Premium
Stepwise Combinatorial Evolution of Akt Bisubstrate Inhibitors
Author(s) -
Lee Jung Hwan,
Kumar Sanjai,
Lawrence David S.
Publication year - 2008
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200700583
Subject(s) - computational biology , protein kinase b , directed evolution , peptide , computer science , chemistry , kinase , combinatorial chemistry , phosphorylation , biochemistry , biology , gene , mutant
Bisubstrate analogue inhibitors have recently received considerable attention as mechanistic and structural probes of protein kinases. A stepwise library‐based strategy was employed to create a potent bisubstrate inhibitor of Akt from an extraordinarily weak nonphosphorylatable peptide. The combinatorial methodology offers a means to retain desirable properties during the directed evolution of inhibitory species.
Accelerating Research
Robert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom
Address
John Eccles HouseRobert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom