Structure-enhanced methods in the development of non-nucleoside inhibitors targeting HIV reverse transcriptase variants.


:Resistance continues to emerge as a leading cause for antiretroviral treatment failure. Several mutations in HIV reverse transcriptase (RT) confer resistance to non-nucleoside inhibitors (NNRTIs), vital components of antiretroviral combination therapies. Since the majority of mutations are located in the NNRTI binding pocket, crystal structures of RT variants in complex with NNRTIs have provided ideas for new drug design strategies. This article reviews the impact of RT crystal structures on the multidisciplinary design and development of new inhibitors with improved resistance profiles.


Future Microbiol


Future microbiology


Frey KM




Has Abstract


2015-01-01 00:00:00












  • Group A Streptococcus encounters with host macrophages.

    abstract::Group A Streptococcus (GAS) is a leading human bacterial pathogen with diverse clinical manifestations. Macrophages constitute a critical first line of host defense against GAS infection, using numerous surface and intracellular receptors such as Toll-like receptors and inflammasomes for pathogen recognition and activ...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Valderrama JA,Nizet V

    更新日期:2018-01-01 00:00:00

  • Use of high-throughput mass spectrometry to elucidate host-pathogen interactions in Salmonella.

    abstract::Capabilities in mass spectrometry are evolving rapidly, with recent improvements in sensitivity, data analysis and, most important from the standpoint of this review, much higher throughput, allowing analysis of many samples in a single day. This short review describes how these improvements in mass spectrometry can b...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Rodland KD,Adkins JN,Ansong C,Chowdhury S,Manes NP,Shi L,Yoon H,Smith RD,Heffron F

    更新日期:2008-12-01 00:00:00

  • Type B coxsackieviruses and their interactions with the innate and adaptive immune systems.

    abstract::Coxsackieviruses are important human pathogens, and their interactions with the innate and adaptive immune systems are of particular interest. Many viruses evade some aspects of the innate response, but coxsackieviruses go a step further by actively inducing, and then exploiting, some features of the host cell respons...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Kemball CC,Alirezaei M,Whitton JL

    更新日期:2010-09-01 00:00:00

  • Human papillomavirus: gene expression, regulation and prospects for novel diagnostic methods and antiviral therapies.

    abstract::Human papillomaviruses (HPVs) cause diseases ranging from benign warts to invasive tumors. A subset of these viruses termed 'high risk' infect the cervix where persistent infection can lead to cervical cancer. Although many HPV genomes have been sequenced, knowledge of virus gene expression and its regulation is still...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Graham SV

    更新日期:2010-10-01 00:00:00

  • Cryptococcal infections in children: retrospective study and review from Australia.

    abstract::Aim: Cryptococcosis causes significant morbidity and mortality worldwide, but pediatric data are limited. Methods: A retrospective literature review of Australian pediatric cryptococcosis and additional 10-year audit of cases from a large pediatric network. Results: 22 cases of cryptococcosis in children were identifi...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Grimshaw A,Palasanthiran P,Huynh J,Marais B,Chen S,McMullan B

    更新日期:2019-12-01 00:00:00

  • Complementary roles of the Cek1 and Cek2 MAP kinases in Candida albicans cell-wall biogenesis.

    abstract:AIMS:To investigate whether Cek2 (as Cek1) is involved in the biogenesis of the fungal cell wall and to uncover differences and similitudes between both proteins. MATERIALS & METHODS:We used molecular genetics to characterize the role of Cek2 in MTL-heterozygous cells. RESULTS:Deletion of CEK2 (similar to CEK1) rende...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Correia I,Román E,Prieto D,Eisman B,Pla J

    更新日期:2016-01-01 00:00:00

  • Immunotherapeutic potential of neutralizing antibodies targeting conserved regions of the HCV envelope glycoprotein E2.

    abstract::HCV is a major cause of chronic liver disease worldwide. There is no vaccine available and the current antiviral therapies fail to cure approximately half of treated patients. Liver disease caused by HCV infection is the most common indication for orthotopic liver transplantation. Unfortunately, reinfection of the new...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Angus AG,Patel AH

    更新日期:2011-03-01 00:00:00

  • The dominance of bacterial genotypes leads to susceptibility variations under sublethal antibiotic pressure.

    abstract:AIM:To investigate the collective resistance of the bacteria population with resistant horizontal gene transfer under sublethal bactericide pressure. MATERIALS & METHODS:By employing qualitative analysis of ordinary differential equations, particularly bifurcation theory and several numerical simulations, a modified 4...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Xu S,Yang J,Yin C,Zhao X

    更新日期:2018-02-01 00:00:00

  • Evaluation of different microtiter plate-based methods for the quantitative assessment of Staphylococcus aureus biofilms.

    abstract:AIM:To quantitatively assess Staphylococcus aureus biofilms. MATERIALS & METHODS:In addition to the qualitative Congo red agar (CRA) method, we used the bioluminescence (BLM), safranine (SAF), crystal violet (CRV) and resazurin (RES) high-throughput microtiter plate-based quantitative assays. RESULTS:60.47% (26/43) o...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Elkhatib WF,Khairalla AS,Ashour HM

    更新日期:2014-01-01 00:00:00

  • Use of the plaque assay for testing the antibiotic susceptibility of intracellular bacteria.

    abstract::The plaque assay was first described for titration of bacterial inoculums and clonal isolation, and was later adapted for testing antibiotics susceptibility and to study virulence factors and motility of bacteria. Over time, the sensitivity and reproducibility of the technique has been improved. Usually, the number of...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Edouard S,Raoult D

    更新日期:2013-10-01 00:00:00

  • Post-translational modifications of host proteins by Legionella pneumophila: a sophisticated survival strategy.

    abstract::Eukaryotic proteins are tightly regulated by post-translational modifications, leading to a very subtle degree of regulation in time and space. Pathogen-mediated post-translational modifications are key strategies to modulate host factors by targeting central signaling pathways in the host cell. Legionella pneumophila...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Rolando M,Buchrieser C

    更新日期:2012-03-01 00:00:00

  • COVID-19: mask efficacy is dependent on both fabric and fit.

    abstract::Aim: Face masks are an important addition to our arsenal in the fight against COVID-19. The aim of this study is to present a novel method of measuring mask performance which can simultaneously assess both fabric penetration and leakage due to poor fit. Materials & methods: A synthetic aerosol is introduced into the l...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Darby S,Chulliyallipalil K,Przyjalgowski M,McGowan P,Jeffers S,Giltinan A,Lewis L,Smith N,Sleator RD

    更新日期:2021-01-01 00:00:00

  • Proteomic studies of Bacillus anthracis.

    abstract::Bacillus anthracis is a Gram-positive, spore-forming bacterium representing the etiological cause of anthrax, a rare lethal disease of animals and humans. Development of anthrax countermeasures has gained increasing attention owing to the potential use of B. anthracis spores as a bioterror weapon. The various forms of...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Chitlaru T,Shafferman A

    更新日期:2009-10-01 00:00:00

  • Nanoscale exploration of microbial surfaces using the atomic force microscope.

    abstract::Atomic force microscopy (AFM) has recently opened a variety of novel possibilities for imaging and manipulating microbial surfaces in their native environment. While AFM imaging offers a means to visualize surface structures at high resolution and in physiological conditions, AFM force spectroscopy enables researchers...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Dufrêne YF

    更新日期:2006-12-01 00:00:00

  • Prospects for defined epitope vaccines for respiratory syncytial virus.

    abstract::The history of vaccines for respiratory syncytial virus (RSV) illustrates the complex immunity and immunopathology to this ubiquitous virus, starting from the failed formalin-inactivated vaccine trials performed in the 1960s. An attractive alternative to traditional live or killed virus vaccines is a defined vaccine c...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Anderson R,Huang Y,Langley JM

    更新日期:2010-04-01 00:00:00

  • Efflux pump induction by quaternary ammonium compounds and fluoroquinolone resistance in bacteria.

    abstract::Biocides, primarily those containing quaternary ammonium compounds (QAC), are heavily used in hospital environments and various industries (e.g., food, water, cosmetic). To date, little attention has been paid to potential implications of QAC use in the emergence of antibiotic resistance, especially fluoroquinolone-re...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Buffet-Bataillon S,Tattevin P,Maillard JY,Bonnaure-Mallet M,Jolivet-Gougeon A

    更新日期:2016-01-01 00:00:00

  • Direct and indirect effects of the 13-valent pneumococcal conjugate vaccine administered to infants and young children.

    abstract::This paper analyzes the most recent reports regarding the direct and indirect effects of the 13-valent pneumococcal conjugate vaccine (PCV13) when administered to infants and young children. PCV13 extends the protective effects reported for the 7-valent pneumococcal conjugate vaccine (PCV7). A further reduction in the...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Esposito S,Principi N,ESCMID Vaccine Study Group.

    更新日期:2015-01-01 00:00:00

  • How Cryptococcus interacts with the blood-brain barrier.

    abstract::Cryptococcus demonstrates predilection for invasion of the brain, but the mechanism by which Cryptococcus crosses the blood-brain barrier (BBB) to cause brain invasion is largely unknown. In order for Cryptococcus to cross the BBB, there must be a way to either cross human brain microvascular endothelial cells, which ...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Tseng HK,Huang TY,Wu AY,Chen HH,Liu CP,Jong A

    更新日期:2015-01-01 00:00:00

  • Inhibition of growth and gene expression in Staphylococcus aureus by anti-gyrA peptide nucleic acid.

    abstract::Aim: Multidrug-resistant Staphylococcus aureus isolates have become a serious concern in clinical microbiology. Antisense strategy, which specifically targets essential genes, could be helpful. Materials & methods:S. aureus cultures were treated with peptide conjugate-peptide nucleic acid (PPNA) specific for the gyrA ...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Tavakoli M,Hashemi A,Vaezjalali M,Mohammadzadeh M,Goudarzi H

    更新日期:2019-09-01 00:00:00

  • The ferric uptake regulator of Helicobacter pylori: a critical player in the battle for iron and colonization of the stomach.

    abstract::Helicobacter pylori is arguably one of the most successful pathogens; it colonizes the stomachs of more than half of the human population. Colonization and persistence in such an inhospitable niche requires the presence of exquisite adaptive mechanisms. One of the proteins that contributes significantly to the remarka...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Pich OQ,Merrell DS

    更新日期:2013-06-01 00:00:00

  • The differential effect of clarithromycin and azithromycin on induction of macrolide resistance in Mycobacterium abscessus.

    abstract::Aim: Antibiotic resistance in Mycobacterium abscessus renders treatment poorly effective. Despite erm(41)-gene-mediated macrolide resistance, treatment with azithromycin or clarithromycin is recommended. It is contested whether macrolides differ in erm(41) induction. We determine whether this is the case. Methods:M. a...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Schildkraut JA,Pennings LJ,Ruth MM,de Brouwer AP,Wertheim HF,Hoefsloot W,de Jong A,van Ingen J

    更新日期:2019-06-01 00:00:00

  • Amino acid capture and utilization within the Mycobacterium tuberculosis phagosome.

    abstract::Mycobacterium tuberculosis, the agent of TB, is a facultative intracellular bacterial pathogen that replicates inside host macrophages and other phagocytes within a membrane-bound vacuole or phagosome. How M. tuberculosis captures and exploits vital nutrients inside host cells is an intensive research area that might ...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Gouzy A,Poquet Y,Neyrolles O

    更新日期:2014-01-01 00:00:00

  • Clinical metagenomics for the management of hospital- and healthcare-acquired pneumonia.

    abstract::The increasing burden of multidrug-resistant bacteria affects the management of several infections. In order to prescribe adequate antibiotics, clinicians facing severe infections such as hospital-acquired pneumonia (HAP) need to promptly identify the pathogens and know their antibiotic susceptibility profiles (AST), ...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Ruppé E,Baud D,Schicklin S,Guigon G,Schrenzel J

    更新日期:2016-01-01 00:00:00

  • Salmonella enterica as a vaccine carrier.

    abstract::Salmonella enterica is an invasive, facultative intracellular gastrointestinal pathogen causing human diseases such as gastroenteritis and typhoid fever. Virulence-attenuated strains of this pathogen have interesting capacities for the generation of live vaccines. Attenuated live typhoidal and nontyphoidal Salmonella ...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Hegazy WA,Hensel M

    更新日期:2012-01-01 00:00:00

  • Alterations of zinc homeostasis in response to Cryptococcus neoformans in a murine macrophage cell line.

    abstract:AIM:To evaluate alterations of zinc homeostasis in macrophages exposed to Cryptococcus neoformans. Materials & methods: Using a fluorescent zinc probe-based flow cytometry and atomic absorption spectrometry, zinc levels were evaluated in J774.A1 cell lines exposed to C. neoformans H99 cells. The transcription profile o...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Dos Santos FM,Piffer AC,Schneider RO,Ribeiro NS,Garcia AWA,Schrank A,Kmetzsch L,Vainstein MH,Staats CC

    更新日期:2017-05-01 00:00:00

  • Safety, tolerability and pharmacokinetics of AFN-1252 administered as immediate release tablets in healthy subjects.

    abstract:AIMS:AFN-1252 is a novel inhibitor of FabI, an essential enzyme in Staphylococcus spp. This study was undertaken to assess the safety, tolerability and pharmacokinetic properties of AFN-1252, following oral administration in an ascending dose trial. MATERIALS & METHODS:This was a double-blind, randomized, placebo-cont...

    journal_title:Future microbiology

    pub_type: 杂志文章,随机对照试验


    authors: Hafkin B,Kaplan N,Hunt TL

    更新日期:2015-01-01 00:00:00

  • Dosing antibiotics in neonates: review of the pharmacokinetic data.

    abstract::Antibiotics are often used in neonates despite the absence of relevant dosing information in drug labels. For neonatal dosing, clinicians must extrapolate data from studies for adults and older children, who have strikingly different physiologies. As a result, dosing extrapolation can lead to increased toxicity or eff...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Rivera-Chaparro ND,Cohen-Wolkowiez M,Greenberg RG

    更新日期:2017-09-01 00:00:00

  • Epidemic of surgical-site infections by a single clone of rapidly growing mycobacteria in Brazil.

    abstract:AIM:Our aim is to investigate if the clusters of postsurgical mycobacterial infections, reported between 2004 and 2008 in seven geographically distant states in Brazil, were caused by a single mycobacterial strain. MATERIALS & METHODS:Available information from 929 surgical patients was obtained from local health auth...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Leão SC,Viana-Niero C,Matsumoto CK,Lima KV,Lopes ML,Palaci M,Hadad DJ,Vinhas S,Duarte RS,Lourenço MC,Kipnis A,das Neves ZC,Gabardo BM,Ribeiro MO,Baethgen L,de Assis DB,Madalosso G,Chimara E,Dalcolmo MP

    更新日期:2010-06-01 00:00:00

  • SAMHD1: a novel antiviral factor in intrinsic immunity.

    abstract::Some intracellular/membranous factors exert intrinsic immunity against viral pathogens. Most recently, SAMHD1 has been shown to be one of these factors. SAMHD1 is a nucleus-localized protein, and mutations in the gene are associated with Aicardi-Goutières syndrome. As a triphosphohydrolase, it depletes the intracellul...

    journal_title:Future microbiology

    pub_type: 杂志文章,评审


    authors: Chen Z,Zhang L,Ying S

    更新日期:2012-09-01 00:00:00

  • Investigation of an XDR-Acinetobacter baumannii ST2 outbreak in an intensive care unit of a Lebanese tertiary care hospital.

    abstract::Aim: We sought to investigate the genetic epidemiological relatedness of carbapenem-resistant Acinetobacter baumannii (CRAB) strains of a suspected outbreak in a Lebanese tertiary care hospital to implement necessary infection prevention and control measures. Methods: Twenty-eight nonduplicate CRAB isolates detected a...

    journal_title:Future microbiology

    pub_type: 杂志文章


    authors: Osman M,B Halimeh F,Rafei R,Mallat H,Tom JE,Raad EB,M Diene S,Jamal S,Atrouni AA,Dabboussi F,Moudani W,Madec JY,Saras E,Lupo A,Haenni M,Rolain JM,Hamze M

    更新日期:2020-10-01 00:00:00