- Ribonuclease-Activated Cancer Prodrug
[作者:ELLIS GREGORY A; MCGRATH NICHOLAS A; PALTE MICHAEL J; RAINES RONALD T,期刊:ACS Medicinal Chemistry Letters, 页码:268-272 , 文章类型: Article,,卷期:2012年3-4]
- Cancer chemotherapeutic agents often have a narrow therapeutic index that challenges the maintenance of a safe and effective dose. Consistent plasma concentrations of a drug can be obtained by using a timed-release prodr...
- Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization
[作者:DOWLING JAMES E; CHUAQUI CLAUDIO; PONTZ TIMOTHY W; LYNE PAUL D; LARSEN NICHOLAS A; BLOCK MICHAEL H; CHEN HUAWEI; SU NANCY; WU ALLAN; RUSSELL DANIEL; POLLARD HANNAH; LEE JOHN W; PENG BO; THAKUR KUMAR; YE QING; ZHANG TAO; BRASSIL PATRICK; RACICOT VICKI; BAO LARRY; DENZ CHRISTOPHER R; COOKE EMMA,期刊:ACS Medicinal Chemistry Letters, 页码:278-283 , 文章类型: Article,,卷期:2012年3-4]
- In this paper we describe a series of 3-cyano-5-aryl-7-aminopyrazolo[1,5-a]-pyrimidine hits identified by kinase-focused subset screening as starting points for the structure-based design of conformationally constrained ...
- Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst(3) Antagonist
[作者:PASTERNAK ALEXANDER; FENG ZHE; DE JESUS REYNALDA; YE ZHIXIONG; HE SHUWEN; DOBBELAAR PETER; BRADLEY SCOTT A; CHICCHI GARY G; TSAO KWEILAN; TRUSCA DORINA; EIERMANN GEORGE J; LI CAI; FENG YUE; WU MARGARET; SHAO QING; ZHANG BEI B; NARGUND RAVI; MILLS SANDER G; HOWARD ANDREW D; YANG LIHU; ZHOU YUNPING,期刊:ACS Medicinal Chemistry Letters, 页码:289-293 , 文章类型: Article,,卷期:2012年3-4]
- This letter provides the first pharmacological proof of principle that the sst(3) receptor mediates glucose-stimulated insulin secretion (GSIS) from pancreatic beta-cells. To enable these studies, we identified the selec...
- Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor
[作者:HARPER STEVEN; MCCAULEY JOHN A; RUDD MICHAEL T; FERRARA MARCO; DIFILIPPO MARCELLO; CRESCENZI BENEDETTA; KOCH UWE; PETROCCHI ALESSIA; HOLLOWAY M KATHARINE; BUTCHER JOHN W; ROMANO JOSEPH J; BUSH KIMBERLY J; GILBERT KEVIN F; MCINTYRE CHARLES J; NGUYEN KEVIN T; NIZI EMANUELA; CARROLL STEVEN S; LUDMERER STEVEN W; BURLEIN CHRISTINE; DIMUZIO JILLIAN M; GRAHAM DONALD J; MCHALE CAROLYN M; STAHLHUT MARK W; OLSEN DAVID B; MONTEAGUDO EDITH; CIANETTI SIMONA; GIULIANO CLAUDIO; PUCCI VINCENZO; TRAINOR NICOLE; FANDOZZI CHRISTINE M; ROWLEY MICHAEL; COLEMAN PAUL J; VACCA JOSEPH P; SUMMA VINCENZO; LIVERTON NIGEL J,期刊:ACS Medicinal Chemistry Letters, 页码:332-336 , 文章类型: Article,,卷期:2012年3-4]
- A new class of HCV NS3/4a protease inhibitors containing a P2 to P4 macrocyclic constraint was designed using a molecular modeling-derived strategy. Building on the profile of previous clinical compounds and exploring th...
|