Výsledky vyhledávání - "Pratiq A. Patel"

Synthesis and antiproliferative activity of derivatives of the phyllanthusmin class of arylnaphthalene lignan lactones

Autor: Andrew C. Huntsman, Soumendrakrishna Karmahapatra, Alexandria N. Young, Joanna E. Burdette, Malcolm S. Cole, Hee Byung Chai, Denisse Herrera, Jack C. Yalowich, Yulin Ren, John L. Woodard, A. Douglas Kinghorn, James R. Fuchs, Ragu Kanagasabai, Pratiq A. Patel

Publikováno v: Bioorganicmedicinal chemistry. 26(9)

A series of arylnaphthalene lignan lactones based on the structure of the phyllanthusmins, a class of potent natural products possessing diphyllin as the aglycone, has been synthesized and screened for activity against multiple cancer cell lines. SAR

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b9f76c953e57e920688fc03b3a998a9
https://pubmed.ncbi.nlm.nih.gov/29656990

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The A128T Resistance Mutation Reveals Aberrant Protein Multimerization as the Primary Mechanism of Action of Allosteric HIV-1 Integrase Inhibitors

Autor: Yasuhiro Koh, Mamuka Kvaratskhelia, Alison Slaughter, Lei Feng, Alan Engelman, Nikolozi Shkriabai, Jacques J. Kessl, Hiroaki Mitsuya, Nivedita Jena, Ross C. Larue, Pratiq A. Patel, Amit Sharma, James R. Fuchs

Publikováno v: Journal of Biological Chemistry. 288:15813-15820

Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are a very promising new class of anti-HIV-1 agents that exhibit a multimodal mechanism of action by allosterically modulating IN multimerization and interfering with IN-lens epithelium-derived gro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::054379f725cd8dce41d456506c662a57
https://doi.org/10.1074/jbc.m112.443390

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Allosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation

Autor: Hao Wang, Lei Feng, Yasuhiro Koh, Alan Engelman, Weifeng Wang, Alison Slaughter, Pratiq A. Patel, Kellie A. Jurado, Jacques J. Kessl, Allison Ballandras-Colas, James R. Fuchs, Mamuka Kvaratskhelia

Publikováno v: Proceedings of the National Academy of Sciences. 110:8690-8695

Integration is essential for HIV-1 replication, and the viral integrase (IN) protein is an important therapeutic target. Allosteric IN inhibitors (ALLINIs) that engage the IN dimer interface at the binding site for the host protein lens epithelium-de

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f36e37db9d90e3a6cff1c99bc4a29f2b
https://doi.org/10.1073/pnas.1300703110

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Indole-based Allosteric Inhibitors of HIV-1 Integrase

Autor: Pratibha C. Koneru, Nivedita Jena, Pratiq A. Patel, Janet Antwi, Mosaad S. Mohamed, Matthew J. Kobe, Guqin Shi, Jacques J. Kessl, Lei Feng, Chenglong Li, James R. Fuchs, Nina Kvaratskhelia, Yara E. Mansour

Employing a scaffold hopping approach, a series of allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) have been synthesized based on an indole scaffold. These compounds incorporate the key elements utilized in quinoline-based ALLINIs for binding to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::295e070ab652040d73122f41f53fbf44
https://europepmc.org/articles/PMC5018460/

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HRP2 determines the efficiency and specificity of HIV-1 integration in LEDGF/p75 knockout cells but does not contribute to the antiviral activity of a potent LEDGF/p75-binding site integrase inhibitor

Autor: James R. Fuchs, Steven Smith, Hao Wang, Andrea L. Ferris, Mamuka Kvaratskhelia, Peter Cherepanov, Alan Engelman, Xiang Li, Pratiq A. Patel, Kellie A. Jurado, Xiaolin Wu, Ming-Chieh Shun, Stephen H. Hughes

Publikováno v: Nucleic Acids Research

The binding of integrase (IN) to lens epithelium-derived growth factor (LEDGF)/p75 in large part determines the efficiency and specificity of HIV-1 integration. However, a significant residual preference for integration into active genes persists in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e28a4e88303c5b4f370a83fe74e211d
https://doi.org/10.1093/nar/gks913

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The mechanism of H171T resistance reveals the importance of Nδ-protonated His171 for the binding of allosteric inhibitor BI-D to HIV-1 integrase

Autor: Ross C. Larue, Nikoloz Shkriabai, James R. Fuchs, Nivedita Jena, Jacques J. Kessl, Mamuka Kvaratskhelia, Alan Engelman, Lei Feng, Kellie A. Jurado, Pratiq A. Patel, Hind J. Fadel, Ronald M. Levy, Eric M. Poeschla, Alison Slaughter, Nanjie Deng

Publikováno v: Retrovirology

Background Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are an important new class of anti-HIV-1 agents. ALLINIs bind at the IN catalytic core domain (CCD) dimer interface occupying the principal binding pocket of its cellular cofactor LEDGF/

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::832e3c61e010dbc7db45475994fd2e14
http://europepmc.org/articles/PMC4251946

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Direct Diazo-Transfer Reaction on β-lactam: Synthesis and Preliminary Biological Activities of 6-Triazolylpenicillanic Acids

Autor: Po C. Chen, Adegboyega K. Oyelere, Rebekah E. Wharton, Pratiq A. Patel

In this study we report the first example of a direct diazo-transfer reaction on readily available 6-aminopenicillanates to give 6-azidopenicillanates in high yield. Subsequent Cu(I)-catalyzed Huisgen cycloaddition between these 6-azidopenicillanates

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::21725e54f319663ecf85ebe3da8d18d6
https://europepmc.org/articles/PMC2755539/

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