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Crystal structure of human immunodeficiency virus (HIV) type 2 protease in complex with a reduced amide inhibitor and comparison with HIV-1 protease structures.

机译：人免疫缺陷病毒（HIV）2型蛋白酶的晶体结构与酰胺抑制剂含量降低的复合物，并与HIV-1蛋白酶结构进行比较。

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The crystal structure of HIV-2 protease in complex with a reduced amide inhibitor [BI-LA-398; Phe-Val-Phe-psi (CH2NH)-Leu-Glu-Ile-amide] has been determined at 2.2-A resolution and refined to a crystallographic R factor of 17.6%. The rms deviation from ideality in bond lengths is 0.018 A and in bond angles is 2.8 degrees. The largest structural differences between HIV-1 and HIV-2 proteases are located at residues 15-20, 34-40, and 65-73, away from the flap region and the substrate binding sites. The rms distance between equivalent C alpha atoms of HIV-1 and HIV-2 protease structures excluding these residues is 0.5 A. The shapes of the S1 and S2 pockets in the presence of this inhibitor are essentially unperturbed by the amino acid differences between HIV-1 and HIV-2 proteases. The interaction of the inhibitor with HIV-2 protease is similar to that observed in HIV-1 protease structures. The unprotected N terminus of the inhibitor interacts with the side chains of Asp-29 and Asp-30. The glutamate side chain of the inhibitor forms hydrogen bonds with the main-chain amido groups of residues 129 and 130.

机译：HIV-2蛋白酶的晶体结构与还原的酰胺抑制剂[BI-LA-398; [Phe-Val-Phe-psi（CH2NH）-Leu-Glu-Ile-amide]已在2.2-A分辨率下测定，并精炼至结晶R因子17.6％。粘结长度与理想值的均方根偏差为0.018 A，粘结角为2.8度。 HIV-1和HIV-2蛋白酶之间最大的结构差异位于残基15-20、34-40和65-73，远离襟翼区域和底物结合位点。 HIV-1和HIV-2蛋白酶结构（不包括这些残基）的等效Cα原子之间的均方根距离为0.5A。在存在这种抑制剂的情况下，S1和S2口袋的形状基本上不受HIV-之间氨基酸差异的干扰1和HIV-2蛋白酶。抑制剂与HIV-2蛋白酶的相互作用类似于在HIV-1蛋白酶结构中观察到的相互作用。抑制剂的未保护的N末端与Asp-29和Asp-30的侧链相互作用。抑制剂的谷氨酸侧链与残基129和130的主链酰胺基形成氢键。

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Tong L; Pav S; Pargellis C; Dô F; Lamarre D; Anderson P C;
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年度 1993
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1. Polymorphism of the Human Immunodeficiency Virus Type 1 (HIV-1) Protease Gene and Response of HIV-1-Infected Patients to a Protease Inhibitor [J] . Philippe Bossi, Mireille Mouroux, Anne Yvon, Journal of Clinical Microbiology . 1999,第9期

机译：人类免疫缺陷病毒1型（HIV-1）蛋白酶基因的多态性和HIV-1感染患者对蛋白酶抑制剂的反应。
2. Design and synthesis of HIV-1 protease inhibitors. Novel tetrahydrofuran P2/P2'-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex. [J] . Oscarsson K, Lahmann M, Lindberg J, Bioorganic and medicinal chemistry . 2003,第6期

机译：HIV-1蛋白酶抑制剂的设计和合成。新型四氢呋喃P2 / P2'-基团与HIV-1蛋白酶的Asp29 / 30相互作用。从抑制剂蛋白酶复合物的X射线晶体结构确定结合。
3. Comparison of Human Immunodeficiency Virus Type 1 (HIV-1) Protease Mutations in HIV-1 Genomes Detected in Plasma and in Peripheral Blood Mononuclear Cells from Patients Receiving Combination Drug Therapy [J] . Nathalie Koch, Nouara Yahi, Franck Ariasi, Journal of Clinical Microbiology . 1999,第5期

机译：从接受联合药物治疗的患者血浆和外周血单个核细胞中检测到的HIV-1基因组中的人类免疫缺陷病毒1型（HIV-1）蛋白酶突变的比较
4. Susceptibility to a non-conventional (folding) protease inhibitor of human immunodeficiency virus Type 1 isolates in vitro [C] . S. RUSCONI, M. Lo CICERO, S. FERRAMOSCA, International School of Physics "Enrico Fermi" . 2007

机译：对人免疫缺陷病毒的非常规（折叠）蛋白酶抑制剂的易感性在体外1型分离物
5. Isolation and characterization of RNA aptamers targeted to the aspartyl protease of the human immunodeficiency virus type 1 (HIV-1). [D] . Duclair, Sonald. 2010

机译：靶向人免疫缺陷病毒1型（HIV-1）天冬氨酰蛋白酶的RNA适体的分离和鉴定。
6. Crystal structure of human immunodeficiency virus (HIV) type 2 protease in complex with a reduced amide inhibitor and comparison with HIV-1 protease structures. [O] . L Tong, S Pav, C Pargellis, 1993

机译：人免疫缺陷病毒（HIV）2型蛋白酶的晶体结构与酰胺抑制剂含量降低的复合物并与HIV-1蛋白酶结构进行比较。
7. Studies of Human Immunodeficiency Virus Type 1 (HIV-1) Protease Inhibitors. III. Structure-Activity Relationship of HIV-1 Protease Inhibitors Containing Cyclohexylalanylalanine Hydroxyethylene Dipeptide lsostere. [O] . Mitsuya SAKURAI, Susumu HIGASHIDA, Machiko SUGANO, 1994

机译：人免疫缺陷病毒型1（HIV-1）蛋白酶抑制剂的研究。 III。 HIV-1蛋白酶抑制剂的结构 - 活性关系含有环己酰丙氨酸羟乙基二肽LSOSTERE的抑制剂。

Crystal structure of human immunodeficiency virus (HIV) type 2 protease in complex with a reduced amide inhibitor and comparison with HIV-1 protease structures.

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