TY - JOUR
T1 - Genetically selected cyclic-peptide inhibitors of AICAR transformylase homodimerization
AU - Tavassoli, Ali
AU - Benkovic, Stephen J.
PY - 2005/4/29
Y1 - 2005/4/29
N2 - (Graph Presented) Finding the needle in a haystack need not be as troublesome as once thought. By coupling disruption of protein-protein (X-X) interactions to host-cell survival (see figure), inhibitors of ATIC (a key enzyme in the de novo purine biosynthetic pathway) were readily identified from a biosynthesized library of 107 small molecules. The activity and selectivity of nine cyclic peptides selected by this method were demonstrated in vivo and in vitro. AICAR=aminoimidazole-4-carboxamide ribonucleotide.
AB - (Graph Presented) Finding the needle in a haystack need not be as troublesome as once thought. By coupling disruption of protein-protein (X-X) interactions to host-cell survival (see figure), inhibitors of ATIC (a key enzyme in the de novo purine biosynthetic pathway) were readily identified from a biosynthesized library of 107 small molecules. The activity and selectivity of nine cyclic peptides selected by this method were demonstrated in vivo and in vitro. AICAR=aminoimidazole-4-carboxamide ribonucleotide.
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U2 - 10.1002/anie.200500417
DO - 10.1002/anie.200500417
M3 - Article
C2 - 15830403
AN - SCOPUS:18844408408
SN - 1433-7851
VL - 44
SP - 2760
EP - 2763
JO - Angewandte Chemie - International Edition
JF - Angewandte Chemie - International Edition
IS - 18
ER -