Výsledky vyhledávání - "Linah N. Rusere"

Drug Design Strategies to Avoid Resistance in Direct-Acting Antivirals and Beyond

Autor: Florian Leidner, Ashley N. Matthew, Linah N. Rusere, Gordon J. Lockbaum, Mina Henes, Debra A. Ragland, Desaboini Nageswara Rao, Jacqueto Zephyr, Djade I. Soumana, Celia A. Schiffer, Janet L. Paulsen, Nese Kurt Yilmaz, Kristina L. Prachanronarong, Ellen A. Nalivaika, Shurong Hou, Jennifer Timm, Akbar Ali

Publikováno v: Chem Rev

Drug resistance is prevalent across many diseases, rendering therapies ineffective with severe financial and health consequences. Rather than accepting resistance after the fact, proactive strategies need to be incorporated into the drug design and d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13a52faa3b6205d783bd755f6513d82d
https://doi.org/10.1021/acs.chemrev.0c00648

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HIV-1 Protease Inhibitors Incorporating Stereochemically Defined P2′ Ligands To Optimize Hydrogen Bonding in the Substrate Envelope

Autor: Gordon J. Lockbaum, Celia A. Schiffer, Ellen A. Nalivaika, Nese Kurt Yilmaz, Linah N. Rusere, Mina Henes, Sook-Kyung Lee, Klajdi Kosovrasti, Ronald Swanstrom, Akbar Ali, Ean Spielvogel

Publikováno v: J Med Chem

A structure-guided design strategy was used to improve the resistance profile of HIV-1 protease inhibitors by optimizing hydrogen bonding and van der Waals interactions with the protease while staying within the substrate envelope. Stereoisomers of 4

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28fd17d85004f72f6d3054a61ca9e475
https://doi.org/10.1021/acs.jmedchem.9b00838

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Inhibiting HTLV-1 Protease: A Viable Antiviral Target

Autor: Mina Henes, Celia A. Schiffer, Nese Kurt Yilmaz, Mohan Somasundaran, Gordon J. Lockbaum, Linah N. Rusere, Akbar Ali, Ellen A. Nalivaika, Klajdi Kosovrasti, Louis M. Mansky, Nathaniel Talledge

Publikováno v: ACS Chem Biol

Human T-cell lymphotropic virus type 1 (HTLV-1) is a retrovirus that can cause severe paralytic neurologic disease and immune disorders as well as cancer. An estimated 20 million people worldwide are infected with HTLV-1, with prevalence reaching 30%

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1ef76a256b99966f051bbbb9aa17023
https://pubmed.ncbi.nlm.nih.gov/33619959

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Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere

Autor: Sook-Kyung Lee, Mina Henes, Ronald Swanstrom, Celia A. Schiffer, Linah N. Rusere, Klajdi Kosovrasti, Ean Spielvogel, Akbar Ali, Gordon J. Lockbaum, Desaboini Nageswara Rao, Nese Kurt Yilmaz, Ellen A. Nalivaika

Publikováno v: J Med Chem

The design, synthesis, and X-ray structural analysis of hybrid HIV-1 protease inhibitors (PIs) containing bis-tetrahydrofuran (bis-THF) in a pseudo-C2-symmetric dipeptide isostere are described. A series of PIs were synthesized by incorporating bis-T

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::75d68a1620aaedab54d48716ccf0a5ee
https://pubmed.ncbi.nlm.nih.gov/32672965

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Structural Adaptation of Darunavir Analogs Against Primary Resistance Mutations in HIV-1 Protease

Autor: Florian Leidner, Klajdi Kosovrasti, Akbar Ali, Nese Kurt Yilmaz, Linah N. Rusere, Gordon J. Lockbaum, Mina Henes, Celia A. Schiffer, Ellen A. Nalivaika

HIV-1 protease is one of the prime targets of agents used in antiretroviral therapy against HIV. However, under selective pressure of protease inhibitors, primary mutations at the active site weaken inhibitor binding to confer resistance. Darunavir (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc0f67249fe909e586a6af1e3eeb9110

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Quinoxaline-Based Linear HCV NS3/4A Protease Inhibitors Exhibit Potent Activity against Drug Resistant Variants

Autor: Akbar Ali, Ashley N. Matthew, Muhammad Jahangir, Linah N. Rusere, Gordon J. Lockbaum, Alicia Newton, Wei Huang, Nese Kurt Yilmaz, Celia A. Schiffer, Christos J. Petropoulos

[Image: see text] A series of linear HCV NS3/4A protease inhibitors was designed by eliminating the P2–P4 macrocyclic linker in grazoprevir, which, in addition to conferring conformational flexibility, allowed structure–activity relationship (SAR

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a72cbd231f641c417a7be77891c2c8a5
https://europepmc.org/articles/PMC6047049/

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Dengue Virus NS2B/NS3 Protease Inhibitors Exploiting the Prime Side

Autor: Celia A. Schiffer, Nese Kurt Yilmaz, Linah N. Rusere, Akbar Ali, Djade I. Soumana, Kuan-Hung Lin

The mosquito-transmitted dengue virus (DENV) infects millions of people in tropical and subtropical regions. Maturation of DENV particles requires proper cleavage of the viral polyprotein, including processing of 8 of the 13 substrate cleavage sites

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a4b455db58610e2c0399d27f7171b29
https://europepmc.org/articles/PMC5411607/

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Design and synthesis of potent macrocyclic HIV-1 protease inhibitors involving P1–P2 ligands

Autor: Masayuki Amano, Heather L. Osswald, Hiroaki Mitsuya, Gary E. Schiltz, Arun K. Ghosh, D. Eric Walters, Linah N. Rusere

Publikováno v: Org. Biomol. Chem.. 12:6842-6854

A series of potent macrocyclic HIV-1 protease inhibitors have been designed and synthesized. The compounds incorporated 16- to 19-membered macrocyclic rings between a nelfinavir-like P2 ligand and a tyrosine side chain containing a hydroxyethylamine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28ecc01d0d6f55011b81da5278c66f91
https://doi.org/10.1039/c4ob00738g

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