HIV microbicides: state-of-the-art and new perspectives on the development of entry inhibitors

Inhibition of DC-SIGN-Mediated HIV Infection by a Linear Trimannoside Mimic in a Tetravalent Presentation

(2010) Sara Sattin et al.   ACS Chemical Biology

Pradimicin S, a Highly Soluble Nonpeptidic Small-Size Carbohydrate-Binding Antibiotic, Is an Anti-HIV Drug Lead for both Microbicidal and Systemic Use

(2010) J. Balzarini et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Discovery of Novel Small Molecule Orally Bioavailable C−X−C Chemokine Receptor 4 Antagonists That Are Potent Inhibitors of T-Tropic (X4) HIV-1 Replication

(2010) Renato T. Skerlj et al.   JOURNAL OF MEDICINAL CHEMISTRY

New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

(2010) Jonathan B. Baell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Safety, Tolerability, and Pharmacokinetics of SPL7013 Gel (VivaGel®): A Dose Ranging, Phase I Study

(2010) John OʼLoughlin et al.   SEXUALLY TRANSMITTED DISEASES

Enhancement of Human Immunodeficiency Virus Type 1 Replication Is Not Intrinsic to All Polyanion-Based Microbicides

(2009) S. Sonza et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Rapamycin enhances aplaviroc anti-HIV activity: Implications for the clinical development of novel CCR5 antagonists

(2009) Olga Latinovic et al.   ANTIVIRAL RESEARCH

Capture and transmission of HIV-1 by the C-type lectin L-SIGN (DC-SIGNR) is inhibited by carbohydrate-binding agents and polyanions

(2009) Joeri Auwerx et al.   ANTIVIRAL RESEARCH

Development of topical microbicides to prevent the sexual transmission of HIV

(2009) Robert W. Buckheit et al.   ANTIVIRAL RESEARCH

[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring

(2009) Maosheng Duan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Spiropiperidine CCR5 antagonists

(2009) David M. Rotstein et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

1-Amido-1-phenyl-3-piperidinylbutanes — CCR5 antagonists for the treatment of HIV. Part 1

(2009) Christopher G. Barber et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

1-Amido-1-phenyl-3-piperidinylbutanes – CCR5 antagonists for the treatment of HIV: Part 2

(2009) Christopher G. Barber et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

4,4-Disubstituted cyclohexylamine based CCR5 chemokine receptor antagonists as anti-HIV-1 agents

(2009) Maosheng Duan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines as CXCR4 antagonists with potent activity against HIV-1

(2009) Kristjan S. Gudmundsson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The design and discovery of novel amide CCR5 antagonists

(2009) David C. Pryde et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles

(2009) Rena Nishizawa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles

(2009) Rémy C. Lemoine et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Non-peptide entry inhibitors of HIV-1 that target the gp41 coiled coil pocket

(2009) Kent D. Stewart et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure-based design, synthesis and biological evaluation of new N-carboxyphenylpyrrole derivatives as HIV fusion inhibitors targeting gp41

(2009) Yong Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Multivalent Manno-Glyconanoparticles Inhibit DC-SIGN-Mediated HIV-1 Trans-Infection of Human T Cells

(2009) Olga Martínez-Ávila et al.   CHEMBIOCHEM

GoldManno-Glyconanoparticles: Multivalent Systems to Block HIV-1 gp120 Binding to the Lectin DC-SIGN

(2009) Olga Martínez-Ávila et al.   CHEMISTRY-A EUROPEAN JOURNAL

Microbicides for HIV prevention: reality or hope?

(2009) Ian McGowan   CURRENT OPINION IN INFECTIOUS DISEASES

Maraviroc: a new CCR5 antagonist

(2009) Shilpa Sayana et al.   Expert Review of Anti-Infective Therapy

Pathogen recognition by DC-SIGN shapes adaptive immunity

(2009) Teunis BH Geijtenbeek et al.   Future Microbiology

Dusting the sugar fingerprint: C-type lectin signaling in adaptive immunity

(2009) Jeroen den Dunnen et al.   IMMUNOLOGY LETTERS

In vitro synergistic activity against CCR5-tropic HIV-1 with combinations of potential candidate microbicide molecules HHA, KRV2110 and enfuvirtide (T20)

(2009) M.-A. Jenabian et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Anti-AIDS Agents. 78.†Design, Synthesis, Metabolic Stability Assessment, and Antiviral Evaluation of Novel Betulinic Acid Derivatives as Potent Anti-Human Immunodeficiency Virus (HIV) Agents

(2009) Keduo Qian et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Attachment. 5. An Evolution from Indole to Azaindoles Leading to the Discovery of 1-(4-Benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a Drug Candidate That Demonstrates Antiviral Activity in HIV-1-Infected Subjects∞

(2009) Tao Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Binding Optimization through Coordination Chemistry: CXCR4 Chemokine Receptor Antagonists from Ultrarigid Metal Complexes

(2009) Abid Khan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Combinations of the First and Next Generations of Human Immunodeficiency Virus (HIV) Fusion Inhibitors Exhibit a Highly Potent Synergistic Effect against Enfuvirtide- Sensitive and -Resistant HIV Type 1 Strains

(2009) C. Pan et al.   JOURNAL OF VIROLOGY

Antiviral drug discovery: Ten more compounds, and ten more stories (part B)

(2009) Erik De Clercq   MEDICINAL RESEARCH REVIEWS

Multivalent Benzoboroxole Functionalized Polymers as gp120 Glycan Targeted Microbicide Entry Inhibitors

(2009) Julie I. Jay et al.   MOLECULAR PHARMACEUTICS

A synthetic CD4–heparan sulfate glycoconjugate inhibits CCR5 and CXCR4 HIV-1 attachment and entry

(2009) Françoise Baleux et al.   Nature Chemical Biology

HIV-1 and influenza antibodies: seeing antigens in new ways

(2009) Peter D Kwong et al.   NATURE IMMUNOLOGY

Carbohydrate-specific signaling through the DC-SIGN signalosome tailors immunity to Mycobacterium tuberculosis, HIV-1 and Helicobacter pylori

(2009) Sonja I Gringhuis et al.   NATURE IMMUNOLOGY

From carbohydrate leads to glycomimetic drugs

(2009) Beat Ernst et al.   NATURE REVIEWS DRUG DISCOVERY

Vaccination with ALVAC and AIDSVAX to Prevent HIV-1 Infection in Thailand

(2009) Supachai Rerks-Ngarm et al.   NEW ENGLAND JOURNAL OF MEDICINE

Scaleable manufacture of HIV-1 entry inhibitor griffithsin and validation of its safety and efficacy as a topical microbicide component

(2009) B. R. O'Keefe et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Addition of a cholesterol group to an HIV-1 peptide fusion inhibitor dramatically increases its antiviral potency

(2009) P. Ingallinella et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

HIV fusion inhibitors

(2009) M. I. Qadir et al.   REVIEWS IN MEDICAL VIROLOGY

HIV-1 entry inhibitors: an overview

(2009) Daniel R Kuritzkes   Current Opinion in HIV and AIDS

Soluble CD4 and CD4-Mimetic Compounds Inhibit HIV-1 Infection by Induction of a Short-Lived Activated State

(2009) Hillel Haim et al.   PLoS Pathogens

C-type lectins on dendritic cells: key modulators for the induction of immune responses

(2008) Yvette van Kooyk   BIOCHEMICAL SOCIETY TRANSACTIONS

Innate signaling by the C-type lectin DC-SIGN dictates immune responses

(2008) Jeroen den Dunnen et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

Synthesis of Novel DC-SIGN Ligands with an α-Fucosylamide Anchor

(2008) Gabriele Timpano et al.   CHEMBIOCHEM

Safety concerns for the potential use of cyanovirin-N as a microbicidal anti-HIV agent

(2008) Dana Huskens et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

CD4-anchoring HIV-1 Fusion Inhibitor with Enhanced Potency andin VivoStability

(2008) Changhua Ji et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cyanovirin-N potently inhibits human immunodeficiency virus type 1 infection in cellular and cervical explant models

(2008) V. Buffa et al.   JOURNAL OF GENERAL VIROLOGY

Design, Synthesis, and Biological Evaluation ofN-Carboxyphenylpyrrole Derivatives as Potent HIV Fusion Inhibitors Targeting gp41

(2008) Kun Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Efficacy assessment of a cell-mediated immunity HIV-1 vaccine (the Step Study): a double-blind, randomised, placebo-controlled, test-of-concept trial

(2008) Susan P Buchbinder et al.   LANCET

Efficacy of Carraguard for prevention of HIV infection in women in South Africa: a randomised, double-blind, placebo-controlled trial

(2008) Stephanie Skoler-Karpoff et al.   LANCET

Vaginal microbicides and the prevention of HIV transmission

(2008) Blayne Cutler et al.   LANCET INFECTIOUS DISEASES

HIV entry inhibitors and their potential in HIV therapy

(2008) Keduo Qian et al.   MEDICINAL RESEARCH REVIEWS

Lack of Effectiveness of Cellulose Sulfate Gel for the Prevention of Vaginal HIV Transmission

(2008) Lut Van Damme et al.   NEW ENGLAND JOURNAL OF MEDICINE

Targeting the carbohydrates on HIV-1: Interaction of oligomannose dendrons with human monoclonal antibody 2G12 and DC-SIGN

(2008) S.-K. Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Whither or Wither Microbicides?

(2008) R. M. Grant et al.   SCIENCE

Antiretroviral Drug–Based Microbicides to Prevent HIV-1 Sexual Transmission

(2007) Per Johan Klasse et al.   Annual Review of Medicine

Distinct roles for DC-SIGN+-dendritic cells and Langerhans cells in HIV-1 transmission

(2007) Lot de Witte et al.   TRENDS IN MOLECULAR MEDICINE