Orthosteric and Allosteric Dual Targeting of the Nuclear Receptor RORγt with a Bitopic Ligand
Sign Up to like & getrecommendations! Published in 2021 at "ACS Chemical Biology"
DOI: 10.1021/acschembio.0c00941
Abstract: 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 IL-17a. Dysregulation of RORγt has been linked to… read more here.
Keywords: orthosteric allosteric; bit; ror; bitopic ... See more keywords
New Insights into Bitopic Orthosteric/Allosteric Ligands of Cannabinoid Receptor Type 2
Sign Up to like & getrecommendations! Published in 2023 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms24032135
Abstract: Very recently, we have developed a new generation of ligands targeting the cannabinoid receptor type 2 (CB2R), namely JR compounds, which combine the pharmacophoric portion of the CB2R positive allosteric modulator (PAM), EC21a, with that… read more here.
Keywords: bitopic dualsteric; bitopic; cannabinoid receptor; receptor type ... See more keywords
Exploring the putative mechanism of allosteric modulations by mixed-action kappa/mu opioid receptor bitopic modulators.
Sign Up to like & getrecommendations! Published in 2021 at "Future medicinal chemistry"
DOI: 10.4155/fmc-2020-0308
Abstract: The modulation and selectivity mechanisms of seven mixed-action kappa opioid receptor (KOR)/mu opioid receptor (MOR) bitopic modulators were explored. Molecular modeling results indicated that the 'message' moiety of seven bitopic modulators shared the same binding mode with the orthosteric… read more here.
Keywords: opioid receptor; mor; bitopic; bitopic modulators ... See more keywords