Results 1 to 10 of about 37,458 (256)

Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator

Cells, 2022
The parathyroid hormone type 1 receptor (PTH1R) acts as a canonical class B G protein-coupled receptor, regulating crucial functions including calcium homeostasis and bone formation. The identification and development of PTH1R non-peptide allosteric modulators have obtained widespread attention.
Mengrong Li, Yiqiong Bao, Ran Xu, Miaomiao Li, Lili Xi, Jingjing Guo   +5 more
openaire   +4 more sources

Allosteric Modulation of Chemoattractant Receptors [PDF]

Frontiers in Immunology, 2016
Chemoattractants control selective leukocyte homing via interactions with a dedicated family of related G protein-coupled receptor (GPCR). Emerging evidence indicates that the signaling activity of these receptors, as for other GPCR, is influenced by allosteric modulators, which interact with the receptor in a binding site distinct from the binding ...
Maria Candida Cesta, Marcello eAllegretti, Massimo eLocati, Massimo eLocati   +3 more
openaire   +4 more sources

Allosteric modulation of gonadotropin receptors

Frontiers in Endocrinology, 2023
Gonadotropins regulate reproductive functions by binding to G protein-coupled receptors (FSHR and LHCGR) expressed in the gonads. They activate multiple, cell-specific signalling pathways, consisting of ligand-dependent intracellular events. Signalling cascades may be modulated by synthetic compounds which bind allosteric sites of FSHR and LHCGR or by ...
Clara Lazzaretti, Manuela Simoni, Manuela Simoni, Manuela Simoni, Livio Casarini, Livio Casarini, Elia Paradiso   +6 more
openaire   +4 more sources

Functional dynamics and allosteric modulation of TRPA1

Structure, 2023
The cation channel TRPA1 is a potentially important drug target, and characterization of TRPA1 functional dynamics might help guide structure-based drug design. Here, we present results from long-timescale molecular dynamics simulations of TRPA1 with an allosteric activator, allyl isothiocyanate (AITC), in which we observed spontaneous transitions from
Heidi Koldsø, Vishwanath Jogini, David E Shaw   +2 more
exaly   +3 more sources

Structural pharmacology of SV2A reveals an allosteric modulation mechanism in the major facilitator superfamily. [PDF]

Nat Commun
The synaptic vesicle glycoprotein 2A (SV2A), a member of the major facilitator superfamily (MFS), is a key target for antiseizure medications and a biomarker for synaptic density imaging.
Pidathala S, Chen X, Dai Y, Nguyen LN, Gorgulla C, Niu Y, Liu F, Lee CH.   +7 more
europepmc   +2 more sources

Conformational fingerprinting of allosteric modulators in metabotropic glutamate receptor 2

eLife, 2022
Activation of G protein-coupled receptors (GPCRs) is an allosteric process. It involves conformational coupling between the orthosteric ligand binding site and the G protein binding site. Factors that bind at non-cognate ligand binding sites to alter the
Brandon Wey-Hung Liauw, Arash Foroutan, Michael R Schamber, Weifeng Lu, Hamid Samareh Afsari, Reza Vafabakhsh   +5 more
doaj   +1 more source

Glycine Transporter 2: Mechanism and Allosteric Modulation

Frontiers in Molecular Biosciences, 2021
Neurotransmitter sodium symporters (NSS) are a subfamily of SLC6 transporters responsible for regulating neurotransmitter signalling. They are a major target for psychoactive substances including antidepressants and drugs of abuse, prompting substantial ...
Zachary J. Frangos, Ryan P. Cantwell Chater, Robert J. Vandenberg   +2 more
doaj   +1 more source

Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics

eLife, 2023
Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug discovery. Despite decades of research, a molecular-level understanding of the general principles that govern the myriad pharmacological effects exerted by GPCR ...
Ziva Vuckovic, Jinan Wang, Vi Pham, Jesse I Mobbs, Matthew J Belousoff, Apurba Bhattarai, Wessel AC Burger, Geoff Thompson, Mahmuda Yeasmin, Vindhya Nawaratne, Katie Leach, Emma T van der Westhuizen, Elham Khajehali, Yi-Lynn Liang, Alisa Glukhova, Denise Wootten, Craig W Lindsley, Andrew Tobin, Patrick Sexton, Radostin Danev, Celine Valant, Yinglong Miao, Arthur Christopoulos, David M Thal   +23 more
doaj   +1 more source

Prospects for the use of allosteric drugs in real-world clinical practice

Реальная клиническая практика: данные и доказательства, 2023
While the clinical validity of the use of allosteric regulation is known, scientists are working on the discovery of new methods for the development of allosteric drugs that can modulate the functions of enzymes, depending on the desired therapeutic ...
I. R. Svechkareva, A. S. Kolbin
doaj   +1 more source

Chronic cough relief by allosteric modulation of P2X3 without taste disturbance

Nature Communications, 2023
P2X receptors are cation channels that sense extracellular ATP. Many therapeutic candidates targeting P2X receptors have begun clinical trials or acquired approval for the treatment of refractory chronic cough (RCC) and other disorders.
Chang-Run Guo, Zhong-Zhe Zhang, Xing Zhou, Meng-Yang Sun, Tian-Tian Li, Yun-Tao Lei, Yu-Hao Gao, Qing-Quan Li, Chen-Xi Yue, Yu Gao, Yi-Yu Lin, Cui-Yun Hao, Chang-Zhu Li, Peng Cao, Michael X. Zhu, Ming-Qiang Rong, Wen-Hui Wang, Ye Yu   +17 more
doaj   +1 more source