TMC310911, a novel human immunodeficiency virus type 1 protease inhibitor, shows in vitro an improved resistance profile and higher genetic barrier to resistance compared with current protease inhibitors.

Dierynck I; Van Marck H; Van Ginderen M; Jonckers TH; Nalam MN; Schiffer CA; Raoof A; Kraus G; Picchio G

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TMC310911, a novel human immunodeficiency virus type 1 protease inhibitor, shows in vitro an improved resistance profile and higher genetic barrier to resistance compared with current protease inhibitors.

机译：与目前的蛋白酶抑制剂相比，TMC310911是一种新型的人类免疫缺陷病毒1型蛋白酶抑制剂，在体外显示出更高的耐药性和更高的耐药遗传障碍。

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TMC310911 is a novel human immunodeficiency virus type 1 (HIV-1) protease inhibitor (PI) structurally closely related to darunavir (DRV) but with improved virological characteristics. TMC310911 has potent activity against wild-type (WT) HIV-1 (median 50% effective concentration [EC(50)], 14 nM) and a wide spectrum of recombinant HIV-1 clinical isolates, including multiple-PI-resistant strains with decreased susceptibility to currently approved PIs (fold change [FC] in EC(50), >10). For a panel of 2,011 recombinant clinical isolates with decreased susceptibility to at least one of the currently approved PIs, the FC in TMC310911 EC(50) was

机译：TMC310911是一种新型人免疫缺陷病毒1型（HIV-1）蛋白酶抑制剂（PI），在结构上与达那韦（DRV）密切相关，但具有改善的病毒学特征。 TMC310911对野生型（WT）HIV-1（中值50％有效浓度[EC（50）]，14 nM）和多种重组HIV-1临床分离株，包括对多种PI耐药的菌株具有有效的活性。降低了对当前批准的PI的敏感性（EC（50）中的倍数变化[FC]，> 10）。对于一组2,011个对至少一种当前批准的PI敏感度降低的重组临床分离株，TMC310911 EC（50）中的FC对于82％的分离株为

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《Antimicrobial agents and chemotherapy.》 |2011年第12期|共9页
作者
Dierynck I; Van Marck H; Van Ginderen M; Jonckers TH; Nalam MN; Schiffer CA; Raoof A; Kraus G; Picchio G;
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1. TMC310911, a novel human immunodeficiency virus type 1 protease inhibitor, shows in vitro an improved resistance profile and higher genetic barrier to resistance compared with current protease inhibitors. [J] . Dierynck I, Van Marck H, Van Ginderen M, Antimicrobial agents and chemotherapy. . 2011,第12期

机译：与目前的蛋白酶抑制剂相比，TMC310911是一种新型的人类免疫缺陷病毒1型蛋白酶抑制剂，在体外显示出更高的耐药性和更高的耐药遗传障碍。
2. Novel human immunodeficiency virus type 1 protease mutations potentially involved in resistance to protease inhibitors. [J] . Svicher V, Ceccherini Silberstein F, Erba F, Antimicrobial agents and chemotherapy. . 2005,第5期

机译：新型的人类免疫缺陷病毒1型蛋白酶突变可能与蛋白酶抑制剂的抗性有关。
3. Association of a Novel Human Immunodeficiency Virus Type 1 Protease Substrate Cleft Mutation, L23I, with Protease Inhibitor Therapy and In Vitro Drug Resistance. [J] . Johnston E, Winters MA, Rhee SY, Antimicrobial agents and chemotherapy. . 2004,第12期

机译：新型人类免疫缺陷病毒1型蛋白酶底物裂口突变L23I与蛋白酶抑制剂治疗和体外耐药性的关联。
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. Drug resistance mechanisms and drug design strategies for human immunodeficiency virus and hepatitis C virus proteases [D] . Wang, Yong 2012

机译：人类免疫缺陷病毒和丙型肝炎病毒蛋白酶的耐药机制和药物设计策略
6. TMC310911 a Novel Human Immunodeficiency Virus Type 1 Protease Inhibitor Shows In Vitro an Improved Resistance Profile and Higher Genetic Barrier to Resistance Compared with Current Protease Inhibitors [O] . Inge Dierynck, Herwig Van Marck, Marcia Van Ginderen, 2011

机译：TMC310911一种新型的人类免疫缺陷病毒1型蛋白酶抑制剂与目前的蛋白酶抑制剂相比具有更好的体外抗药性和更高的抗药性遗传屏障
7. TMC310911, a Novel Human Immunodeficiency Virus Type 1 Protease Inhibitor, Shows In Vitro an Improved Resistance Profile and Higher Genetic Barrier to Resistance Compared with Current Protease Inhibitors ▿ † [O] . Dierynck, Inge, Van Marck, Herwig, Van Ginderen, Marcia, 2011

机译：TMC310911，一种新型的人类免疫缺陷病毒1型蛋白酶抑制剂，与目前的蛋白酶抑制剂相比，具有更高的抗药性和更高的遗传抵抗力 ▿ †

TMC310911, a novel human immunodeficiency virus type 1 protease inhibitor, shows in vitro an improved resistance profile and higher genetic barrier to resistance compared with current protease inhibitors.

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