Search Results - "Cottom, Josh"
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1
Waste management needs a data revolution – Is plastic pollution an opportunity?
Published in Waste management & research (01-09-2021)Get full text
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Identification and Optimization of Novel Small c‑Abl Kinase Activators Using Fragment and HTS Methodologies
Published in Journal of medicinal chemistry (28-02-2019)“…Abelson kinase (c-Abl) is a ubiquitously expressed, nonreceptor tyrosine kinase which plays a key role in cell differentiation and survival. It was…”
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Abstract 6590: Novel WRN helicase inhibitors selectively target microsatellite unstable cancer cells
Published in Cancer research (Chicago, Ill.) (22-03-2024)“…Microsatellite-unstable (MSI) cancers depend on the WRN helicase to resolve replication stress from expanded (TA)-dinucleotide repeats. WRN is a promising…”
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Abstract 1628: A small-molecule inhibitor of WRN selectively kills MSI-H cancer cells and phenocopies WRN genetic defects
Published in Cancer research (Chicago, Ill.) (04-04-2023)“…Werner syndrome protein (WRN) is a RecQ-family helicase involved in the maintenance of genome integrity. Germline mutations in WRN cause premature aging and…”
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Structure-guided optimization of small molecule c-Abl activators
Published in Journal of computer-aided molecular design (01-02-2014)“…c-Abl kinase is maintained in its normal inactive state in the cell through an assembled, compact conformation. We describe two chemical series that bind to…”
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2-Phenyl-4-piperazinylbenzimidazoles: Orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor
Published in Bioorganic & medicinal chemistry (01-07-2008)“…Antagonism of the gonadotropin releasing hormone (GnRH) receptor has shown positive clinical results in numerous reproductive tissue disorders such as…”
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Assay development and high-throughput screening of small molecular c-Abl kinase activators
Published in Journal of biomolecular screening (01-01-2011)“…A 2-step kinase assay was developed and used in a high-throughput screen (HTS) of more than 1 million compounds in an effort to identify c-Abl tyrosine kinase…”
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Discovery and Characterization of a Cell-Permeable, Small-Molecule c-Abl Kinase Activator that Binds to the Myristoyl Binding Site
Published in Chemistry & biology (25-02-2011)“…c-Abl kinase activity is regulated by a unique mechanism involving the formation of an autoinhibited conformation in which the N-terminal myristoyl group binds…”
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