Kathleen M. Frey
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View article: Skin Lipid–Microbe Interplay Links <i>Staphylococcus hominis</i> to Barrier Control in Adult Atopic Dermatitis
Skin Lipid–Microbe Interplay Links <i>Staphylococcus hominis</i> to Barrier Control in Adult Atopic Dermatitis Open
Background Skin surface lipids and commensal microbes are essential for the epidermal barrier, but their mutual interactions remain poorly understood. Methods We conducted high‐resolution shotgun lipidomics of tape strips from lesional and…
View article: Exploring novel <scp>HIV</scp>‐1 reverse transcriptase inhibitors with drug‐resistant mutants: A double mutant surprise
Exploring novel <span>HIV</span>‐1 reverse transcriptase inhibitors with drug‐resistant mutants: A double mutant surprise Open
HIV‐1 reverse transcriptase (RT) remains a key target for HIV drug development. As successful management of the disease requires lifelong treatment, the emergence of resistance mutations is inevitable, making development of new RT inhibito…
View article: Crystal structure of dihydrofolate reductase from the filarial nematode W. bancrofti in complex with NADPH and folate
Crystal structure of dihydrofolate reductase from the filarial nematode W. bancrofti in complex with NADPH and folate Open
Lymphatic filariasis is a debilitating illness with an estimated 50 million cases as of 2018. The majority of cases are caused by the parasitic worm W . bancrofti and additional cases by the worms B . malayi and B . timori . Dihydrofolate …
View article: Structural Studies and Structure Activity Relationships for Novel Computationally Designed Non-nucleoside Inhibitors and Their Interactions With HIV-1 Reverse Transcriptase
Structural Studies and Structure Activity Relationships for Novel Computationally Designed Non-nucleoside Inhibitors and Their Interactions With HIV-1 Reverse Transcriptase Open
Reverse transcriptase (RT) from the human immunodeficiency virus continues to be an attractive drug target for antiretroviral therapy. June 2022 will commemorate the 30th anniversary of the first Human Immunodeficiency Virus (HIV) RT cryst…
View article: Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance
Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance Open
Catechol diether compounds have nanomolar antiviral and enzymatic activity against HIV with reverse transcriptase (RT) variants containing K101P, a mutation that confers high-level resistance to FDA-approved non-nucleoside inhibitors efavi…
View article: Structure-Based Evaluation of Non-nucleoside Inhibitors with Improved Potency and Solubility That Target HIV Reverse Transcriptase Variants
Structure-Based Evaluation of Non-nucleoside Inhibitors with Improved Potency and Solubility That Target HIV Reverse Transcriptase Variants Open
The development of novel non-nucleoside inhibitors (NNRTIs) with activity against variants of HIV reverse transcriptase (RT) is crucial for overcoming treatment failure. The NNRTIs bind in an allosteric pocket in RT ∼10 Å away from the act…
View article: Illuminating the Molecular Mechanisms of Tyrosine Kinase Inhibitor Resistance for the FGFR1 Gatekeeper Mutation: The Achilles’ Heel of Targeted Therapy
Illuminating the Molecular Mechanisms of Tyrosine Kinase Inhibitor Resistance for the FGFR1 Gatekeeper Mutation: The Achilles’ Heel of Targeted Therapy Open
Human fibroblast growth factor receptors (FGFRs) 1-4 are a family of receptor tyrosine kinases that can serve as drivers of tumorigenesis. In particular, FGFR1 gene amplification has been implicated in squamous cell lung and breast cancers…