GPR35: from enigma to therapeutic target
G Milligan - Trends in Pharmacological Sciences, 2023 - cell.com
The orphan G-protein-coupled receptor 35 (GPR35), although poorly characterised, is
attracting considerable interest as a therapeutic target. Marked differences in pharmacology …
attracting considerable interest as a therapeutic target. Marked differences in pharmacology …
GPR35 and mediators from platelets and mast cells in neutrophil migration and inflammation
Neutrophil recruitment from circulation to sites of inflammation is guided by multiple
chemoattractant cues emanating from tissue cells, immune cells, and platelets. Here, we …
chemoattractant cues emanating from tissue cells, immune cells, and platelets. Here, we …
Allosteric regulation of G-protein-coupled receptors: from diversity of molecular mechanisms to multiple allosteric sites and their ligands
AO Shpakov - International Journal of Molecular Sciences, 2023 - mdpi.com
Allosteric regulation is critical for the functioning of G protein-coupled receptors (GPCRs)
and their signaling pathways. Endogenous allosteric regulators of GPCRs are simple ions …
and their signaling pathways. Endogenous allosteric regulators of GPCRs are simple ions …
GPR35 acts a dual role and therapeutic target in inflammation
Y Wu, P Zhang, H Fan, C Zhang, P Yu, X Liang… - Frontiers in …, 2023 - frontiersin.org
GPR35 is a G protein-coupled receptor with notable involvement in modulating inflammatory
responses. Although the precise role of GPR35 in inflammation is not yet fully understood …
responses. Although the precise role of GPR35 in inflammation is not yet fully understood …
GPR35 antagonist CID-2745687 attenuates anchorage-independent cell growth by inhibiting YAP/TAZ activity in colorectal cancer cells
W Otkur, X Liu, H Chen, S Li, T Ling, H Lin… - Frontiers in …, 2023 - frontiersin.org
Background and purpose: GPR35, a member of the orphan G-protein-coupled receptor, was
recently implicated in colorectal cancer (CRC). However, whether targeting GPR35 by …
recently implicated in colorectal cancer (CRC). However, whether targeting GPR35 by …
Recent advances in GPR35 pharmacology; 5-HIAA serotonin metabolite becomes a ligand
DS Im - Archives of Pharmacal Research, 2023 - Springer
GPR35, an orphan receptor, has been waiting for its ligand since its cloning in 1998. Many
endogenous and exogenous molecules have been suggested to act as agonists of GPR35 …
endogenous and exogenous molecules have been suggested to act as agonists of GPR35 …
Allosteric drugs: New principles and design approaches
WV Tee, IN Berezovsky - Current Opinion in Structural Biology, 2024 - Elsevier
Focusing on an important biomedical implication of allostery–design of allosteric drugs, we
describe characteristics of allosteric sites, effectors, and their modes of actions …
describe characteristics of allosteric sites, effectors, and their modes of actions …
[HTML][HTML] Multi-omics approach to identifying isoform variants as therapeutic targets in cancer patients
Cancer-specific alternatively spliced events (ASE) play a role in cancer pathogenesis and
can be targeted by immunotherapy, oligonucleotide therapy, and small molecule inhibition …
can be targeted by immunotherapy, oligonucleotide therapy, and small molecule inhibition …
Activation of Multiple G Protein Pathways to Characterize the Five Dopamine Receptor Subtypes Using Bioluminescence Technology
D Mönnich, LJ Humphrys, C Höring… - ACS Pharmacology & …, 2024 - ACS Publications
G protein-coupled receptors show preference for G protein subtypes but can recruit multiple
G proteins with various downstream signaling cascades. This functional selection can guide …
G proteins with various downstream signaling cascades. This functional selection can guide …
Nanobody-mediated dualsteric engagement of the angiotensin receptor broadens biased ligand pharmacology
NB Emidio, BM Small, AR Keller, RW Cheloha… - Molecular …, 2024 - ASPET
Dualsteric G protein-coupled receptor (GPCR) ligands are a class of bitopic ligands that
consist of an orthosteric pharmacophore, which binds to the pocket occupied by the …
consist of an orthosteric pharmacophore, which binds to the pocket occupied by the …