Search Results - "Lewis, Hal A"
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Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core
Published in Bioorganic & medicinal chemistry letters (01-05-2015)“…Glycogen synthase kinase-3 (GSK-3) has been proposed to play a crucial role in the pathogenesis of many diseases including cancer, stroke, bipolar disorders,…”
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Channel Gating Regulation by the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) First Cytosolic Loop
Published in The Journal of biological chemistry (22-01-2016)“…In this study, we present data indicating a robust and specific domain interaction between the cystic fibrosis transmembrane conductance regulator (CFTR) first…”
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Structures of a minimal human CFTR first nucleotide-binding domain as a monomer, head-to-tail homodimer, and pathogenic mutant
Published in Protein engineering, design and selection (01-05-2010)“…Upon removal of the regulatory insert (RI), the first nucleotide binding domain (NBD1) of human cystic fibrosis transmembrane conductance regulator (CFTR) can…”
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Methotrexate-induced cutaneous ulceration in 3 nonpsoriatic patients: Report of a rare side effect
Published in JAAD Case Reports (01-05-2017)Get full text
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Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form
Published in Proceedings of the National Academy of Sciences - PNAS (27-03-2018)“…For cancer cells to survive and proliferate, they must escape normal immune destruction. One mechanism by which this is accomplished is through immune…”
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The Tetranucleotide UCAY Directs the Specific Recognition of RNA by the Nova K-Homology 3 Domain
Published in Proceedings of the National Academy of Sciences - PNAS (23-05-2000)“…The Nova family of proteins are target antigens in the autoimmune disorder paraneoplastic opsoclonus-myoclonus ataxia and contain K-homology (KH)-type RNA…”
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Structure–activity relationship (SAR) studies on substituted N-(pyridin-3-yl)-2-amino-isonicotinamides as highly potent and selective glycogen synthase kinase-3 (GSK-3) inhibitors
Published in Bioorganic & medicinal chemistry letters (01-02-2023)“…[Display omitted] In our continuing efforts to explore structure–activity relationships around the novel class of potent, isonicotinamide-based GSK3 inhibitors…”
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Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase‑3 Inhibitors
Published in Journal of medicinal chemistry (11-02-2016)“…GSK-3 is a serine/threonine kinase that has numerous substrates. Many of these proteins are involved in the regulation of diverse cellular functions, including…”
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5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site Inhibitors
Published in Journal of medicinal chemistry (14-02-2019)“…A series of 5,6,7,8-tetrahydro-1,6-naphthyridine derivatives targeting the allosteric lens-epithelium-derived-growth-factor-p75 (LEDGF/p75)-binding site on…”
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Neutrophil‐predominant bullous pemphigoid induced by checkpoint inhibitors: A case series
Published in Journal of cutaneous pathology (01-08-2020)“…Checkpoint inhibitors have been revolutionary in the treatment of metastatic melanoma, non‐small‐cell lung cancer, and renal cell carcinoma. By restricting…”
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Inhibition of influenza virus replication via small molecules that induce the formation of higher-order nucleoprotein oligomers
Published in Proceedings of the National Academy of Sciences - PNAS (13-09-2011)“…Influenza nucleoprotein (NP) plays multiple roles in the virus life cycle, including an essential function in viral replication as an integral component of the…”
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Crystal structures of Nova-1 and Nova-2 K-homology RNA-binding domains
Published in Structure (London) (15-02-1999)“…Background: Nova-1 and Nova-2 are related neuronal proteins that were initially cloned using antisera obtained from patients with the autoimmune neurological…”
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Pemphigus foliaceus in a patient with gastrointestinal stromal tumor treated with adjuvant imatinib mesylate
Published in Dermatology online journal (01-01-2020)“…Pemphigus is an autoimmune bullous disease with a number of described associations, including medications, which have been grouped into three structural…”
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SGX393 inhibits the CML mutant Bcr-AblT315I and preempts in vitro resistance when combined with nilotinib or dasatinib
Published in Proceedings of the National Academy of Sciences - PNAS (08-04-2008)“…Imatinib inhibits Bcr-Abl, the oncogenic tyrosine kinase that causes chronic myeloid leukemia. The second-line inhibitors nilotinib and dasatinib are effective…”
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Impact of the ΔF508 Mutation in First Nucleotide-binding Domain of Human Cystic Fibrosis Transmembrane Conductance Regulator on Domain Folding and Structure
Published in The Journal of biological chemistry (14-01-2005)“…Cystic fibrosis is caused by defects in the cystic fibrosis transmembrane conductance regulator (CFTR), commonly the deletion of residue Phe-508 (ΔF508) in the…”
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Overuse of Magnetic Resonance Imaging in the Diagnosis and Treatment of Moderate to Severe Osteoarthritis
Published in The Iowa orthopaedic journal (2018)“…MRI in the evaluation of end-stage knee joint osteoarthritis (OA) is usually unnecessary when radiographic and clinical evidence of gonarthrosis is clear. The…”
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Human Apolipoprotein E4 Worsens Acute Axonal Pathology but Not Amyloid-β Immunoreactivity After Traumatic Brain Injury in 3xTG-AD Mice
Published in Journal of neuropathology and experimental neurology (01-05-2013)“…ABSTRACTApolipoprotein E4 (APOE4) genotype is a risk factor for poor outcome after traumatic brain injury (TBI), particularly in young patients, but the…”
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Structure of nucleotide-binding domain 1 of the cystic fibrosis transmembrane conductance regulator
Published in The EMBO journal (28-01-2004)“…Cystic fibrosis transmembrane conductance regulator (CFTR) is an ATP‐binding cassette (ABC) transporter that functions as a chloride channel…”
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Sequence-Specific RNA Binding by a Nova KH Domain: Implications for Paraneoplastic Disease and the Fragile X Syndrome
Published in Cell (04-02-2000)“…The structure of a Nova protein K homology (KH) domain recognizing single-stranded RNA has been determined at 2.4 Å resolution. Mammalian Nova antigens (1 and…”
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SGX393 inhibits the CML mutant Bcr-Abl[superscript T315I] and preempts in vitro resistance when combined with nilotinib or dasatinib
Published in Proceedings of the National Academy of Sciences - PNAS (08-04-2008)“…Imatinib inhibits Bcr-Abl, the oncogenic tyrosine kinase that causes chronic myeloid leukemia. The second-line inhibitors nilotinib and dasatinib are effective…”
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