Discovery of novel hepatoselective HMG-CoA reductase inhibitors for treating hypercholesterolemia: a bench-to-bedside case study on tissue selective drug distribution.

Autor: Pfefferkorn JA; Pfizer Global Research & Development, Eastern Point Road, Groton, CT 06340, USA. jeffrey.a.pfefferkorn@pfizer.com, Litchfield J, Hutchings R, Cheng XM, Larsen SD, Auerbach B, Bush MR, Lee C, Erasga N, Bowles DM, Boyles DC, Lu G, Sekerke C, Askew V, Hanselman JC, Dillon L, Lin Z, Robertson A, Olsen K, Boustany C, Atkinson K, Goosen TC, Sahasrabudhe V, Chupka J, Duignan DB, Feng B, Scialis R, Kimoto E, Bi YA, Lai Y, El-Kattan A, Bakker-Arkema R, Barclay P, Kindt E, Le V, Mandema JW, Milad M, Tait BD, Kennedy R, Trivedi BK, Kowala M

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 May 01; Vol. 21 (9), pp. 2725-31. Date of Electronic Publication: 2010 Nov 26.

Effects of tunicamycin on the binding and degradation of low density lipoproteins and glycoprotein synthesis in cultured human fibroblasts.

Autor: Chatterjee, S, Kwiterovich, P O, Sekerke, C S

Publikováno v: Journal of Biological Chemistry; May 1979, Vol. 254 Issue: 10 p3704-3707, 4p

Divergent pharmacologic activities of PD 132301-2 and CL 277,082, urea inhibitors of acyl-CoA:cholesterol acyltransferase.

Autor: Krause, B R, Black, A, Bousley, R, Essenburg, A, Cornicelli, J, Holmes, A, Homan, R, Kieft, K, Sekerke, C, Shaw-Hes, M K

Publikováno v: The Journal of Pharmacology and Experimental Therapeutics; November 1993, Vol. 267 Issue: 2 p734-743, 10p

Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic acid (PF-3052334) as a candidate for the treatment of hypercholesterolemia.

Autor: Pfefferkorn JA; Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, Michigan 48105, USA. jeffrey.a.pfefferkorn@pfizer.com, Choi C, Larsen SD, Auerbach B, Hutchings R, Park W, Askew V, Dillon L, Hanselman JC, Lin Z, Lu GH, Robertson A, Sekerke C, Harris MS, Pavlovsky A, Bainbridge G, Caspers N, Kowala M, Tait BD

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2008 Jan 10; Vol. 51 (1), pp. 31-45. Date of Electronic Publication: 2007 Dec 12.

Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase.

Autor: Bratton LD; Pfizer Global Research and Development, Michigan Laboratories, Ann Arbor, MI 48105, USA., Auerbach B, Choi C, Dillon L, Hanselman JC, Larsen SD, Lu G, Olsen K, Pfefferkorn JA, Robertson A, Sekerke C, Trivedi BK, Unangst PC

Publikováno v: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2007 Aug 15; Vol. 15 (16), pp. 5576-89. Date of Electronic Publication: 2007 May 17.