Author/Authors :
Krystal J. Alligood، نويسنده , , Paul S. Charifson، نويسنده , , Renae Crosby، نويسنده , , Thomas G. Consler، نويسنده , , Paul L. Feldman، نويسنده , , Robert T. Gampe Jr.، نويسنده , , Tona M. Gilmer، نويسنده , , Steven R. Jordan، نويسنده , , Mark W. Milstead، نويسنده , , Christopher Mohr، نويسنده , , Michael R. Peel، نويسنده , , Warren Rocque، نويسنده , , Marc Rodriguez، نويسنده , , David W. Rusnak، نويسنده , , Lisa M. Shewchuk، نويسنده , , Daniel D. Sternbach، نويسنده ,
Abstract :
The X-ray crystal structure of the src SH2 domain revealed the presence of a thiol residue (Cys 188) located proximal to the phosphotyrosine portion of a dipeptide ligand. An aldehyde bearing ligand (1) was designed to position an electrophilic carbonyl group in the vicinity of the thiol. X-ray crystallographic and NMR examination of the complex formed between (1) and the src SH2 domain revealed a hemithioacetal formed by addition of the thiol to the aldehyde group with an additional stabilizing hydrogen bond between the acetal hydroxyl and a backbone carbonyl.
