Integrase: An Important Therapeutic Target in the Fight Against HIV/AIDS Infection
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作者:
dos Santos, Monique Luiza A.
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Univ Fed Fluminense, Lab Quim Med Computac, Dept Farm, Fac Farm, Niteroi, RJ, BrazilUniv Fed Fluminense, Lab Quim Med Computac, Dept Farm, Fac Farm, Niteroi, RJ, Brazil
dos Santos, Monique Luiza A.
[1
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Albuquerque, Magaly G.
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Univ Fed Rio de Janeiro, Lab Modelagem Mol LabMMol, Dept Quim Organ, Inst Quim, Rio De Janeiro, RJ, BrazilUniv Fed Fluminense, Lab Quim Med Computac, Dept Farm, Fac Farm, Niteroi, RJ, Brazil
Albuquerque, Magaly G.
[2
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de Brito, Monique A.
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Univ Fed Fluminense, Lab Quim Med Computac, Dept Farm, Fac Farm, Niteroi, RJ, BrazilUniv Fed Fluminense, Lab Quim Med Computac, Dept Farm, Fac Farm, Niteroi, RJ, Brazil
de Brito, Monique A.
[1
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机构:
[1] Univ Fed Fluminense, Lab Quim Med Computac, Dept Farm, Fac Farm, Niteroi, RJ, Brazil
[2] Univ Fed Rio de Janeiro, Lab Modelagem Mol LabMMol, Dept Quim Organ, Inst Quim, Rio De Janeiro, RJ, Brazil
The acquired immunodeficiency syndrome (AIDS) is caused by the human immunodeficiency virus (HIV) that infects cells of the immune system, destroying them or causing damage to its operation. Among all the HIV enzymes, integrase is responsible for the insertion of viral DNA in the host DNA. The aim of this article is to describe the integrase inhibitors drugs and report cases of resistance, in addition to discussing new promising compounds that are being evaluated as integrase inhibitors. Currently, there are only three drugs in clinical use that belong to the class of integrase inhibitors: raltegravir (a pirimidinone carboxamide derivative, elvitegravir (a quinoline derivative) and dolutegravir (a diazatricyclo carboxamide derivative). However, several cases of resistance to drugs of this class are described in the literature, and the mutations of the enzyme responsible for such profile are known. Many compounds with integrase inhibitory action are under development. The use of the integrase enzyme as a target against HIV/AIDS infection is promising. In addition, the integration is a complex stage of the viral replication cycle, and new details of this process are being discovered every minute, which encourages the accomplishment of more studies for the development of new drugs of this class.
机构:
Univ Calif Los Angeles, David Geffen Sch Med, Calif NanoSyst Inst, Ctr Hlth Sci 52 175, Los Angeles, CA 90095 USAUniv Calif Los Angeles, David Geffen Sch Med, Calif NanoSyst Inst, Ctr Hlth Sci 52 175, Los Angeles, CA 90095 USA
Nel, Andre
Swindells, Susan
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Coll Med, Dept Internal Med, Omaha, NE USAUniv Calif Los Angeles, David Geffen Sch Med, Calif NanoSyst Inst, Ctr Hlth Sci 52 175, Los Angeles, CA 90095 USA
Swindells, Susan
Bronich, Tatiana
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Coll Pharm, Dept Pharmaceut Sci, Omaha, NE 68198 USAUniv Calif Los Angeles, David Geffen Sch Med, Calif NanoSyst Inst, Ctr Hlth Sci 52 175, Los Angeles, CA 90095 USA
Bronich, Tatiana
Gendelman, Howard E.
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Coll Med, Dept Pharmacol & Expt Neurosci, 985880 Nebraska Med Ctr, Omaha, NE 68198 USAUniv Calif Los Angeles, David Geffen Sch Med, Calif NanoSyst Inst, Ctr Hlth Sci 52 175, Los Angeles, CA 90095 USA