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5KYJ

Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core

Summary for 5KYJ
Entry DOI10.2210/pdb5kyj/pdb
Related5I4V 5KYA
DescriptorOxysterols receptor LXR-beta, Retinoic acid receptor RXR-beta, (6~{R})-5-(5-fluoranyl-2-methoxy-pyrimidin-4-yl)-2-(3-methylsulfonylphenyl)-6-propan-2-yl-4,6-dihydropyrrolo[3,4-c]pyrazole, ... (4 entities in total)
Functional Keywordsdna binding protein, nuclear receptors, liver x receptor, retinoic acid x receptor, lxrbeta-lbd/rxrbeta-lbd heterodimer, chemical modulators
Biological sourceHomo sapiens (Human)
More
Cellular locationNucleus : P55055 P28702
Total number of polymer chains4
Total formula weight122281.91
Authors
Chen, G.,McKeever, B.M. (deposition date: 2016-07-21, release date: 2016-09-21, Last modification date: 2023-10-04)
Primary citationTice, C.M.,Noto, P.B.,Fan, K.Y.,Zhao, W.,Lotesta, S.D.,Dong, C.,Marcus, A.P.,Zheng, Y.J.,Chen, G.,Wu, Z.,Van Orden, R.,Zhou, J.,Bukhtiyarov, Y.,Zhao, Y.,Lipinski, K.,Howard, L.,Guo, J.,Kandpal, G.,Meng, S.,Hardy, A.,Krosky, P.,Gregg, R.E.,Leftheris, K.,McKeever, B.M.,Singh, S.B.,Lala, D.,McGeehan, G.M.,Zhuang, L.,Claremon, D.A.
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
Bioorg.Med.Chem.Lett., 26:5044-5050, 2016
Cited by
PubMed: 27599745
DOI: 10.1016/j.bmcl.2016.08.089
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.8 Å)
Structure validation

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