Search Results - "Burger, Matthew T"
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Pan-PIM Kinase Inhibition Provides a Novel Therapy for Treating Hematologic Cancers
Published in Clinical cancer research (01-04-2014)“…PIM kinases have been shown to act as oncogenes in mice, with each family member being able to drive progression of hematologic cancers. Consistent with this,…”
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Identification of N‑(4-((1R,3S,5S)‑3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies
Published in Journal of medicinal chemistry (12-11-2015)“…Pan proviral insertion site of Moloney murine leukemia (PIM) 1, 2, and 3 kinase inhibitors have recently begun to be tested in humans to assess whether pan PIM…”
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Human CD180 Transmits Signals via the PIM-1L Kinase
Published in PloS one (10-11-2015)“…Toll-like receptors (TLRs) are important sensors of the innate immune system that recognize conserved structural motifs and activate cells via a downstream…”
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Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer
Published in ACS medicinal chemistry letters (13-10-2011)“…Phosphoinositide-3-kinases (PI3Ks) are important oncology targets due to the deregulation of this signaling pathway in a wide variety of human cancers. Herein…”
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Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors
Published in ACS medicinal chemistry letters (13-01-2011)“…Phospoinositide-3-kinases (PI3K) are important oncology targets due to the deregulation of this signaling pathway in a wide variety of human cancers. A series…”
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Design, Synthesis, and In Vitro and In Vivo Evaluation of Cereblon Binding Bruton’s Tyrosine Kinase (BTK) Degrader CD79b Targeted Antibody–Drug Conjugates
Published in Bioconjugate chemistry (21-02-2024)“…Antibody–drug conjugates (ADCs) are an established modality that allow for targeted delivery of a potent molecule, or payload, to a desired site of action…”
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Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic
Published in Journal of medicinal chemistry (12-03-2020)“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
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Synthesis and Structure–Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases
Published in Journal of medicinal chemistry (10-12-2020)“…Overexpression of PIM 1, 2, and 3 kinases is frequently observed in many malignancies. Previously, we discovered a potent and selective pan-PIM kinase…”
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Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers
Published in Journal of medicinal chemistry (22-06-2017)“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
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Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases
Published in Bioorganic & medicinal chemistry letters (01-11-2011)“…A series of novel 3,5-disubstituted indole derivatives as potent and selective inhibitors of all three members of the Pim kinase family is described. High…”
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Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model
Published in Bioorganic & medicinal chemistry letters (01-02-2016)“…[Display omitted] Alterations in PI3K/AKT signaling are known to be implicated with tumorigenesis. The PI3 kinases family of lipid kinases has been an…”
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Design, synthesis and structure activity relationship of potent pan-PIM kinase inhibitors derived from the pyridyl carboxamide scaffold
Published in Bioorganic & medicinal chemistry letters (01-05-2016)“…[Display omitted] The Pim proteins (1, 2 and 3) are serine/threonine kinases that have been found to be upregulated in many hematological malignancies and…”
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Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors
Published in ACS medicinal chemistry letters (12-12-2013)“…Proviral insertion of Moloney virus (PIM) 1, 2, and 3 kinases are serine/threonine kinases that normally function in survival and proliferation of…”
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Synthesis and Antibacterial Activity of Novel C12 Vinyl Ketolides
Published in Journal of medicinal chemistry (09-03-2006)“…A novel series of C12 vinyl erythromycin derivatives have been discovered which exhibit in vitro and in vivo potency against key respiratory pathogens. The C12…”
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Synthesis and antibacterial activity of novel C12 ethyl ketolides
Published in Bioorganic & medicinal chemistry (15-08-2006)“…A novel series of C(12) ethyl erythromycin derivatives have been discovered which exhibit in vitro and in vivo potency against key respiratory pathogens,…”
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Synthetic Ionophores. Encoded Combinatorial Libraries of Cyclen-based Receptors for Cu2+ and Co2
Published in Journal of organic chemistry (01-11-1995)Get full text
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Synthetic strategies in combinatorial chemistry
Published in Current opinion in chemical biology (01-06-1997)“…Different synthetic strategies are required for the two kinds of libraries being developed for combinatoral chemistry. Preparation of a ‘focused’ library…”
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Simple Structural Requirements for Sequence-Selective Peptide Receptors? Tripeptide Binding by a Podand Ionophore
Published in Journal of organic chemistry (11-07-1997)“…A simple, dye(R)-labeled and conformationally restricted ionophore 2 was prepared and screened for peptide binding using solid-supported combinatorial…”
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