Title : Rapid development of a potent photo-triggered inhibitor of the serine hydrolase RBBP9 - Liu_2012_Chembiochem_13_2082 |
Author(s) : Liu X , Dix M , Speers AE , Bachovchin DA , Zuhl AM , Cravatt BF , Kodadek TJ |
Ref : Chembiochem , 13 :2082 , 2012 |
Abstract :
The serine hydrolases constitute a large class of enzymes that play important roles in physiology. There is great interest in the development of potent and selective pharmacological inhibitors of these proteins. Traditional active-site inhibitors often have limited selectivity within this superfamily and are tedious and expensive to discover. Using the serine hydrolase RBBP9 as a model target, we designed a rapid and relatively inexpensive route to highly selective peptoid-based inhibitors that can be activated by visible light. This technology provides rapid access to photo-activated tool compounds capable of selectively blocking the function of particular serine hydrolases. |
PubMedSearch : Liu_2012_Chembiochem_13_2082 |
PubMedID: 22907802 |
Gene_locus related to this paper: human-RBBP9 |
Gene_locus | human-RBBP9 |
Family | Hydrolase_RBBP9_YdeN |
Liu X, Dix M, Speers AE, Bachovchin DA, Zuhl AM, Cravatt BF, Kodadek TJ (2012)
Rapid development of a potent photo-triggered inhibitor of the serine hydrolase RBBP9
Chembiochem
13 :2082
Liu X, Dix M, Speers AE, Bachovchin DA, Zuhl AM, Cravatt BF, Kodadek TJ (2012)
Chembiochem
13 :2082