Designing drugs and chemical probes with the dualsteric approach
J Zha, J He, C Wu, M Zhang, X Liu… - Chemical Society Reviews, 2023 - pubs.rsc.org
Traditionally, drugs are monovalent, targeting only one site on the protein surface. This
includes orthosteric and allosteric drugs, which bind the protein at orthosteric and allosteric …
includes orthosteric and allosteric drugs, which bind the protein at orthosteric and allosteric …
[HTML][HTML] Autoregulation of GPCR signalling through the third intracellular loop
The third intracellular loop (ICL3) of the G protein-coupled receptor (GPCR) fold is important
for the signal transduction process downstream of receptor activation,–. Despite this, the lack …
for the signal transduction process downstream of receptor activation,–. Despite this, the lack …
Allosteric communication regulates ligand‐specific GPCR activity
G protein‐coupled receptors (GPCRs) are membrane‐bound proteins that are ubiquitously
expressed in many cell types and take part in mediating multiple signaling pathways …
expressed in many cell types and take part in mediating multiple signaling pathways …
[HTML][HTML] Double drugging of prolyl-tRNA synthetase provides a new paradigm for anti-infective drug development
Toxoplasmosis is caused by Toxoplasma gondii and in immunocompromised patients it may
lead to seizures, encephalitis or death. The conserved enzyme prolyl-tRNA synthetase …
lead to seizures, encephalitis or death. The conserved enzyme prolyl-tRNA synthetase …
Streamlining Design, Engineering, and Applications of Nicotinamide Riboside Kinase for Sustainable Biosynthesis of Nicotinamide Mononucleotide in Flow
F Cheng, XH Wu, H Li, KX Li, Q Guo… - ACS Sustainable …, 2023 - ACS Publications
The market demand for β-nicotinamide mononucleotide (NMN), an antiaging health product,
is rapidly expanding. Consequently, there is an urgent requirement for an environment …
is rapidly expanding. Consequently, there is an urgent requirement for an environment …
Orthosteric and allosteric dual targeting of the nuclear receptor RORγt with a bitopic ligand
FA Meijer, GJM Oerlemans, L Brunsveld - ACS Chemical Biology, 2021 - ACS Publications
The RORγt nuclear receptor (NR) is of critical importance for the differentiation and
proliferation of T helper 17 (Th17) cells and their production of the pro-inflammatory cytokine …
proliferation of T helper 17 (Th17) cells and their production of the pro-inflammatory cytokine …
Activation Microswitches in Adenosine Receptor A2A Function as Rheostats in the Cell Membrane
Although multiple components of the cell membrane modulate the stability and activation of
G protein-coupled receptors (GPCRs), insights into the dynamics of GPCR structures come …
G protein-coupled receptors (GPCRs), insights into the dynamics of GPCR structures come …
[HTML][HTML] Bayesian network models identify cooperative GPCR: G protein interactions that contribute to G protein coupling
E Mukhaleva, N Ma, WJC Van Der Velden… - Journal of Biological …, 2024 - ASBMB
Cooperative interactions in protein-protein interfaces demonstrate the interdependency or
the linked network-like behavior and their effect on the coupling of proteins. Cooperative …
the linked network-like behavior and their effect on the coupling of proteins. Cooperative …
ER/K-link—Leveraging a native protein linker to probe dynamic cellular interactions
TM Gupte, M Ritt, S Sivaramakrishnan - Methods in enzymology, 2021 - Elsevier
ER/K α-helices are a subset of single alpha helical domains, which exhibit unusual stability
as isolated protein secondary structures. They adopt an elongated structural conformation …
as isolated protein secondary structures. They adopt an elongated structural conformation …
[HTML][HTML] Kinase inhibitors allosterically disrupt a regulatory interaction to enhance PKCα membrane translocation
The eukaryotic kinase domain has multiple intrinsically disordered regions whose
conformation dictates kinase activity. Small molecule kinase inhibitors (SMKIs) rely on …
conformation dictates kinase activity. Small molecule kinase inhibitors (SMKIs) rely on …