Search Results - "Marineau, Jason J."
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Discovery and Characterization of SY-1365, a Selective, Covalent Inhibitor of CDK7
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Recent studies suggest that targeting transcriptional machinery can lead to potent and selective anticancer effects in cancers dependent on high and constant…”
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Gene expression–based discovery of atovaquone as a STAT3 inhibitor and anticancer agent
Published in Blood (06-10-2016)“…The oncogenic transcription factor signal transducer and activator of transcription 3 (STAT3) is frequently activated inappropriately in a wide range of…”
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Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7
Published in Journal of medicinal chemistry (27-01-2022)“…CDK7 has emerged as an exciting target in oncology due to its roles in two important processes that are misregulated in cancer cells: cell cycle and…”
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Genome-wide localization of small molecules
Published in Nature biotechnology (01-01-2014)“…A new method called Chem-seq reveals the genomic binding sites of drugs that target DNA and chromatin. A vast number of small-molecule ligands, including…”
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Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors
Published in Nature communications (18-12-2012)“…Selective inhibition of protein methyltransferases is a promising new approach to drug discovery. An attractive strategy towards this goal is the development…”
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Selective inhibition of CDK7 reveals high-confidence targets and new models for TFIIH function in transcription
Published in Genes & development (01-11-2020)“…CDK7 associates with the 10-subunit TFIIH complex and regulates transcription by phosphorylating the C-terminal domain (CTD) of RNA polymerase II (RNAPII). Few…”
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Biased Multicomponent Reactions to Develop Novel Bromodomain Inhibitors
Published in Journal of medicinal chemistry (13-11-2014)“…BET bromodomain inhibition has contributed new insights into gene regulation and emerged as a promising therapeutic strategy in cancer. Structural analogy of…”
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Structure-Guided DOT1L Probe Optimization by Label-Free Ligand Displacement
Published in ACS chemical biology (20-03-2015)“…The DOT1L lysine methyltransferase has emerged as a validated therapeutic target in MLL-rearranged (MLLr) acute leukemias. Although S-adenosylmethionine…”
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Development and Evaluation of a Solid-Supported Cyclobutadieneiron Tricarbonyl Complex for Parallel Synthesis Applications
Published in ACS combinatorial science (11-06-2012)“…Cycloadditions of cyclobutadiene can offer rapid access to rigid polycyclic ring systems. Further functionalization of these strained-ring cycloadducts can…”
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7,9-Diaryl-1,6,8-trioxaspiro[4.5]dec-3-en-2-ones: Readily accessible and highly potent anticancer compounds
Published in Bioorganic & medicinal chemistry letters (15-08-2014)“…7,9-Diaryl-1,6,8-trioxaspiro[4.5]dec-3-en-2-ones are a recently described group of spirocyclic butenolides that can be generated rapidly and as a single…”
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Corrigendum: Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors
Published in Nature communications (01-05-2013)Get full text
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Abstract 3230: Genome-wide localization of anti-cancer drugs
Published in Cancer research (Chicago, Ill.) (01-10-2014)“…Abstract A vast number of small-molecule ligands, including therapeutic drugs under development and in clinical use, elicit their effects by binding specific…”
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Genome-wide determination of drug localization
Published in Nature biotechnology (15-12-2013)“…A vast number of small-molecule ligands, including therapeutic drugs under development and in clinical use, elicit their effects by binding specific proteins…”
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Correction: Corrigendum: Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors
Published in Nature communications (21-05-2013)“…Nature Communications 3: Article number: 1288 (2012); Published: 18 December 2012; Updated: 21 May 2013. While this Article was undergoing peer review,…”
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