A5109426168- PI3K/AKT/mTOR signaling in cancer
- Asymmetric Hydrogenation and Catalysis
- Cyclopropane Reaction Mechanisms
- Chemical Synthesis and Reactions
- Nanomaterials for catalytic reactions
- Chronic Lymphocytic Leukemia Research
- Ammonia Synthesis and Nitrogen Reduction
- Protein Kinase Regulation and GTPase Signaling
- Catalytic C–H Functionalization Methods
- Biochemical and Molecular Research
- Peptidase Inhibition and Analysis
- Protein Degradation and Inhibitors
- Asymmetric Synthesis and Catalysis
- Ubiquitin and proteasome pathways
- Chemical Reactions and Isotopes
- Coordination Chemistry and Organometallics
- Chemical Synthesis and Analysis
- Hydrogen Storage and Materials
- Chronic Myeloid Leukemia Treatments
- Fungal Plant Pathogen Control
- Synthesis and Catalytic Reactions
- HER2/EGFR in Cancer Research
- Melanoma and MAPK Pathways
- Cytokine Signaling Pathways and Interactions
- Advanced Synthetic Organic Chemistry
Wenzhou Medical University
2025
Henan Polytechnic University
2025
Wellspring Biosciences (United States)
2013-2022
Kura Oncology (United States)
2017-2021
Intel (United States)
2009-2013
La Jolla Alcohol Research
2010-2011
Genomics Institute of the Novartis Research Foundation
2005-2010
University at Buffalo, State University of New York
2000-2002
Wake Forest University
2001
Fudan University
1995-1999
KRAS gain-of-function mutations occur in approximately 30% of all human cancers. Despite more than 30 years KRAS-focused research and development efforts, no targeted therapy has been discovered for cancers with mutations. Here, we describe ARS-853, a selective, covalent inhibitor KRAS(G12C) that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein preventing activation. Based on rates engagement inhibition observed along mutant-specific mass spectrometry-based assay...
The protein-protein interaction between menin and mixed lineage leukemia 1 (MLL1) plays a critical role in acute leukemias with translocations of the MLL1 gene or mutations nucleophosmin (NPM1) gene. As step toward clinical translation menin-MLL1 inhibitors, we report development MI-3454, highly potent orally bioavailable inhibitor interaction. MI-3454 profoundly inhibited proliferation induced differentiation cells primary patient samples NPM1 mutations. When applied as single agent,...
Tetrakis[N-[4-dodecylphenyl)sulfonyl]-(S)-prolinate]dirhodium [Rh2(S-DOSP)4]-catalyzed decomposition of methyl aryldiazoacetates in the presence substituted ethylbenzenes results benzylic C−H activation by means a rhodium−carbenoid-induced insertion. A Hammet study showed that positive charge buildup occurred on carbon transition state step. toluene and isopropylbenzene is possible, but competing double cyclopropanation occurs with these substrates. The highly regioselective...
The second generation of Bcr-Abl inhibitors nilotinib, dasatinib, and bosutinib developed to override imatinib resistance are not active against the T315I "gatekeeper" mutation. Here we describe a type-II inhibitor 2 (GNF-7), based upon 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one scaffold which is capable potently inhibiting wild-type as well other clinically relevant mutants such G250E, Q252H, Y253H, E255K, E255V, F317L, M351T in biochemical cellular assays. In addition, compound...
Herein, a DBU-catalyzed 1,6-Michael addition of para-quinone methides (p-QMs) under mild reaction conditions with high efficiency (turnover number up to 103) and good excellent yields is reported. The transformation proceeds smoothly range nucleophiles, providing diverse diarylmethane scaffolds efficiency. Mechanistic studies revealed that DBU an proton acceptor donor can promote the methanol p-QMs. A preliminary investigation was also conducted antibacterial properties products.
Trinuclear gold clusters functionalized with N-heterocyclic carbene (NHC) ligands were thermally decomposed to form NHC-stabilized nanoparticles. By systematically adjusting the substituents and electronic structures of carbenes, size Auδ- active sites resulting nanoparticles controlled, thereby modulating their catalytic performance in conversion CO CO2 at minimum temperature 50 °C an excellent efficiency.
[reaction: see text]. Tetrakis[N-[4-dodecylphenyl)sulfonyl]-(S)-prolinato]-dirhodium [Rh2(S-DOSP)4] catalyzed decomposition of methyl aryldiazoacetates in the presence alkenes results allylic C-H activation by means a rhodium-carbene induced insertion. The resulting gamma,delta-unsaturated esters are equivalent to products that would be traditionally obtained from an asymmetric Claisen rearrangement. Highly regio- and enantioselective insertions can achieved, certain cases, good...
The intramolecular type II [3 + 4] cycloaddition between vinylcarbenoids and furans is a practical method for the construction of 5-oxo-10-oxatricyclo[6.2.1.04,9]undeca-3,8(11)-dienes, containing two anti-Bredt double bonds. These tricyclic systems are well functionalized eventual elaboration to natural product CP-263,114. rhodium-stabilized generated by dirhodium tetracarboxylate catalyzed decomposition vinyldiazoacetates. generally considered occur tandem cyclopropanation/Cope...
Abstract Nitroarenes can be conveniently reduced to primary amines in good excellent yields by sodium borohydride the presence of bismuth chloride or antimony chloride.