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Scaffold rearrangement of dihydroxypyrimidine inhibitors of HIV integrase: Docking model revisited by Jing Tang; Kasthuraiah Maddali; Yves Pommier; Yuk Y. Sham; Zhengqiang Wang is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Scaffold rearrangement of dihydroxypyrimidine inhibitors of HIV integrase: Docking model revisited about?

A series of dihydroxypyrimidine (DHP) derivatives were designed as inhibitors of HIV integrase (IN) based on known homology models. Through chemical synthesis and biochemical assays it was found that the activity profile of these compounds largely deviates from predictions with existing models. With the recently disclosed IN crystal structure of prototype foamy virus (PFV), a new HIV IN homology model was constructed featuring a critical IN/DNA interface previously lacking. With this new model, docking results completely corroborated observed biological activities. This new model should provide a more accurate and improved platform for the design of new inhibitors of HIV IN.

Who reads Scaffold rearrangement of dihydroxypyrimidine inhibitors of HIV integrase: Docking model revisited?

Author

Jing Tang; Kasthuraiah Maddali; Yves Pommier; Yuk Y. Sham; Zhengqiang Wang

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

2010

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)