Targeting the gatekeeper residue in phosphoinositide 3-kinases
PJ Alaimo, ZA Knight, KM Shokat
Index: Alaimo, Peter J.; Knight, Zachary A.; Shokat, Kevan M. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 8 p. 2825 - 2836
Full Text: HTML
Citation Number: 60
Abstract
A single residue in the ATP binding pocket of protein kinases—termed the gatekeeper—has been shown to control sensitivity to a wide range of small molecule inhibitors (Chem. Biol. 2004, 11, 691; Chem. Biol. 1999, 6, 671). Kinases that possess a small side chain at this position (Thr, Ala, or Gly) are readily targeted by structurally diverse classes of inhibitors, whereas kinases that possess a larger residue at this position are broadly resistant. ...
Related Articles:
Silver catalyzed zinc Barbier reaction of benzylic halides in water
[Bieber, Lothar W.; Storch, Elisabeth C.; Malvestiti, Ivani; Da Silva, Margarete F. Tetrahedron Letters, 1998 , vol. 39, # 51 p. 9393 - 9396]