Results 41 to 50 of about 4,452,404 (339)
The CB1 cannabinoid receptor (CB1R) contains one of the longest N termini among class A G protein-coupled receptors. Mutagenesis studies suggest that the allosteric binding site of cannabidiol (CBD) involves residues from the N terminal domain.
Jakub Jakowiecki +5 more
doaj +1 more source
Allosite: a method for predicting allosteric sites [PDF]
Abstract Motivation: The use of allosteric modulators as preferred therapeutic agents against classic orthosteric ligands has colossal advantages, including higher specificity, fewer side effects and lower toxicity. Therefore, the computational prediction of allosteric sites in proteins is receiving increased attention in the field of ...
Wenkang, Huang +10 more
openaire +2 more sources
Methicillin-resistant Staphylococcus aureus (MRSA) tolerates β-lactam antibiotics by carrying out cell wall synthesis with the transpeptidase Penicillin-binding protein 2a (PBP2a), which cannot be inhibited by β-lactams. It has been proposed that PBP2a’s
Y. Chiang, M. Wong, J. Essex
semanticscholar +1 more source
A common allosteric site and mechanism in caspases [PDF]
We present a common allosteric mechanism for control of inflammatory and apoptotic caspases. Highly specific thiol-containing inhibitors of the human inflammatory caspase-1 were identified by using disulfide trapping, a method for site-directed small-molecule discovery.
Justin M, Scheer +2 more
openaire +2 more sources
α-conotoxins are 13–19 amino acid toxin peptides that bind various nicotinic acetylcholine receptor (nAChR) subtypes. α-conotoxin Mr1.7c (MrIC) is a 17 amino acid peptide that targets α7 nAChR.
Alican Gulsevin +6 more
doaj +1 more source
Development of allosteric modulators of GPCRs for treatment of CNS disorders
The discovery of allosteric modulators of G protein-coupled receptors (GPCRs) provides a promising new strategy with potential for developing novel treatments for a variety of central nervous system (CNS) disorders.
Hilary Highfield Nickols +1 more
doaj +1 more source
The dopamine transporter (DAT) serves a critical role in controlling dopamine (DA)-mediated neurotransmission by regulating the clearance of DA from the synapse and extrasynaptic regions and thereby modulating DA action at postsynaptic DA receptors ...
Shaili Aggarwal +4 more
doaj +1 more source
The novel coronavirus disease 2019 (COVID‐19) caused by severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) still has serious negative effects on health, social life, and economics.
Merve Yuce +5 more
semanticscholar +1 more source
Considerable progress has been made in recent years towards the identification and characterisation of novel subtype-selective modulators of nicotinic acetylcholine receptors (nAChRs).
Victoria R. Sanders, Neil S. Millar
doaj +1 more source
Structure and allosteric regulation of human NAD-dependent isocitrate dehydrogenase
Human NAD-dependent isocitrate dehydrogenase or HsIDH3 catalyzes the decarboxylation of isocitrate into α-ketoglutarate in the TCA cycle. HsIDH3 exists and functions as a heterooctamer composed of the αβ and αγ heterodimers, and is regulated ...
Pengkai Sun +3 more
doaj +1 more source

