1e2l
From Proteopedia
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Revision as of 12:59, 30 October 2007
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KINETICS AND CRYSTAL STRUCTURE OF THE WILD-TYPE AND THE ENGINEERED Y101F MUTANT OF HERPES SIMPLEX VIRUS TYPE 1 THYMIDINE KINASE INTERACTING WITH (NORTH)-METHANOCARBA-THYMIDINE
Overview
Kinetic and crystallographic analyses of wild-type Herpes simplex virus, type 1 thymidine kinase (TK(HSV1)) and its Y101F-mutant [TK(HSV1)(Y101F)], acting on the potent antiviral drug 2'-exo-methanocarba-thymidine (MCT), have been performed. The kinetic study reveals a 12-fold K(M) increase for, thymidine processed with Y101F as compared to the wild-type TK(HSV1)., Furthermore, MCT is a substrate for both wild-type and mutant TK(HSV1)., Its binding affinity for TK(HSV1) and TK(HSV1)(Y101F), expressed as K(i), is 11 microM and 51 microM, respectively, whereas the K(i) for human, cytosolic thymidine kinase is as high as 1.6 mM, rendering TK(HSV1) a, selectivity filter for antiviral activity. Moreover, TK(HSV1)(Y101F) shows, a decrease in the quotient of the catalytic efficiency ... [(full description)]
About this Structure
1E2L is a [Single protein] structure of sequence from [Human herpesvirus 4] with SO4 and TMC as [ligands]. Active as [Thymidine kinase], with EC number [2.7.1.21]. Structure known Active Sites: AC1 and AC2. Full crystallographic information is available from [OCA].
Reference
Kinetics and crystal structure of the wild-type and the engineered Y101F mutant of Herpes simplex virus type 1 thymidine kinase interacting with (North)-methanocarba-thymidine., Prota A, Vogt J, Pilger B, Perozzo R, Wurth C, Marquez VE, Russ P, Schulz GE, Folkers G, Scapozza L, Biochemistry. 2000 Aug 8;39(31):9597-603. PMID:10924157
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