| Structural highlights
Function
RORG_HUMAN Possible nuclear receptor for hydroxycholesterols, the binding of which strongly promotes coactivators recruitment. Essential for thymopoiesis and the development of several secondary lymphoid tissues, including lymph nodes. Involved in lineage specification of uncommitted CD4(+) T-helper cells into Th17 cells. Regulate the expression of several components of the circadian clock.
Publication Abstract from PubMed
A novel series of tertiary amines as retinoid-related orphan receptor gamma-t (RORgammat) inverse agonists was discovered through agonist/inverse agonist conversion. The level of RORgammat inhibition can be enhanced by modulating the conformational disruption of H12 in RORgammat LBD. Linker exploration and rational design led to the discovery of more potent indole-based RORgammat inverse agonists.
Discovery of Tertiary Amine and Indole Derivatives as Potent RORgammat Inverse Agonists.,Yang T, Liu Q, Cheng Y, Cai W, Ma Y, Yang L, Wu Q, Orband-Miller LA, Zhou L, Xiang Z, Huxdorf M, Zhang W, Zhang J, Xiang JN, Leung S, Qiu Y, Zhong Z, Elliott JD, Lin X, Wang Y ACS Med Chem Lett. 2013 Nov 22;5(1):65-8. doi: 10.1021/ml4003875. eCollection, 2014 Jan 9. PMID:24900774[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Yang T, Liu Q, Cheng Y, Cai W, Ma Y, Yang L, Wu Q, Orband-Miller LA, Zhou L, Xiang Z, Huxdorf M, Zhang W, Zhang J, Xiang JN, Leung S, Qiu Y, Zhong Z, Elliott JD, Lin X, Wang Y. Discovery of Tertiary Amine and Indole Derivatives as Potent RORgammat Inverse Agonists. ACS Med Chem Lett. 2013 Nov 22;5(1):65-8. doi: 10.1021/ml4003875. eCollection, 2014 Jan 9. PMID:24900774 doi:http://dx.doi.org/10.1021/ml4003875
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