title: Crystals of HIV-1 reverse transcriptase diffracting to 2.2 A resolution.
abstract: Reverse transcriptase (RT) from the human immunodeficiency virus type 1 has been crystallized in four closely related forms, the best of which diffract X-rays to 2.2 A resolution. The RT was crystallized as a complex with a non-nucleoside inhibitor, either nevirapine or a nevirapine analogue. Crystals grew from 6% PEG 3400 buffered at pH 5. These were of space group P2(1)2(1)2(1) with unit cell parameters a = 147 A, b = 112 A, c = 79 A (form A), with one RT heterodimer in the asymmetric unit. Changes in unit cell parameters and degree of crystalline order were observed on soaking pregrown crystals in various solutions, giving three further sets of unit cells. These were a = 143 A, b = 112, A, c = 79 A (form B), a = 141 A, b = 111 A, c = 73 A (form C), a = 143 A, b = 117 A, c = 66.5 A (form D). The last two forms diffract X-rays to 2.2 A resolution. Structure determinations of these latter crystal forms of RT should give a detailed atomic model for this therapeutically important drug target.
authors.affiliation: Wellcome Research Laboratories, Beckenham, Kent, U.K.
authors.forename: D K
authors.initials: DK
authors.lastname: Stammers
authors.forename: D O
authors.initials: DO
authors.lastname: Somers
authors.forename: C K
authors.initials: CK
authors.lastname: Ross
authors.forename: I
authors.initials: I
authors.lastname: Kirby
authors.forename: P H
authors.initials: PH
authors.lastname: Ray
authors.forename: J E
authors.initials: JE
authors.lastname: Wilson
authors.forename: M
authors.initials: M
authors.lastname: Norman
authors.forename: J S
authors.initials: JS
authors.lastname: Ren
authors.forename: R M
authors.initials: RM
authors.lastname: Esnouf
authors.forename: E F
authors.initials: EF
authors.lastname: Garman
mesh_terms: D018360:Crystallography, X-Ray; D054303:HIV Reverse Transcriptase; D015497:HIV-1 / Q000201:enzymology*; D019829:Nevirapine; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology; D012194:RNA-Directed DNA Polymerase / Q000737:chemistry*; D018894:Reverse Transcriptase Inhibitors
chemical_list: D011725:Pyridines; D018894:Reverse Transcriptase Inhibitors; D019829:Nevirapine; D054303:HIV Reverse Transcriptase; D012194:RNA-Directed DNA Polymerase