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عنوان فارسی مقاله:
ارزیابی بالینی مرکاپتو بنزو آمید و پیش دارو برای مهار NCp7 ویروس نقص ایمنی انسانی
عنوان انگلیسی مقاله:
Preclinical evaluation of a mercaptobenzamide and its prodrug for NCp7-targeted inhibition of human immunodeficiency virus
سال انتشار : 2016
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مقدمه انگلیسی مقاله:
1. Introduction
Fixed-dose combination antiretroviral therapy has reduced AIDS-associated morbidity and mortality in patients infected with HIV-1 due to excellent efficacy and tolerability. Despite the development of highly effective antiretroviral agents (ARVs), therapy does not eradicate HIV infections and life-long treatment is necessary (Berg, 1986). In the course of long-term treatment, emergence of drug-resistant HIV which reduces the effectiveness of antiretroviral therapy can threaten virologic suppression of HIV. Developing novel therapeutics with a high genetic barrier to HIV resistance and low toxicity thus remains a necessity. The development of a specific virucidal compound with the ability to interfere with multiple stages of HIV replication has the potential to add significantly to the ability to treat HIV infection. The nucleocapsid protein 7 (NCp7) of HIV is an unexploited target to disrupt HIV with small molecules (Mori et al., 2015). Established HIV targets for therapeutic applications are enzymes (namely HIV protease, integrase, or reverse transcriptase) or viral entry/fusion inhibitors. HIV-1 NCp7 is a small, 55 amino acid protein that contains two highly conserved zinc fingers derived from a Cys-Xaa2-Cys-Xaa4-His-Xaa4-Cys (CCHC) motif. The main role of NCp7 is to bind to viral RNA and protect it from degradation (Covey, 1986; Guo et al., 2002; Ramboarina et al., 1999; Tanchou et al., 1998). The alteration of any one of the zinc-chelating amino acids or surrounding amino acids results in the production of noninfectious virus. NCp7 functions at multiple stages of HIV replication, including: reverse transcription, integration, Tat-promoted transcription, auto-catalysis of Gag-Pol precursors to form functional protease, promotion of Gag assembly and interaction with viral genomic RNA, and protection of double-stranded HIV genomic RNA from degradation (Buckman et al., 2003; Guo et al., 2000; Hargittai et al., 2004; Turpin et al., 1996; Zybarth and Carter, 1995; Berkowitz et al., 1993; Dawson and Yu, 1998; Shubsda et al., 2002; Lapadat-Tapolsky et al., 1993). The mechanistic activities of NCp7 suggest a potentially high genetic barrier to the selection of resistance and suggest that any resistant strains that may emerge might suffer significant loss of fitness. In vitro evaluations have confirmed that removal of zinc from the zinc fingers results in a loss of viral infectivity, impaired reverse transcription, and defective Gag-precursor maturation.
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کلمات کلیدی:
Preclinical evaluation of a mercaptobenzamide and its prodrug for ... www.ncbi.nlm.nih.gov/pubmed/27568924 Aug 26, 2016 - Preclinical evaluation of a mercaptobenzamide and its prodrug for NCp7-targeted inhibition of human immunodeficiency virus. Hartman TL(1) ... Mrinmoy Saha - Preclinical evaluation of a merc... | ACS Network https://communities.acs.org/docs/DOC-61034 Dec 8, 2016 - Mrinmoy Saha - Preclinical evaluation of a mercaptobenzamide and its prodrug for NCp7-targeted inhibition of human immunodeficiency virus. Studies on the Mechanism of Inactivation of the HIV-1 Nucleocapsid ... pubs.acs.org/doi/abs/10.1021/jm0492195 by LM Miller Jenkins - 2005 - Cited by 42 - Related articles Mar 25, 2005 - The HIV-1 nucleocapsid protein (NCp7) is a small basic protein with two ... which is important for future design of anti-HIV-1 compounds that target NCp7. .... Preclinical evaluation of a mercaptobenzamide and its prodrug for ... [PDF]Table 1 iranarze.ir/wp-content/uploads/2016/10/E1097.pdf Aug 26, 2016 - Preclinical evaluation of a mercaptobenzamide and its prodrug for. NCp7-targeted inhibition of human immunodeficiency virus. T.L. Hartman a ...
