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参考文献:The Discovery,Characterization And Crystallographically Determined Binding Mode Of An Fmoc-Containing Inhibitor Of Hiv-1 Protease
标题:The Discovery,Characterization And Crystallographically Determined Binding Mode Of An Fmoc-Containing Inhibitor Of Hiv-1 Protease
摘要:A Pharmacophore Derived From The Structure Of The Dithiolane Derivative Of Haloperidol Bound In The Active Site Of The Hiv-1 Protease (Hiv-1 Pr) Has Been Used To Search A Three-Dimensional Database For New Inhibitory Frameworks. This Search Identified An Fmoc-Protected N-Tosyl Arginine As A Lead Candidate. A Derivative In Which The Arginine Carboxyl Has Been Converted To An Amide Has Been Crystallized With Hiv-1 Pr And The Structure Has Been Determined To A Resolution Of 2.5 Angstrom With A Final R-Factor Of 18.5%. The Inhibitor Binds In An Extended Conformation That Results In occupancy Of The S2,S1',And S3' Subsites Of The Active Site. Initial Structure-Activity Studies Indicate That: (1) The Fmoc Fluorenyl Moiety Interacts Closely With Active Site Residues And Is Important For Binding; (2) The N-G-Tosyl Group Is Necessary To Suppress Protonation Of The Arginine Guanidinyl Terminus; And (3) The Arginine Carboxamide Function Is Involved In Interactions With The Water Coordinated To The Catalytic Aspartyl Groups. Fmoc-Protected Arginine Derivatives,Which Appear To Be Relatively Specific And Nontoxic,Offer Promise For The Development Of Useful Hiv-1 Protease Inhibitors. (C) 1997 Elsevier Science Ltd.
DOI:10.1016/s0968-0896(97)00078-3