HIV-1 integrase: from biology to chemotherapeutics
| العنوان: | HIV-1 integrase: from biology to chemotherapeutics |
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| المؤلفون: | Zeinalipour-Loizidou, E., Nicolaou, Charalambos P., Nicolaïdes, Andrew N., Kostrikis, Leontios G. |
| المساهمون: | Kostrikis, Leontios G. [0000-0002-5340-7109] |
| المصدر: | Current HIV Research Curr.HIV Res. |
| سنة النشر: | 2007 |
| مصطلحات موضوعية: | antivirus agent, l 870812, Human immunodeficiency virus 1, gs 9137, HIV Integrase, protein MAP30, indolicidin, life cycle, curcumin, gs 1937, virus replication, media_common, fz 41, antiretrovirus agent, computer aided design, quantitative structure activity relation, salicylhydrazide, clinical trial, highly active antiretroviral therapy, molecular mechanics, unclassified drug, enzyme activity, dicaffeoylquinic acid, enzyme structure, Structure and function, antiinfective agent, n (4 fluorobenzyl) 8 hydroxy 5 (tetrahydro 2h 1,2 thiazin 2 yl) 1,6 naphthyridine 7 carboxamide s,s dioxide, Infectious Diseases, DNA integration, Anti-Retroviral Agents, real time polymerase chain reaction, drug withdrawal, antiviral activity, Hiv 1 integrase, thalassiolin a, Computer-Aided Design, drug potency, virus DNA, l 870712, Drug, medicine.medical_specialty, drug design, media_common.quotation_subject, protein GAP31, review, l 900612, 1 [5 (4 fluorobenzyl) 2 furyl] 3 (1,2,4 triazol 3 yl) 1,3 propanedione, virus RNA, Computer-aided drug design, Acquired immunodeficiency syndrome (AIDS), HIV-1 integrase, Virology, unindexed drug, medicine, Humans, human, HIV Integrase Inhibitors, DNA binding, Intensive care medicine, thalassiolin C, thalassiolin B, suramin, v 165, nonhuman, cichoric acid, drug potentiation, indolicidin derivative, Inhibitors, Mechanism (biology), business.industry, integrase inhibitor, drug targeting, X ray crystallography, virus load, Human immunodeficiency virus 1 infection, protein K159, medicine.disease, zintevir, Informatics, Drug Design, Immunology, mercaptosalicylhydrazide, integrase, business, high throughput screening |
| الوصف: | AIDS has claimed the lives of 25 million people worldwide, an additional 40 million people are HIV-infected and new cases are being diagnosed every year. Despite the fact that HAART has moved AIDS from the category of terminal diseases to that of treatable chronic illnesses, its long-term therapeutic success may be compromised by the development of resistance to the currently used drugs. Despite the availability of RT, PR and fusion inhibitors, the development of further drugs such as inhibitors that target the third enzyme IN is essential for the clinical management of HIV-infected patients. The absence of cellular homolgues to IN and the unique nature of the reactions catalyzed by IN, make it an ideal target for drug design. Considerable progress towards designing HIV-1 IN inhibitors has been made over the last years and several lead compounds have been identified, synthesized and clinically studied. This review focuses on the existing knowledge of the biology of HIV-1 IN with emphasis on the mechanism of integration, structure and function and the technologies for measuring IN activity. This is followed by the current trends on designing HIV-1 IN inhibitors with the aid of molecular informatics and a review on the main classes of HIV-1 IN inhibitors reported this far with special emphasis on the clinical candidates. © 2007 Bentham Science Publishers Ltd. 5 4 365 388 Tradenames: ar 177 fz 41 gs 9137 l 870712 l 870810 l 900612, Merck s 1360 t 30177 v 165 Manufacturers: Merck Cited By :25 |
| تدمد: | 1873-4251 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::65378c1f3f2281741708f721842cf575Test https://pubmed.ncbi.nlm.nih.gov/17627500Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....65378c1f3f2281741708f721842cf575 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 18734251 |
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