Search Results - "LASKO, Loren M"
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Targeting Lineage-specific MITF Pathway in Human Melanoma Cell Lines by A-485, the Selective Small-molecule Inhibitor of p300/CBP
Published in Molecular cancer therapeutics (01-12-2018)“…Metastatic melanoma is responsible for approximately 80% of deaths from skin cancer. Microphthalmia-associated transcription factor (MITF) is a…”
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Discovery of a Potent and Selective Covalent p300/CBP Inhibitor
Published in ACS medicinal chemistry letters (13-05-2021)“…Aberrant gene activation driven by the histone acetyltransferases p300 and CREB binding protein (CBP) has been linked to several diseases, including cancers…”
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Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours
Published in Nature (London) (05-10-2017)“…A potent and selective catalytic inhibitor of p300/CBP histone acetyltransferases suppresses tumour proliferation across multiple cell lineages, illustrating…”
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IL-23 induces regulatory T cell plasticity with implications for inflammatory skin diseases
Published in Scientific reports (27-11-2019)“…Foxp3 + regulatory T cells (Tregs) represent a major fraction of skin resident T cells. Although normally protective, Tregs have been shown to produce…”
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The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity
Published in Nature chemical biology (01-03-2017)“…Editorial Summary SUV4-20 members mediate the di- and trimethylation of lysine 20 on histone H4. A chemical screen led to the identification of A-196 as a…”
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ABT-888, an Orally Active Poly(ADP-Ribose) Polymerase Inhibitor that Potentiates DNA-Damaging Agents in Preclinical Tumor Models
Published in Clinical cancer research (01-05-2007)“…Purpose: To evaluate the preclinical pharmacokinetics and antitumor efficacy of a novel orally bioavailable poly(ADP-ribose) polymerase (PARP) inhibitor,…”
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Discovery of spirohydantoins as selective, orally bioavailable inhibitors of p300/CBP histone acetyltransferases
Published in Bioorganic & medicinal chemistry letters (01-05-2021)“…[Display omitted] p300 and CREB-binding protein (CBP) are essential for a multitude of cellular processes. Dysregulation of p300/CBP histone acetyltransferase…”
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Author Correction: Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours
Published in Nature (London) (01-06-2018)“…In the originally published version of this Letter, the authors Arthur F. Kluge, Michael A. Patane and Ce Wang were inadvertently omitted from the author list…”
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Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors
Published in Bioorganic & medicinal chemistry letters (15-12-2012)“…A high throughput screening (HTS) hit, 1 (Plk1 Ki=2.2μM) was optimized and evaluated for the enzymatic inhibition of Plk-1 kinase. Molecular modeling suggested…”
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Pyrimidine-Based Tricyclic Molecules as Potent and Orally Efficacious Inhibitors of Wee1 Kinase
Published in ACS medicinal chemistry letters (08-01-2015)“…Aided by molecular modeling, compounds with a pyrimidine-based tricyclic scaffold were designed and confirmed to inhibit Wee1 kinase. Structure–activity…”
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Abstract LB-A23: Discovery of a potent catalytic p300/CBP inhibitor that targets lineage-specific tumors
Published in Molecular cancer therapeutics (01-01-2018)“…The dynamic and reversible acetylation of proteins catalyzed by histone acetyltransferases (HATs) and histone deacetylases (HDACs) is a major epigenetic…”
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Discovery of a potent catalytic p300/CBP inhibitor that targets lineage-specific tumors
Published in Nature (London) (27-09-2017)“…The dynamic and reversible acetylation of proteins catalyzed by histone acetyltransferases (HATs) and histone deacetylases (HDACs) is a major epigenetic…”
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