Opportunities and challenges for the development of M1 muscarinic receptor positive allosteric modulators in the treatment for neurocognitive deficits
HTM Nguyen, ET van der Westhuizen… - British Journal of …, 2024 - Wiley Online Library
Targeting allosteric sites of M1 muscarinic acetylcholine receptors (M1 receptors) is a
promising strategy to treat neurocognitive disorders, such as Alzheimer's disease and …
promising strategy to treat neurocognitive disorders, such as Alzheimer's disease and …
Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs
Allosteric modulators are highly desirable as drugs, particularly for G-protein-coupled
receptor (GPCR) targets, because allosteric drugs can achieve selectivity between closely …
receptor (GPCR) targets, because allosteric drugs can achieve selectivity between closely …
Selective modulation of dynamic protein complexes
JM Garlick, AK Mapp - Cell chemical biology, 2020 - cell.com
Dynamic proteins perform critical roles in cellular machines, including those that control
proteostasis, transcription, translation, and signaling. Thus, dynamic proteins are prime …
proteostasis, transcription, translation, and signaling. Thus, dynamic proteins are prime …
Multitargeting nature of muscarinic orthosteric agonists and antagonists
J Myslivecek - Frontiers in Physiology, 2022 - frontiersin.org
Muscarinic receptors (mAChRs) are typical members of the G protein-coupled receptor
(GPCR) family and exist in five subtypes from M1 to M5. Muscarinic receptor subtypes do not …
(GPCR) family and exist in five subtypes from M1 to M5. Muscarinic receptor subtypes do not …
Computational investigation of drug bank compounds against 3C-like protease (3CLpro) of SARS-CoV-2 using deep learning and molecular dynamics simulation
Blocking the main replicating enzyme, 3 Chymotrypsin-like protease (3CL pro) is the most
promising drug development strategy against the SARS-CoV-2 virus, responsible for the …
promising drug development strategy against the SARS-CoV-2 virus, responsible for the …