Search Results - "Lacey, Brian"
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Pharmacological inhibition of hematopoietic progenitor kinase 1 positively regulates T-cell function
Published in PloS one (03-12-2020)“…Hematopoietic progenitor kinase 1 (HPK1), a hematopoietic cell-specific Ste20-related serine/threonine kinase, is a negative regulator of signal transduction…”
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2
An orally available non-nucleotide STING agonist with antitumor activity
Published in Science (American Association for the Advancement of Science) (21-08-2020)“…Pharmacological activation of the STING (stimulator of interferon genes)-controlled innate immune pathway is a promising therapeutic strategy for cancer. Here…”
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3
Discovery of a Novel cGAMP Competitive Ligand of the Inactive Form of STING
Published in ACS medicinal chemistry letters (10-01-2019)“…Drugging large protein pockets is a challenge due to the need for higher molecular weight ligands, which generally possess undesirable physicochemical…”
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4
Structural basis for effectiveness of siderophore-conjugated monocarbams against clinically relevant strains of Pseudomonas aeruginosa
Published in Proceedings of the National Academy of Sciences - PNAS (21-12-2010)“…Pseudomonas aeruginosa is an opportunistic Gram-negative pathogen that causes nosocomial infections for which there are limited treatment options…”
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5
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer
Published in Journal of medicinal chemistry (14-04-2022)“…Stereochemically and structurally complex cyclic dinucleotide-based stimulator of interferon genes (STING) agonists were designed and synthesized to access a…”
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6
Multiple Synthetic Routes to the Mini-Protein Omomyc and Coiled-Coil Domain Truncations
Published in Journal of organic chemistry (07-02-2020)“…The Myc transcription factor represents an “undruggable” target of high biological interest due to its central role in various cancers. An abbreviated form of…”
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The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer
Published in Journal of medicinal chemistry (08-04-2021)“…Protein arginine methyltransferase 5 (PRMT5) is a type II arginine methyltransferase that catalyzes the post-translational symmetric dimethylation of protein…”
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Allosteric Modulation of Protein Arginine Methyltransferase 5 (PRMT5)
Published in ACS medicinal chemistry letters (10-09-2020)“…Protein arginine methyltransferase 5 (PRMT5) belongs to a family of enzymes that regulate the posttranslational modification of histones and other proteins via…”
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Clinically Relevant Gram-Negative Resistance Mechanisms Have No Effect on the Efficacy of MC-1, a Novel Siderophore-Conjugated Monocarbam
Published in Antimicrobial Agents and Chemotherapy (01-12-2012)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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10
Identification of Potent Reverse Indazole Inhibitors for HPK1
Published in ACS medicinal chemistry letters (11-03-2021)“…Hematopoietic progenitor kinase (HPK1), a negative regulator of TCR-mediated T-cell activation, has been recognized as a novel antitumor immunotherapy target…”
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11
Seasonality of Nosema ceranae Infections and Their Relationship with Honey Bee Populations, Food Stores, and Survivorship in a North American Region
Published in Veterinary sciences (08-09-2020)“…Nosema ceranae is an emerging pathogen of the western honey bee (Apis mellifera L.), and thus its seasonality and impact on bee colonies is not sufficiently…”
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12
Distinctive Attributes of β-Lactam Target Proteins in Acinetobacter baumannii Relevant to Development of New Antibiotics
Published in Journal of the American Chemical Society (21-12-2011)“…Multi-drug-resistant forms of the Gram-negative pathogen Acinetobacter baumannii are an emerging threat to human health and further complicate the general…”
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13
Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds
Published in ACS medicinal chemistry letters (08-04-2021)“…Hematopoietic progenitor kinase 1 (HPK1), a serine/threonine kinase, is a negative immune regulator of T cell receptor (TCR) and B cell signaling that is…”
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14
Early Insights into the Interactions of Different β-Lactam Antibiotics and β-Lactamase Inhibitors against Soluble Forms of Acinetobacter baumannii PBP1a and Acinetobacter sp. PBP3
Published in Antimicrobial Agents and Chemotherapy (01-11-2012)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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15
Development of High-Throughput Assays for Evaluation of Hematopoietic Progenitor Kinase 1 Inhibitors
Published in SLAS discovery (01-01-2021)“…Hematopoietic progenitor kinase 1 (HPK1), also referred to as mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1), is a serine/threonine kinase…”
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16
Selenium in Thioredoxin Reductase: A Mechanistic Perspective
Published in Biochemistry (Easton) (02-12-2008)“…Most high M r thioredoxin reductases (TRs) have the unusual feature of utilizing a vicinal disulfide bond (Cys1−Cys2) which forms an eight-membered ring during…”
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Characterization of mitochondrial thioredoxin reductase from C. elegans
Published in Biochemical and biophysical research communications (04-08-2006)“…Thioredoxin reductase catalyzes the NADPH-dependent reduction of the catalytic disulfide bond of thioredoxin. In mammals and other higher eukaryotes,…”
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Investigation of the C-Terminal Redox Center of High-M r Thioredoxin Reductase by Protein Engineering and Semisynthesis
Published in Biochemistry (Easton) (21-08-2007)“…High-molecular weight thioredoxin reductases (TRs) catalyze the reduction of the redox-active disulfide bond of thioredoxin, but an important difference in the…”
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Investigation of the C-Terminal Redox Center of High-Mr Thioredoxin Reductase by Protein Engineering and Semisynthesis
Published in Biochemistry (Easton) (21-08-2007)“…High-molecular weight thioredoxin reductases (TRs) catalyze the reduction of the redox-active disulfide bond of thioredoxin, but an important difference in the…”
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20
Synthesis of peptide substrates for mammalian thioredoxin reductase
Published in Journal of peptide science (01-05-2008)“…Mammalian thioredoxin reductase (TR) catalyzes the reduction of the redox‐active disulfide bond of thioredoxin (Trx) and is similar in structure and mechanism…”
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