Abstract:
: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.
journal_name
Curr HIV Resjournal_title
Current HIV researchauthors
Zeinalipour-Loizidou E,Nicolaou C,Nicolaides A,Kostrikis LGdoi
10.2174/157016207781023965subject
Has Abstractpub_date
2007-07-01 00:00:00pages
365-88issue
4eissn
1570-162Xissn
1873-4251journal_volume
5pub_type
杂志文章,评审abstract::Natural or experimental infection of the African sooty mangabey (SM) with the simian immunodeficiency virus (SIV) results in chronic high levels of virus replication but is associated with none of the debilitating immunopathology, including the marked CD4 T-cell depletion, persistent cell activation and acquired immun...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016209787048465
更新日期:2009-01-01 00:00:00
abstract:BACKGROUND:The emergence of drug-resistant viral strains has created the need for the development of novel anti-HIV agents with a diverse structure that targets key enzymes in the HIV lifecycle. OBJECTIVE:Considering the pharmacophore of integrase inhibitors, one of the validated targets for anti-HIV therapy, we desig...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X17666191210105809
更新日期:2020-01-01 00:00:00
abstract::The human immunodeficiency virus-1 (HIV-1) Vpr protein plays multiple roles in HIV-1 replication. In early infection, Vpr provides help in the nuclear localization of pre-integration complex. Subsequently, Vpr induces cell cycle arrest of infected cells at G2/M phase. Cell cycle arrest facilitates higher rate of viral...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016209787581508
更新日期:2009-03-01 00:00:00
abstract::Drug use and HIV/AIDS are global public health issues. The World Health Organization (WHO) estimates that up to 30% of HIV infections are related to drug use and associated behaviors. The intersection, of the twin epidemics of HIV and drug/alcohol use, results in difficult medical management issues for the health care...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016209788680598
更新日期:2009-07-01 00:00:00
abstract::Human immunodeficiency virus type 1 (HIV) infects macrophages and microglia in the CNS and frequently causes neurocognitive impairment. Although antiviral therapy generally reduces the viral load in the CNS and improves HIV-associated neurological dysfunction, most current antiviral drugs have poor CNS penetrance and ...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016206777709500
更新日期:2006-07-01 00:00:00
abstract::HIV-associated neurocognitive disorders (HAND) remain prevalent despite effective combined anti-retroviral therapy (cART). Cognitive function has been shown to inversely correlate with decreased synaptic and dendritic density. In this study, macaques inoculated with SIV were examined over a 3-month course of infection...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162x1131100049
更新日期:2013-06-01 00:00:00
abstract::The present study assessed the phenotypic aspects of oral-cavity Candida albicans isolates from 300 HIV-1- positive patients, relating the most commonly investigated virulence factors (enzyme typing and germ-tube formation) to the most common morphotypes. The samples were seeded into specific media for isolation and s...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162x113119990042
更新日期:2013-06-01 00:00:00
abstract::Opioid use in HIV infection has been associated with an increased frequency of neurological disease and cognitive impairment and vitamin A deficiency has been linked to progressive HIV disease in drug users. In this report the potential effects of these factors, alone and in combination, on gamma amino butyric acid (G...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016212802138715
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abstract::Mutation of the human immunodeficiency virus by host cells inhibits viral dissemination by creating non-functional variants. However, viral mutation does not always eliminate the ability of the virus to disseminate and, in fact, is thought to promote persistence by generating functional mutants that evade immunity or ...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016208783571919
更新日期:2008-01-01 00:00:00
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journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X15666170517130339
更新日期:2017-01-01 00:00:00
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journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016208785132545
更新日期:2008-06-01 00:00:00
abstract::Hodgkin lymphoma (HL) represents one of the most common types of a non-AIDS-defining tumour that occurs in the HIV population, and its incidence is increasing in the post Highly Active Anti-retroviral Therapy (HAART) era. Despite the aggressiveness of that disease, the outcome of patients with HIV-HL has improved with...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016210790442704
更新日期:2010-03-01 00:00:00
abstract:BACKGROUND:Human milk banking has been promoted to provide donated breast milk for at-risk children whose mothers cannot breastfeed them but this effort was hindered by the advent of HIV epidemic. OBJECTIVE:To estimate the seroprevalence of HIV, syphilis and hepatitis B in the blood of human milk donors registered in ...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X15666170707143541
更新日期:2017-01-01 00:00:00
abstract:BACKGROUND:Previous studies have developed methodologies for predicting the number of CD4+ cells from the total leukocyte and lymphocytes count based on mathematical methodologies, obtaining percentages of effectiveness prediction higher than 90% with a value of less than 5000 leukocytes. OBJECTIVE:To improve the meth...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X17666190306125819
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:Due to the persistence of latent HIV-infected cellular reservoirs, HIV virus can not be eradicated completely. OBJECTIVE:To identify proteins related to HIV latency, we performed a subcellular proteomic study in HIV latent cell lines. METHODS:An established HIV-1 latent cell model (J-Lat Tat-GFP Clone A7 c...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X17666190506155222
更新日期:2019-01-01 00:00:00
abstract::In HIV-1 infected cells, over 40 different mRNA species are produced by alternative splicing of the single HIV-1 primary RNA transcript. In addition, approximately half of the HIV-1 primary RNA transcripts are not spliced and are exported to the cytoplasm where they serve as mRNA and as genomic RNA. In this article, w...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016206775197655
更新日期:2006-01-01 00:00:00
abstract:BACKGROUND:Vaccine against HIV-1 is not currently available. In present, Virus like particles (VLPs) as effective strategy was used in several vaccine developing. Two conserved sequences; V3 loop of gp120 and the membrane-proximal external region (MPER) of gp41 are dominant sites for vaccine studies. OBJECTIVE:In this...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X15666171017122229
更新日期:2017-01-01 00:00:00
abstract:UNLABELLED:Some deficient genetic polymorphisms of the innate immune system have been correlated to a higher susceptibility to different infections, especially in immunocompromised patients. The possible association between an increased incidence of pneumococcal bacteremia in HIV-infected patients, and deficient polymo...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016209787581382
更新日期:2009-03-01 00:00:00
abstract::Recently, a mechanism of negative regulation of immune responses by a specialized population of so-called regulatory T cells (Tregs) has become a focus of intense investigation. Through the discovery of transcription factor Foxp3 as a central molecular determinant of Tregs differentiation and function, the complex bio...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016210791208613
更新日期:2010-06-01 00:00:00
abstract::Several studies have suggested that aerobic physical activity is safe and beneficial for HIV-infected adults. However, there is information lacking regarding whether HIV-infected patients practice physical activity and to what extent. Therefore, the aim of this systematic review was to determine the prevalence of phys...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016212802429794
更新日期:2012-09-01 00:00:00
abstract::The human immunodeficiency virus (HIV) is unique in its capacity to produce chronic disease in almost all infected hosts. To accomplish this, it has evolved multiple mechanisms to effectively evade the immune response. HIV encodes at least one protein that makes infected cells resistant to CTL killing by downmodulatin...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/1570162033352138
更新日期:2003-01-01 00:00:00
abstract::Immunization is an important measure to protect HIV-infected children and adults against certain vaccine preventable diseases. However, the antibody response, which is associated with the level of CD4+ T cell count, is frequently impaired in this group of patients. Certain vaccines enhance virus replication and transi...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/1570162043351084
更新日期:2004-10-01 00:00:00
abstract::The HIV epidemic has resulted in medical, social and economic consequences. There is general agreement that a safe, effective and affordable preventive HIV vaccine is urgently needed to control the epidemic. To date, over 60 phase I/II trials of about 30 candidate vaccines have been conducted worldwide. In 1991, Thail...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/1570162052772933
更新日期:2005-01-01 00:00:00
abstract::The oral cavity of human immunodeficiency virus type I (HIV-1) infected individuals is subjected to a series of opportunistic infections which are usually considered as a prognostic marker for the severity of infection as well as an indicator of immunodeficiency. The highly active antiretroviral therapy (HAART) has si...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016207780636533
更新日期:2007-05-01 00:00:00
abstract:BACKGROUND:Although HIV and injury contribute substantially to disease burdens in lowand middle-income countries (LMIC), their intersection is poorly characterized. OBJECTIVE:This systematic review assessed the prevalence and associated mortality impact of HIVseropositivity among injured patients in LMIC. METHODS:A s...
journal_title:Current HIV research
pub_type: 杂志文章,meta分析,评审
doi:10.2174/1570162X15666170920112743
更新日期:2017-11-23 00:00:00
abstract::Human immunodeficiency virus has evolved several redundant mechanisms to remove its receptor, the CD4 molecule, from the cell surface. Indeed, HIV-1 encodes three proteins, Nef, Vpu and Env, that have a profound effect on CD4 trafficking and catabolism. Given this functional convergence, it is believed that cell surfa...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/1570162043485086
更新日期:2004-01-01 00:00:00
abstract::Modern combination antiretroviral therapy (cART) can bring HIV-1 in blood plasma to level undetectable by standard tests, prevent the onset of acquired immune deficiency syndrome (AIDS), and allow a near-normal life expectancy for HIV-infected individuals. Unfortunately, cART is not curative, as within a few weeks of ...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X18666191231105438
更新日期:2020-01-01 00:00:00
abstract::Interleukin 7 (IL7) is a critical factor for lymphocyte homeostasis. A dysfunction of the IL7/IL7R pathway has previously been described in HIV-1 infection, and promising results were observed in recent analyses of IL7 for therapeutic use in HIV infected individuals. However, further investigations are still warranted...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016212799937209
更新日期:2012-03-01 00:00:00
abstract:BACKGROUND:The change in the prevalence of hypogonadism with age in men with human immunodeficiency virus (HIV) infection is subject to debate. OBJECTIVE:To address this issue, we diagnosed hypogonadism based on serum levels of free testosterone (fTST) rather than total testosterone which is thought to be an inaccurat...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X18666200720000344
更新日期:2020-01-01 00:00:00
abstract::Passive immunization studies in non-human primates have established unequivocally that virus neutralization can prevent infection, providing the impetus for current intense efforts to identify immunogens that elicit broadly neutralizing antibodies in humans. Although Fc-mediated effector function may also contribute t...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/1570162x113116660060
更新日期:2013-07-01 00:00:00