Title of article
Design and identification of selective HER-2 sheddase inhibitors via P1′ manipulation and unconventional P2′ perturbations to induce a molecular metamorphosis
Author/Authors
Wenqing Yao، نويسنده , , Jincong Zhuo، نويسنده , , David M. Burns، نويسنده , , Yun-Long Li، نويسنده , , Ding-Quan Qian، نويسنده , , Colin Zhang، نويسنده , , Chunhong He، نويسنده , , Meizhong Xu، نويسنده , , Eric Shi، نويسنده , , Yanlong Li، نويسنده , , Cindy A. Marando، نويسنده , , Maryanne B. Covington، نويسنده , , Gengjie Yang، نويسنده , , Xiangdong Liu، نويسنده , , Max Pan، نويسنده , , Jordan S. Fridman، نويسنده , , Peggy Scherle، نويسنده , , Zelda R. Wasserman، نويسنده , , Gregory Hollis، نويسنده , , Kris Vaddi، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
159
To page
163
Abstract
In an effort to obtain a MMP selective and potent inhibitor of HER-2 sheddase (ADAM-10), the P1′ group of a novel class of (6S,7S)-7-[(hydroxyamino)carbonyl]-6-carboxamide-5-azaspiro[2.5]octane-5-carboxylates was attenuated and the structure–activity relationships (SAR) will be discussed. In addition, it was discovered that unconventional perturbation of the P2′ moiety could confer MMP selectivity, which was hypothesized to be a manifestation of the P2′ group effecting global conformational changes.
Keywords
P2? group , SAR , piperidine , Global conformation , HER-2 sheddase , ADAM-10 , metalloprotease , MMP , P1? group , Hydroxamic acid
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798938
Link To Document