Results 21 to 30 of about 19,325 (262)

Filamentation modulates allosteric regulation of PRPS

eLife, 2022
Phosphoribosyl pyrophosphate (PRPP) is a key intermediate in the biosynthesis of purine and pyrimidine nucleotides, histidine, tryptophan, and cofactors NAD and NADP. Abnormal regulation of PRPP synthase (PRPS) is associated with human disorders, including Arts syndrome, retinal dystrophy, and gouty arthritis.
Chia-Chun Chang, Guang-Ming Lu, Huan-Huan Hu, Yilan Li, Jiale Zhong, Chen-Jun Guo, Xian Zhou, Boqi Yin, Tianyi Zhang, Ji-Long Liu   +9 more
openaire   +3 more sources

Indomethacin Enhances Type 1 Cannabinoid Receptor Signaling

Frontiers in Molecular Neuroscience, 2019
In addition to its known actions as a non-selective cyclooxygenase (COX) 1 and 2 inhibitor, we hypothesized that indomethacin can act as an allosteric modulator of the type 1 cannabinoid receptor (CB1R) because of its shared structural features with the ...
Robert B. Laprairie, Robert B. Laprairie, Kawthar A. Mohamed, Ayat Zagzoog, Melanie E. M. Kelly, Melanie E. M. Kelly, Lesley A. Stevenson, Roger Pertwee, Eileen M. Denovan-Wright, Ganesh A. Thakur   +9 more
doaj   +1 more source

Conformational transitions and allosteric modulation in a heteromeric glycine receptor

Nature Communications, 2023
Glycine receptors (GlyR) are a critical postsynaptic component of spinal neurons. Here, the auhtors present cryo-EM structures of a heteromeric GlyR in the presence of an antagonist, agonist and agonist with a positive allosteric modulator.
Eric Gibbs, Emily Klemm, David Seiferth, Arvind Kumar, Serban L. Ilca, Philip C. Biggin, Sudha Chakrapani   +6 more
doaj   +1 more source

An NMDAR positive and negative allosteric modulator series share a binding site and are interconverted by methyl groups

eLife, 2018
N-methyl-d-aspartate receptors (NMDARs) are an important receptor in the brain and have been implicated in multiple neurological disorders. Many non-selective NMDAR-targeting drugs are poorly tolerated, leading to efforts to target NMDAR subtypes to ...
Riley Perszyk, Brooke M Katzman, Hirofumi Kusumoto, Steven A Kell, Matthew P Epplin, Yesim A Tahirovic, Rhonda L Moore, David Menaldino, Pieter Burger, Dennis C Liotta, Stephen F Traynelis   +10 more
doaj   +1 more source

Functional Consequences of GPCR Heterodimerization: GPCRs as Allosteric Modulators

Pharmaceuticals, 2011
G Protein Coupled Receptors (GPCRs) represent the largest family of membrane proteins in the human genome, are the targets of approximately 25% of all marketed pharmaceuticals, and the focus of intensive research worldwide given that this superfamily of ...
Karla K.V. Haack, Nael A. McCarty
doaj   +1 more source

Allosteric Modulator Leads Hiding in Plain Site: Developing Peptide and Peptidomimetics as GPCR Allosteric Modulators [PDF]

Frontiers in Chemistry, 2021
Allosteric modulators (AMs) of G-protein coupled receptors (GPCRs) are desirable drug targets because they can produce fewer on-target side effects, improved selectivity, and better biological specificity (e.g., biased signaling or probe dependence) than orthosteric drugs.
Keith M. Olson, John R. Traynor, John R. Traynor, Andrew Alt, Andrew Alt   +4 more
openaire   +3 more sources

An Allosteric Modulator of the Adenosine A1 Receptor Improves Cardiac Function Following Ischaemia in Murine Isolated Hearts

Pharmaceuticals, 2013
The effect of an allosteric modulator of the adenosine A1 receptors was investigated using an ischaemia-reperfusion protocol in murine isolated hearts. Isolated hearts were perfused with Kreb-Henseleit solution gassed with carbogen gas (95% O2 and 5% CO2)
Roselyn B. Rose'Meyer, Shane M. Devine, Peter J. Scammells, Paul J. White, Anna Butcher   +4 more
doaj   +1 more source

Kinetic Trans-omic Analysis Reveals Key Regulatory Mechanisms for Insulin-Regulated Glucose Metabolism in Adipocytes

iScience, 2020
Summary: Insulin regulates glucose metabolism through thousands of regulatory mechanisms; however, which regulatory mechanisms are keys to control glucose metabolism remains unknown.
Satoshi Ohno, Lake-Ee Quek, James R. Krycer, Katsuyuki Yugi, Akiyoshi Hirayama, Satsuki Ikeda, Futaba Shoji, Kumi Suzuki, Tomoyoshi Soga, David E. James, Shinya Kuroda   +10 more
doaj   +1 more source

Identification of potential small molecule allosteric modulator sites on IL-1R1 ectodomain using accelerated conformational sampling method.

PLoS ONE, 2015
The interleukin-1 receptor (IL-1R) is the founding member of the interleukin 1 receptor family which activates innate immune response by its binding to cytokines.
Chao-Yie Yang
doaj   +1 more source

Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Nature Communications, 2021
Here, the authors use smFRET to assess the structural dynamics of metabotropic glutamate receptor mGlu2 and show that a positive allosteric modulator or the Gi protein stabilize mGlu2 in the glutamate-induced active state, leading to the full activation ...
Anne-Marinette Cao, Robert B. Quast, Fataneh Fatemi, Philippe Rondard, Jean-Philippe Pin, Emmanuel Margeat   +5 more
doaj   +1 more source