Search Results - "Goodman, Krista"
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Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4
Published in ACS medicinal chemistry letters (11-05-2017)“…Transient Receptor Potential Vanilloid 4 (TRPV4) is a member of the Transient Receptor Potential (TRP) superfamily of cation channels. TRPV4 is expressed in…”
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Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4)
Published in ACS medicinal chemistry letters (08-08-2019)“…GSK2798745, a clinical candidate, was identified as an inhibitor of the transient receptor potential vanilloid 4 (TRPV4) ion channel for the treatment of…”
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1433 Targeting peptidyl-prolyl isomerase Pin1 to modulate cancer-associated fibroblast phenotype and TGF-beta signaling
Published in Journal for immunotherapy of cancer (01-11-2023)“…BackgroundCancer-associated fibroblasts present a significant barrier to standard of care immunotherapy through multiple mechanisms including deposition of…”
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NADPH oxidase-dependent and -independent mechanisms of reported inhibitors of reactive oxygen generation
Published in Journal of enzyme inhibition and medicinal chemistry (01-02-2013)“…NADPH oxidase isoform-2 (NOX2) generates reactive oxygen species (ROS) that contribute to neurodegenerative and cardiovascular pathologies. However, validation…”
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An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure
Published in Science translational medicine (07-11-2012)“…Pulmonary edema resulting from high pulmonary venous pressure (PVP) is a major cause of morbidity and mortality in heart failure (HF) patients, but current…”
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Potent, Selective and Orally Bioavailable Dihydropyrimidine Inhibitors of Rho Kinase (ROCK1) as Potential Therapeutic Agents for Cardiovascular Diseases
Published in Journal of medicinal chemistry (13-11-2008)“…Recent studies using known Rho-associated kinase isoform 1 (ROCK1) inhibitors along with cellular and molecular biology data have revealed a pivotal role of…”
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Development of Dihydropyridone Indazole Amides as Selective Rho-Kinase Inhibitors
Published in Journal of medicinal chemistry (11-01-2007)“…Rho kinase (ROCK1) mediates vascular smooth muscle contraction and is a potential target for the treatment of hypertension and related disorders. Indazole…”
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Pharmacological Inhibition of C-C Chemokine Receptor 2 Decreases Macrophage Infiltration in the Aortic Root of the Human C-C Chemokine Receptor 2/Apolipoprotein E−/− Mouse: Magnetic Resonance Imaging Assessment
Published in Arteriosclerosis, thrombosis, and vascular biology (01-02-2010)“…PURPOSE—This study assessed the pharmacological effect of a novel selective C-C chemokine receptor (CCR) 2 antagonist (GSK1344386B) on monocyte/macrophage…”
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Discovery of Aminofurazan-azabenzimidazoles as Inhibitors of Rho-Kinase with High Kinase Selectivity and Antihypertensive Activity
Published in Journal of medicinal chemistry (11-01-2007)“…The discovery, proposed binding mode, and optimization of a novel class of Rho-kinase inhibitors are presented. Appropriate substitution on the 6-position of…”
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CCR2 receptor antagonists: Optimization of biaryl sulfonamides to increase activity in whole blood
Published in Bioorganic & medicinal chemistry letters (15-12-2011)“…A series of biarylsulfonamides was identified as hCCR2 receptor antagonist but suffered from high plasma protein binding resulting in a >100 fold shift in…”
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Aminomethylpiperazines as selective urotensin antagonists
Published in Bioorganic & medicinal chemistry (15-08-2008)“…Aminomethylpiperazines, reported previously as being κ-opioid receptor agonists, have been developed into selective, high affinity human urotensin-II…”
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Development of potent and selective small-molecule human Urotensin-II antagonists
Published in Bioorganic & medicinal chemistry (15-06-2008)“…This work describes the development of potent and selective human Urotensin-II antagonists starting from lead compound 1. Several problems relating to oral…”
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Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles
Published in Bioorganic & medicinal chemistry letters (01-07-2008)“…Redesign of the potent human urotensin-II antagonist 1 with the 2-pyrrolidinylmethyl-3-phenyl-piperidine core to a new chemical series with a substituted…”
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Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors
Published in Bioorganic & medicinal chemistry letters (2009)“…A series of potent, selective sulfonylfuran urea endothelial lipase inhibitors is reported. Mechanism of action studies are also discussed. Endothelial lipase…”
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ZUMA-8: A phase 1/2 multicenter study evaluating KTE-X19 in patients (pts) with relapsed/refractory (R/R) chronic lymphocytic leukemia (CLL)
Published in Journal of clinical oncology (20-05-2019)“…Abstract only TPS7566 Background: Despite treatment advances, CLL is largely incurable. First-line targeted therapy with ibrutinib mostly produces durable…”
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Relation of Childhood Sexual Abuse, Intimate Partner Violence, and Depression to Risk Factors for HIV Among Black Men Who Have Sex With Men in 6 US Cities
Published in American journal of public health (1971) (01-12-2015)“…We assessed the relation of childhood sexual abuse (CSA), intimate partner violence (IPV), and depression to HIV sexual risk behaviors among Black men who have…”
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Identification of a Human Whole Blood-Based Endothelial Cell Impedance Assay for Assessing Clinical Transient Receptor Potential Vanilloid 4 Target Engagement Ex Vivo
Published in The Journal of pharmacology and experimental therapeutics (01-03-2021)“…Transient receptor potential vanilloid 4 (TRPV4) channels expressed on pulmonary endothelial cells are activated by elevated pulmonary vascular pressure,…”
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Abstract 5574: Degradation of PIP4K2C by novel bivalent functional degrader LRK-A induces tumor regression in CRC
Published in Cancer research (Chicago, Ill.) (22-03-2024)“…Abstract Phosphatidylinositol 5-phosphate 4-kinase, type II, gamma (PIP4K2C) is a lipid kinase with critical roles in vesicular trafficking,…”
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Engaging, Recruiting, and Retaining Black Men Who Have Sex With Men in Research Studies: Don’t Underestimate the Importance of Staffing—Lessons Learned From HPTN 061, the BROTHERS Study
Published in Journal of public health management and practice (01-11-2014)“…HIV/AIDS in the United States continues to primarily impact men who have sex with men (MSM), with disproportionately high rates among black MSM. The purpose of…”
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Quality home visits: Activities to promote meaningful interactions
Published in Infant mental health journal (01-05-2019)“…ABSTRACT Examination of and support for specific practices that promote high‐quality home visiting are essential as family support programs continue to expand…”
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