Discovery and Exploration of Disubstituted [1,2,5]Oxadiazolo-[3,4-B]Pyrazines as Novel C-C Chemokine Receptor Type 5 Signaling Inhibitors Targeting the Intracellular Allosteric Binding Pocket DOI
Margaux Billen, Sten Reynders, Sandra Claes

et al.

Published: Jan. 1, 2024

Language: Английский

GPCR drug discovery: new agents, targets and indications DOI
José A. Lorente, Aleksandr V. Sokolov, Gavin Ferguson

et al.

Nature Reviews Drug Discovery, Journal Year: 2025, Volume and Issue: unknown

Published: March 3, 2025

Language: Английский

Citations

4
The Use of Biologics for Targeting GPCRs in Metastatic Cancers DOI Creative Commons
Cian McBrien, David O’Connell

BioTech, Journal Year: 2025, Volume and Issue: 14(1), P. 7 - 7

Published: Jan. 30, 2025

A comprehensive review of studies describing the role G-protein coupled receptor (GPCR) behaviour contributing to metastasis in cancer, and developments biotherapeutic drugs towards targeting them, provides a valuable resource toward improving our understanding opportunities effectively target this malignant tumour cell adaptation. Focusing on five most common metastatic cancers lung, breast, colorectal, melanoma, prostate we highlight well-studied characterised GPCRs some less studied receptors that are also implicated development cancers. Of approximately 390 relevant therapeutic targeting, as many 125 these have been identified play promoting disease cancer types. GPCR signalling through well-characterised pathways chemokine receptors, emerging data by orphan is integral aspects phenotype. Despite having detailed information their ligands, there only thirteen approved therapeutics specifically for which three small molecules with remainder including synthetic non-synthetic peptides or monoclonal antibodies. This will cover existing potential use antibodies, proteins peptides, nanobodies therapy.

Language: Английский

Citations

0
Discovery and exploration of disubstituted [1,2,5]oxadiazolo- [3,4-b]pyrazines as novel C-C chemokine receptor type 5 signaling inhibitors targeting the intracellular allosteric binding pocket DOI
Margaux Billen, Sten Reynders, Sandra Claes

et al.

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 117600 - 117600

Published: April 1, 2025

Language: Английский

Citations

0
Discovery and Exploration of Disubstituted [1,2,5]Oxadiazolo-[3,4-B]Pyrazines as Novel C-C Chemokine Receptor Type 5 Signaling Inhibitors Targeting the Intracellular Allosteric Binding Pocket DOI
Margaux Billen, Sten Reynders, Sandra Claes

et al.

Published: Jan. 1, 2024

Language: Английский

Citations

0