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 …

GPR35 and mediators from platelets and mast cells in neutrophil migration and inflammation

M De Giovanni, H Chen, X Li… - Immunological Reviews, 2023 - Wiley Online Library
Neutrophil recruitment from circulation to sites of inflammation is guided by multiple
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 …

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 …

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 …

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 …

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 …

[HTML][HTML] Multi-omics approach to identifying isoform variants as therapeutic targets in cancer patients

TI Shaw, B Zhao, Y Li, H Wang, L Wang… - Frontiers in …, 2022 - frontiersin.org
Cancer-specific alternatively spliced events (ASE) play a role in cancer pathogenesis and
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 …

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 …