Recent advances in the identification of Tat-mediated transactivation inhibitors: progressing toward a functional cure of HIV

Selective inhibition of HIV-1 replication by the CDK9 inhibitor FIT-039

(2015) Mika Okamoto et al.   ANTIVIRAL RESEARCH

Nucleobase modified neamines with a lysine as a linker, their inhibition specificity for TAR-Tat derived from HIV-1

(2015) Ryo Inoue et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Didehydro-Cortistatin A Inhibits HIV-1 Tat Mediated Neuroinflammation and Prevents Potentiation of Cocaine Reward in Tat Transgenic Mice

(2015) Sonia Mediouni et al.   CURRENT HIV RESEARCH

MicroRNA-155 Reinforces HIV Latency

(2015) Debbie S. Ruelas et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Reactivation of latent HIV-1 provirus via targeting protein phosphatase-1

(2015) Mudit Tyagi et al.   Retrovirology

The Tat Inhibitor Didehydro-Cortistatin A Prevents HIV-1 Reactivation from Latency

(2015) Guillaume Mousseau et al.   mBio

Cell-Penetrating, Dimeric α-Helical Peptides: Nanomolar Inhibitors of HIV-1 Transcription

(2014) Sangmok Jang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Phenyl-1-Pyridin-2yl-Ethanone-Based Iron Chelators Increase IκB-α Expression, Modulate CDK2 and CDK9 Activities, and Inhibit HIV-1 Transcription

(2014) Namita Kumari et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands

(2014) Luca Sancineto et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Fragment based search for small molecule inhibitors of HIV-1 Tat-TAR

(2014) Mirco Zeiger et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Small-Molecule Inhibitors of Protein-Protein Interactions: Progressing toward the Reality

(2014) Michelle R. Arkin et al.   CHEMISTRY & BIOLOGY

Tanshinone II A Inhibits Tat-Induced HIV-1 Transactivation Through Redox-Regulated AMPK/Nampt Pathway

(2014) Hong-Sheng Zhang et al.   JOURNAL OF CELLULAR PHYSIOLOGY

CDK9 inhibitor FIT-039 prevents replication of multiple DNA viruses

(2014) Makoto Yamamoto et al.   JOURNAL OF CLINICAL INVESTIGATION

Synthesis and Evaluation of Phosphorus Containing, Specific CDK9/CycT1 Inhibitors

(2014) Gábor Németh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Biologically Active, HIV TAR RNA-Binding Small Molecules Using Small Molecule Microarrays

(2014) Joanna Sztuba-Solinska et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Design, Synthesis and Biological Evaluation of Substituted Guanidine Indole Derivatives as Potential Inhibitors of HIV-1 Tat-TAR Interaction

(2014) Jun Wang et al.   Medicinal Chemistry

Cyclin-Dependent Kinase Inhibitors as Marketed Anticancer Drugs: Where Are We Now? A Short Survey

(2014) Gaëlle Mariaule et al.   MOLECULES

The microRNA miR-29a is associated with human immunodeficiency virus latency

(2014) Paresh Patel et al.   Retrovirology

Triptolide inhibits human immunodeficiency virus type 1 replication by promoting proteasomal degradation of Tat protein

(2014) Zhitao Wan et al.   Retrovirology

Transcriptional control of HIV latency: Cellular signaling pathways, epigenetics, happenstance and the hope for a cure

(2014) Uri Mbonye et al.   VIROLOGY

Sulfonation pathway inhibitors block reactivation of latent HIV-1

(2014) Jeffrey P. Murry et al.   VIROLOGY

Recognition of HIV-TAR RNA using neomycin–benzimidazole conjugates

(2013) Nihar Ranjan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor

(2013) T K Albert et al.   BRITISH JOURNAL OF PHARMACOLOGY

Viral–Host Interactions That Control HIV-1 Transcriptional Elongation

(2013) Huasong Lu et al.   CHEMICAL REVIEWS

Computer-Aided Design, Synthesis and Validation of 2-Phenylquinazolinone Fragments as CDK9 Inhibitors with Anti-HIV-1 Tat-Mediated Transcription Activity

(2013) Luca Sancineto et al.   ChemMedChem

From Small to Powerful: The Fragments Universe and its “Chem-Appeal”

(2013) Luca Sancineto et al.   CURRENT MEDICINAL CHEMISTRY

Blocking HIV-1 Replication by Targeting the Tat-Hijacked Transcriptional Machinery

(2013) Serena Massari et al.   CURRENT PHARMACEUTICAL DESIGN

Cyclin-dependent kinase inhibitors closer to market launch?

(2013) Hervé Galons et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Thermodynamic studies of a series of homologous HIV-1 TAR RNA ligands reveal that loose binders are stronger Tat competitors than tight ones

(2013) Lise Pascale et al.   NUCLEIC ACIDS RESEARCH

HIV-1 transcription and latency: an update

(2013) Carine Van Lint et al.   Retrovirology

RNA Polymerase II Elongation Control

(2012) Qiang Zhou et al.   Annual Review of Biochemistry

Identification of Novel Inhibitors of Human Immunodeficiency Virus Type 1 Replication byIn SilicoScreening Targeting Cyclin T1/Tat Interaction

(2012) Takayuki Hamasaki et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Click Dimers To Target HIV TAR RNA Conformation

(2012) Sunil Kumar et al.   BIOCHEMISTRY

An Analog of the Natural Steroidal Alkaloid Cortistatin A Potently Suppresses Tat-Dependent HIV Transcription

(2012) Guillaume Mousseau et al.   Cell Host & Microbe

Targeting Protein-Protein Interactions: A Promising Avenue of Anti-HIV Drug Discovery

(2012) Peng Zhan et al.   CURRENT MEDICINAL CHEMISTRY

Novel, Selective CDK9 Inhibitors for the Treatment of HIV Infection

(2012) G. Nemeth et al.   CURRENT MEDICINAL CHEMISTRY

Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres

(2012) Radek Jorda et al.   CURRENT PHARMACEUTICAL DESIGN

Perspective of Cyclin-dependent kinase 9 (CDK9) as a Drug Target

(2012) Vladimir Krystof et al.   CURRENT PHARMACEUTICAL DESIGN

Tanshinone derivatives: a patent review (January 2006 – September 2012)

(2012) Xiao-Hong Tian et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Seven sirtuins for seven deadly diseases ofaging

(2012) Brian J. Morris   FREE RADICAL BIOLOGY AND MEDICINE

Redefining the Viral Reservoirs that Prevent HIV-1 Eradication

(2012) Evelyn Eisele et al.   IMMUNITY

A Peptide Nucleic Acid–Aminosugar Conjugate Targeting Transactivation Response Element of HIV-1 RNA Genome Shows a High Bioavailability in Human Cells and Strongly Inhibits Tat-Mediated Transactivation of HIV-1 Transcription

(2012) Indrajit Das et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effect of Mimetic CDK9 Inhibitors on HIV-1-Activated Transcription

(2012) Rachel Van Duyne et al.   JOURNAL OF MOLECULAR BIOLOGY

Small Molecules Targeted to a Non-Catalytic “RVxF” Binding Site of Protein Phosphatase-1 Inhibit HIV-1

(2012) Tatiana Ammosova et al.   PLoS One

Identification of novel CDK9 and Cyclin T1-associated protein complexes (CCAPs) whose siRNA depletion enhances HIV-1 Tat function

(2012) Rajesh Ramakrishnan et al.   Retrovirology

Use of ATP analogs to inhibit HIV-1 transcription

(2012) Aarthi Narayanan et al.   VIROLOGY

The Control of HIV Transcription: Keeping RNA Polymerase II on Track

(2011) Melanie Ott et al.   Cell Host & Microbe

Structural Investigation of the Naphthyridone Scaffold: Identification of a 1,6-Naphthyridone Derivative with Potent and Selective Anti-HIV Activity

(2011) Oriana Tabarrini et al.   ChemMedChem

CD4+ T cells from elite controllers resist HIV-1 infection by selective upregulation of p21

(2011) Huabiao Chen et al.   JOURNAL OF CLINICAL INVESTIGATION

Celastrol Inhibits Tat-Mediated Human Immunodeficiency Virus (HIV) Transcription and Replication

(2011) Vivek Narayan et al.   JOURNAL OF MOLECULAR BIOLOGY

Scalable Synthesis of Cortistatin A and Related Structures

(2011) Jun Shi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Triptolide (TPL) Inhibits Global Transcription by Inducing Proteasome-Dependent Degradation of RNA Polymerase II (Pol II)

(2011) Ying Wang et al.   PLoS One

The Ins and Outs of HIV-1 Tat

(2011) Solène Debaisieux et al.   TRAFFIC

Polyamide Amino Acids trimers as TAR RNA ligands and anti-HIV agents

(2010) Vanessa Bonnard et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The Cellular Lysine Methyltransferase Set7/9-KMT7 Binds HIV-1 TAR RNA, Monomethylates the Viral Transactivator Tat, and Enhances HIV Transcription

(2010) Sara Pagans et al.   Cell Host & Microbe

RNA Grooves Can Accommodate Disulfide-Bridged Bundles of α-Helical Peptides

(2010) Soonsil Hyun et al.   CHEMBIOCHEM

Studies of Anti-HIV Transcription Inhibitor Quinolones: Identification of Potent N1-Vinyl Derivatives

(2010) Oriana Tabarrini et al.   ChemMedChem

Analysis of the roles of HIV-derived microRNAs

(2010) Aarthi Narayanan et al.   EXPERT OPINION ON BIOLOGICAL THERAPY

Cyclin-dependent kinase inhibitors: a survey of recent patent literature

(2010) Hervé Galons et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

6-desfluoroquinolones as HIV-1 Tat-mediated transcription inhibitors

(2010) Oriana Tabarrini et al.   Future Medicinal Chemistry

Expression of a Protein Phosphatase 1 Inhibitor, cdNIPP1, Increases CDK9 Threonine 186 Phosphorylation and Inhibits HIV-1 Transcription

(2010) Tatiana Ammosova et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Nicotinamide phosphoribosyltransferase/sirtuin 1 pathway is involved in human immunodeficiency virus type 1 Tat-mediated long terminal repeat transactivation

(2010) Hong-Sheng Zhang et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

HIV-1 Tat and Host AFF4 Recruit Two Transcription Elongation Factors into a Bifunctional Complex for Coordinated Activation of HIV-1 Transcription

(2010) Nanhai He et al.   MOLECULAR CELL

HIV-1 Tat Assembles a Multifunctional Transcription Elongation Complex and Stably Associates with the 7SK snRNP

(2010) Bijan Sobhian et al.   MOLECULAR CELL

Iron Chelators of the Di-2-pyridylketone Thiosemicarbazone and 2-Benzoylpyridine Thiosemicarbazone Series Inhibit HIV-1 Transcription: Identification of Novel Cellular Targets--Iron, Cyclin-Dependent Kinase (CDK) 2, and CDK9

(2010) Z. Debebe et al.   MOLECULAR PHARMACOLOGY

HIV Persistence and the Prospect of Long-Term Drug-Free Remissions for HIV-Infected Individuals

(2010) D. Trono et al.   SCIENCE

The molecular biology of HIV latency: breaking and restoring the Tat-dependent transcriptional circuit

(2010) Jonathan Karn   Current Opinion in HIV and AIDS

Multivalent binding oligomers inhibit HIV Tat–TAR interaction critical for viral replication

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

Identification of Flavopiridol Analogues that Selectively Inhibit Positive Transcription Elongation Factor (P-TEFb) and Block HIV-1 Replication

(2009) Akbar Ali et al.   CHEMBIOCHEM

Strategies for the design of RNA-binding small molecules

(2009) Fareed Aboul-ela   Future Medicinal Chemistry

HIV-1 regulation of latency in the monocyte-macrophage lineage and in CD4+ T lymphocytes

(2009) Laetitia Redel et al.   JOURNAL OF LEUKOCYTE BIOLOGY

A 1,8-Naphthyridone Derivative Targets the HIV-1 Tat-Mediated Transcription and Potently Inhibits the HIV-1 Replication

(2009) Serena Massari et al.   JOURNAL OF MEDICINAL CHEMISTRY

HIV-1 mRNA 3′ End Processing Is Distinctively Regulated by eIF3f, CDK11, and Splice Factor 9G8

(2009) Susana T. Valente et al.   MOLECULAR CELL

Inhibition of HIV-1 replication by eIF3f

(2009) S. T. Valente et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Simultaneous recognition of HIV-1 TAR RNA bulge and loop sequences by cyclic peptide mimics of Tat protein

(2009) A. Davidson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Studies on anti-HIV quinolones: New insights on the C-6 position

(2008) Serena Massari et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation

(2008) Sonja Baumli et al.   EMBO JOURNAL

Roscovitine-Derived, Dual-Specificity Inhibitors of Cyclin-Dependent Kinases and Casein Kinases 1

(2008) Nassima Oumata et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure−Activity Relationship Study on Anti-HIV 6-Desfluoroquinolones

(2008) Oriana Tabarrini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cyclin-dependent kinase 9: a key transcriptional regulator and potential drug target in oncology, virology and cardiology

(2008) S WANG et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Drug 9AA reactivates p21/Waf1 and inhibits HIV-1 progeny formation

(2008) Weilin Wu et al.   Virology Journal

The Host Cell Sulfonation Pathway Contributes to Retroviral Infection at a Step Coincident with Provirus Establishment

(2008) James W. Bruce et al.   PLoS Pathogens

Amphiphilic Helical Peptides Containing Two Acridine Moieties Display Picomolar Affinity toward HIV-1 RRE and TAR

(2007) Yeongran Lee et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION