Search Results - "Bowen, Scott J."
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Type 2 inhibitor leads of human tropomyosin receptor kinase (hTrkA)
Published in Bioorganic & medicinal chemistry letters (01-10-2019)“…[Display omitted] In silico virtual screening using the ligand-based ROCS approach and the commercially purchasable compound collection from the ZINC database…”
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Lead identification and characterization of hTrkA type 2 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-11-2019)“…Virtual in silico structure-guided modeling, followed by in vitro biochemical screening of a subset of commercially purchasable compound collection resulted in…”
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Pro region engineering of nerve growth factor by deep mutational scanning enables a yeast platform for conformational epitope mapping of anti-NGF monoclonal antibodies
Published in Biotechnology and bioengineering (12-04-2018)“…Nerve growth factor (NGF) plays a central role in multiple chronic pain conditions. As such, anti-NGF monoclonal antibodies (mAbs) that function by…”
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Deciphering the Allosteric Binding Mechanism of the Human Tropomyosin Receptor Kinase A (hTrkA) Inhibitors
Published in ACS chemical biology (21-06-2019)“…Access to cryptic binding pockets or allosteric sites on a kinase that present themselves when the enzyme is in a specific conformational state offers a…”
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Pro region engineering of nerve growth factor by deep mutational scanning enables a yeast platform for conformational epitope mapping of anti‐NGF monoclonal antibodies
Published in Biotechnology and bioengineering (01-08-2018)“…Nerve growth factor (NGF) plays a central role in multiple chronic pain conditions. As such, anti‐NGF monoclonal antibodies (mAbs) that function by…”
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In Pursuit of an Allosteric Human Tropomyosin Kinase A (hTrkA) Inhibitor for Chronic Pain
Published in ACS medicinal chemistry letters (11-11-2021)“…Human β-nerve growth factor (β-NGF) and its associated receptor, human tropomyosin receptor kinase A (hTrkA), have been demonstrated to be key factors in the…”
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Synthetic inhibitor leads of human tropomyosin receptor kinase A (TrkA)
Published in RSC medicinal chemistry (01-03-2020)“…In silico virtual screening followed by in vitro biochemical, biophysical, and cellular screening resulted in the identification of distinctly different h TrkA…”
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Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro[3.5]nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain
Published in Bioorganic & medicinal chemistry letters (01-11-2011)“…Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase responsible for the degradation of fatty acid amide signaling molecules such as…”
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Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 1: Identification of 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane as lead scaffolds
Published in Bioorganic & medicinal chemistry letters (01-11-2011)“…Herein we report the identification of two new fatty acid amide hydrolase (FAAH) inhibitor lead series with FAAH k inact/ K i potency values greater than 1500…”
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Structure based design of novel irreversible FAAH inhibitors
Published in Bioorganic & medicinal chemistry letters (15-10-2009)“…The design and synthesis a series of novel FAAH irreversible azetidine urea inhibitors from PF-3845 are described. Our SAR studies allowed us to optimize this…”
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Synthetic inhibitor leads of human tropomyosin receptor kinase A (hTrkA)† †Atomic coordinates of the kinase domain of hTrkA. Ligand have been deposited in Protein Data Bank (PDB) under PDB codes 1: 6PMB; 3: 6PMA; 5: 6PME; 6: 6PMC. ‡ ‡The manuscript was written by G. S. All authors have given approval to the final version of the manuscript. § §All experimental procedures are available as part of the ESI in ref. 23–25. ¶ ¶Electronic supplementary information (ESI) available: Computational workflow
Published in RSC medicinal chemistry (10-01-2020)“…New h TrkA kinase domain type 2 inhibitors and mixed type 1/type 2 inhibitor leads disclosed here offers a differential starting point to investigate the…”
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Diffuse Vascular Spasm Associated With 4-Bromo-2,5-Dimethoxyamphetamine Ingestion
Published in JAMA : the journal of the American Medical Association (18-03-1983)“…A 39-year-old previously healthy man experienced diffuse, progressive, peripheral arterial spasm 36 hours after the ingestion of concentrated high-grade…”
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