A5057406085- HIV/AIDS drug development and treatment
- Radical Photochemical Reactions
- Click Chemistry and Applications
- Catalytic C–H Functionalization Methods
- Synthesis and biological activity
- Oxidative Organic Chemistry Reactions
- Catalytic Cross-Coupling Reactions
- Hepatitis C virus research
- Asymmetric Synthesis and Catalysis
- Analytical Chemistry and Chromatography
- Chemical Synthesis and Analysis
- Microbial Natural Products and Biosynthesis
- Biotin and Related Studies
- Chemical Reaction Mechanisms
- Ferrocene Chemistry and Applications
- Folate and B Vitamins Research
- Cancer Immunotherapy and Biomarkers
- Immune cells in cancer
- Immune Cell Function and Interaction
- Catalytic Alkyne Reactions
- X-ray Diffraction in Crystallography
- Bacterial Infections and Vaccines
- Ubiquitin and proteasome pathways
- Cannabis and Cannabinoid Research
- Pancreatic function and diabetes
Bristol-Myers Squibb (United States)
2011-2023
Bristol-Myers Squibb (Germany)
2011-2013
Pfizer (United States)
2001-2009
Stanford University
1997-1998
United States Military Academy
1992
A new strategy toward glycosidase inhibitors, represented by valienamine, which is such an inhibitor itself as well a critical unit of pseudooligosaccharides that function this way, evolved from two newly developed palladium-catalyzed reactions. The applicability palladium(0)-catalyzed net regioselective cis-hydroxyamination derives the reaction vinyl epoxides with isocyanates. utilization cocatalyst in required case and may prove generally useful. bidentate phosphite proved to be most...
In an effort to prepare pneumococcal (Pn) capsular polysaccharide (Ps) vaccines that would be immunogenic in infants, covalent conjugates were prepared for Pn types 6B, 14, 19F, and 23F. Each Ps type was covalently bound outer membrane protein complex from Neisseria meningitidis serogroup B evaluated immunogenicity mice infant monkeys. The induced specific anti-Ps antibody responses rhesus African green monkeys; a conjugate of 6B at doses as low 20 ng. Although levels the group-common cell...
Herein described is an operationally simple procedure for generating benzyl indium species from readily available bromides and metal followed by in situ palladium-catalyzed coupling with aryl halides. The provides diarylmethanes modest to excellent yield tolerates a variety of functional groups both partners.
Programmed cell death protein 1 (PD-1) immune checkpoint blockade therapy has revolutionized cancer treatment. Although PD-1 is effective in a subset of patients with cancer, many fail to respond because either primary or acquired resistance. Thus, next-generation strategies are needed expand the depth and breadth clinical responses. Toward this end, we designed human T phenotypic high-throughput screening strategy identify small molecules distinct complementary mechanisms action blockade....
We describe a phenotypic screening and optimization strategy to discover compounds that block intracellular checkpoint signaling in T-cells. identified dual DGKα ζ inhibitors notwithstanding the modest similarity between α relative other DGK isoforms. Optimized produced cytokine release T-cell proliferation consistent with inhibition potentiated an immune response human mouse Additionally, lead inhibitor BMS-502 demonstrated dose-dependent stimulation OT-1 model, setting stage for drug...
Inhibition of α4β1/vascular cell adhesion molecule-1 (VCAM-1) interactions have therapeutic potential in treating allergic airway disease because the importance these molecules trafficking eosinophils, lymphocytes, and monocytes. We examined several small molecule inhibitors α4β1/VCAM-1 with vitro potencies (IC<sub>50</sub> values) ranging from 0.52 nM (CP-664511; 3-[3-(1-{2-[3-methoxy-4-(3-<i>O</i>-tolyl-ureido)phenyl]-acetylamino}-3-methyl-butyl)isoxazol-5-yl]-propionic acid) to 38.5...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTAcidic derivatives of homocysteine thiolactone: utility as anionic linkersW. J. Leanza, L. S. Chupak, R. Tolman, and MarburgCite this: Bioconjugate Chem. 1992, 3, 6, 514–518Publication Date (Print):November 1, 1992Publication History Published online1 May 2002Published inissue 1 November 1992https://pubs.acs.org/doi/10.1021/bc00018a009https://doi.org/10.1021/bc00018a009research-articleACS PublicationsRequest reuse permissionsArticle...
The present study describes a novel methodology for the detection of reactive compounds using in vitro peptide-trapping and liquid chromatography-high-resolution accurate mass spectrometry (LC-HRMS). Compounds that contain electrophilic groups can covalently bind to nucleophilic moieties proteins form adducts. Such adducts are thought be associated with drug-mediated toxicity therefore represent potential liabilities drug discovery programs. In addition, identified biological screening data...
ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXTShort Preparation of (S)-(E)-1-(O-Methylmandeloxy)butadieneBarry M. Trost, Louis S. Chupak, and Thomas LübbersView Author Information Department Chemistry, Stanford University, Stanford, California 94305 Cite this: J. Org. Chem. 1997, 62, 3, 736Publication Date (Web):February 7, 1997Publication History Received20 September 1996Published online7 February 1997Published inissue 1...
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Abstract Review: 52 refs.
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 200 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”