Search Results - "Palmer, James T."
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A Novel, Orally Bioavailable, Small-Molecule Inhibitor of PCSK9 With Significant Cholesterol-Lowering Properties In Vivo
Published in Journal of lipid research (01-11-2022)“…Proprotein convertase subtilisin kexin type 9 (PCSK9) inhibits the clearance of low-density lipoprotein (LDL) cholesterol (LDL-C) from plasma by directly…”
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Discovery of Selective Irreversible Inhibitors for Bruton's Tyrosine Kinase
Published in ChemMedChem (15-01-2007)“…A series of highly selective irreversible inhibitors for Bruton's tyrosine kinase (Btk) was developed using a structural bioinformatics approach. Their…”
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A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove
Published in Bioorganic & medicinal chemistry (15-03-2020)“…[Display omitted] Proprotein convertase (PC) subtilisin kexin type 9 (PCSK9) inhibits the clearance of low density lipoprotein (LDL) cholesterol from plasma by…”
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The making of a world historical moment: The Battle of Tours (732/3) in the nineteenth century
Published in Postmedieval a journal of medieval cultural studies (01-06-2019)“…The Battle of Tours (or Poitiers) in 732/3 is frequently cited as a turning point in world history, when the advance of Muslim Arabs was decisively halted by…”
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The Crystal Structure of Human Cathepsin F and Its Implications for the Development of Novel Immunomodulators
Published in Journal of molecular biology (20-09-2002)“…Cathepsin F is a lysosomal cysteine protease of the papain family, and likely plays a regulatory role in processing the invariant chain that is associated with…”
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The Global Eminent Life: Sixth-Century Collected Biographies from Gregory of Tours to Huijiao of Jiaxiang Temple
Published in Medieval worlds (2018)Get full text
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Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors
Published in Bioorganic & medicinal chemistry letters (15-12-2013)“…The discovery and optimisation of a new class of benzothiazole small molecules that inhibit bacterial DNA gyrase and topoisomerase IV are described…”
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Discovery and in vivo evaluation of alcohol-containing benzothiazoles as potent dual-targeting bacterial DNA supercoiling inhibitors
Published in Bioorganic & medicinal chemistry letters (01-09-2014)“…A series of dual-targeting, alcohol-containing benzothiazoles has been identified with superior antibacterial activity and drug-like properties. Early lead…”
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Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)
Published in Bioorganic & medicinal chemistry letters (15-10-2009)“…Details of SAR studies leading to CYT387, a potent and selective dual JAK1 and JAK2 inhibitor, are reported. A series of phenylaminopyrimidines has been…”
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Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K
Published in Bioorganic & medicinal chemistry letters (01-11-2005)“…Replacing an amide bond with a trifluoroethylamine leads to potent and selective inhibitors of cathepsin K. The CF 3 group provides a non-basic amine that…”
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Optimization of Subsite Binding to the β5 Subunit of the Human 20S Proteasome Using Vinyl Sulfones and 2-Keto-1,3,4-oxadiazoles: Syntheses and Cellular Properties of Potent, Selective Proteasome Inhibitors
Published in Journal of medicinal chemistry (18-05-2006)“…Beginning with the peptide sequence Cbz-Ile-Glu(OtBu)-Ala-Leu found in PSI (3), a series of vinyl sulfones (VS) were synthesized for evaluation as inhibitors…”
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Keto-1,3,4-oxadiazoles as cathepsin K inhibitors
Published in Bioorganic & medicinal chemistry letters (01-06-2006)“…We have prepared a series of cathepsin K inhibitors bearing the keto-1,3,4-oxadiazole warhead capable of forming a hemithioketal complex with the target…”
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Vinyl Sulfones as Mechanism-Based Cysteine Protease Inhibitors
Published in Journal of medicinal chemistry (01-08-1995)Get full text
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A Novel Class of Nonpeptidic Biaryl Inhibitors of Human Cathepsin K
Published in Journal of medicinal chemistry (14-08-2003)“…A novel series of nonpeptidic biaryl compounds was identified as potent and reversible inhibitors of cathepsin K. The P2−P3 amide bond of a known amino…”
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Evidence for a Protective Role of Metallothionein-1 in Focal Cerebral Ischemia
Published in Proceedings of the National Academy of Sciences - PNAS (26-10-1999)“…Metallothioneins (MTs) are a family of metal binding proteins that have been proposed to participate in a cellular defense against zinc toxicity and free…”
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VEGF antagonism reduces edema formation and tissue damage after ischemia/reperfusion injury in the mouse brain
Published in The Journal of clinical investigation (01-12-1999)Get full text
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Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K
Published in Bioorganic & medicinal chemistry letters (15-08-2006)“…A novel series of potent and selective inhibitors of cysteine protease cathepsin K is described. The synthesis and biological profile of a novel series of…”
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β-Substituted Cyclohexanecarboxamide: A Nonpeptidic Framework for the Design of Potent Inhibitors of Cathepsin K
Published in Journal of medicinal chemistry (09-02-2006)“…A new series of nonpeptidic cathepsin K inhibitors that are based on a β-substituted cyclohexanecarboxamide motif has been developed. Lead optimization yielded…”
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