Structural highlights
Function
[HMDH_HUMAN] Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins.
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
Using structure-based design, a novel series of conformationally restricted, pyrrole-based inhibitors of HMG-CoA reductase were discovered. Leading analogs demonstrated potent inhibition of cholesterol synthesis in both in vitro and in vivo models and may be useful for the treatment of hypercholesterolemia and related lipid disorders.
Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors.,Pfefferkorn JA, Choi C, Song Y, Trivedi BK, Larsen SD, Askew V, Dillon L, Hanselman JC, Lin Z, Lu G, Robertson A, Sekerke C, Auerbach B, Pavlovsky A, Harris MS, Bainbridge G, Caspers N Bioorg Med Chem Lett. 2007 Aug 15;17(16):4531-7. Epub 2007 Jun 6. PMID:17574411[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Pfefferkorn JA, Choi C, Song Y, Trivedi BK, Larsen SD, Askew V, Dillon L, Hanselman JC, Lin Z, Lu G, Robertson A, Sekerke C, Auerbach B, Pavlovsky A, Harris MS, Bainbridge G, Caspers N. Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4531-7. Epub 2007 Jun 6. PMID:17574411 doi:10.1016/j.bmcl.2007.05.097
