[PDF][PDF] Biased agonists of the chemokine receptor CXCR3 differentially signal through G i:-arrestin complexes

K Zheng, JS Smith, DS Eiger, A Warman, I Choi… - 2022 - dukespace.lib.duke.edu
… many chemokines act as biased agonists of their receptors (13). The receptor CXC motif
chemokine receptor 3 (CXCR3… In addition, CXCR3 has small-molecule biased agonists, such as …

Pharmacological characterization of chemokine receptor 7 (CCR7) as a potential therapeutic target in cancer

HA Basheer - 2017 - bradscholars.brad.ac.uk
… Keywords: Cancer, Chemokine, CCR7, pharmacology The expression of CCR7 was …
In addition, we characterised OSC-19 as a suitable model to evaluate small molecule CCR7 …

Recent advances in small molecule based cancer immunotherapy

B Cheng, WE Yuan, J Su, Y Liu, J Chen - European Journal of Medicinal …, 2018 - Elsevier
… In this article, we summarize the current advances in the field of small moleculechemokine
receptors and ligands (To date, nearly 50 chemokines and 20 signaling chemokine receptors

Molecular basis of ligand promiscuity, structural mimicry, and atypical dimerization in the chemokine receptors

S Saha, FK Sano, S Sharma, M Ganguly, S Saha… - bioRxiv, 2024 - biorxiv.org
… the chemokine receptors that is capable of recognizing small molecule scaffolds as agonists,
… VUF11418 and VUF10661 are dual agonists of CXCR3 and CXCR7, and therefore, by 264 …

Discovery of the potent, selective, orally available CXCR7 antagonist ACT-1004-1239

S Richard-Bildstein, H Aissaoui, J Pothier… - Journal of Medicinal …, 2020 - ACS Publications
chemokine ligand 12). Importantly, CXCL11 and CXCL12 also bind to the chemokine
receptors CXCR3 … the addition of 5 nM of the small molecule agonist 1. Compounds from our …

Physiological Functions of Biased Signaling at the Chemokine Receptor CXCR3

JS Smith - 2019 - search.proquest.com
… that regulates T cell function, and its endogenous chemokines CXCL9, CXCL10, and …
signaling exists at CXCR3. After identifying small molecule biased CXCR3 agonists using cell-…

Development of photoactivatable allosteric modulators for the chemokine receptor CXCR3

TH Admas, V Bernat, MR Heinrich… - …, 2016 - Wiley Online Library
CXCR3 allosteric binding pocket of AMG 487 and RAMX3, two potent and selective
CXCR3 … Photoaffinity labeling is a common approach to elucidate binding modes of small-molecule

Biased agonism at chemokine receptors: obstacles or opportunities for drug discovery?

CA Anderson, R Solari, JE Pease - Journal of Leucocyte Biology, 2016 - academic.oup.com
receptor is notable for the fact that it binds both the CXCR3 … , no small-molecule chemokine
receptor antagonists have been … Pharmacological characterization of the chemokine receptor, …

Insight into structural requirements for selective and/or dual CXCR3 and CXCR4 allosteric modulators

A Kolarič, U Švajger, T Tomašič, R Brox, T Frank… - European journal of …, 2018 - Elsevier
… 1), we can conclude that in general, small molecule ligands consist of aromatic … characterized
novel negative and positive allosteric modulators of the chemokine receptors CXCR3

[图书][B] Synthesis of the first allosteric biased agonists and computational investigations for the human chemokine receptor CXCR3

L Milanos - 2016 - search.proquest.com
… of small-molecule agonists of CXCR3 was largely neglected and only a few agonists
were … We combined this approach with detailed pharmacological characterization of novel …