Search Results - "RUSSELL, Angela J"
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Structure-based development of new RAS-effector inhibitors from a combination of active and inactive RAS-binding compounds
Published in Proceedings of the National Academy of Sciences - PNAS (12-02-2019)“…The RAS gene family is frequently mutated in human cancers, and the quest for compounds that bind to mutant RAS remains a major goal, as it also does for…”
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Small molecule inhibitors of RAS-effector protein interactions derived using an intracellular antibody fragment
Published in Nature communications (09-08-2018)“…Targeting specific protein–protein interactions (PPIs) is an attractive concept for drug development, but hard to implement since intracellular antibodies do…”
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Combining experimental strategies for successful target deconvolution
Published in Drug discovery today (01-11-2020)“…•Target deconvolution can enhance pharmaceutical R&D productivity.•A combination of approaches is usually required for successful target deconvolution.•Target…”
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Activation of the Immune-Metabolic Receptor GPR84 Enhances Inflammation and Phagocytosis in Macrophages
Published in Frontiers in immunology (20-06-2018)“…GPR84 is a member of the metabolic G protein-coupled receptor family, and its expression has been described predominantly in immune cells. GPR84 activation is…”
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Augmentation of Creatine in the Heart
Published in Mini reviews in medicinal chemistry (01-01-2016)“…Creatine is a principle component of the creatine kinase (CK) phosphagen system common to all vertebrates. It is found in excitable cells, such as…”
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20 Years an Orphan: Is GPR84 a Plausible Medium-Chain Fatty Acid-Sensing Receptor?
Published in DNA and cell biology (01-11-2020)“…GPR84 is an inflammation-induced receptor highly expressed on immune cells, yet its endogenous ligand is still unknown. This makes any interpretation of its…”
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DLL4-Notch Signaling Mediates Tumor Resistance to Anti-VEGF Therapy In Vivo
Published in Cancer research (Chicago, Ill.) (15-09-2011)“…Resistance to VEGF inhibitors is emerging as a major clinical problem. Notch signaling has been implicated in tumor angiogenesis. Therefore, to investigate…”
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The BET inhibitor CPI203 promotes ex vivo expansion of cord blood long-term repopulating HSCs and megakaryocytes
Published in Blood (19-11-2020)“…Although cytokine-mediated expansion of human hematopoietic stem cells (HSCs) can result in high yields of hematopoietic progenitor cells, this generally…”
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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands
Published in Journal of medicinal chemistry (25-04-2013)“…The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided…”
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Chemical Proteomics and Phenotypic Profiling Identifies the Aryl Hydrocarbon Receptor as a Molecular Target of the Utrophin Modulator Ezutromid
Published in Angewandte Chemie International Edition (03-02-2020)“…Duchenne muscular dystrophy (DMD) is a fatal muscle‐wasting disease arising from mutations in the dystrophin gene. Upregulation of utrophin to compensate for…”
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Second-generation compound for the modulation of utrophin in the therapy of DMD
Published in Human molecular genetics (01-08-2015)“…Duchenne muscular dystrophy (DMD) is a lethal, X-linked muscle-wasting disease caused by lack of the cytoskeletal protein dystrophin. There is currently no…”
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Anthelmintic drug discovery: target identification, screening methods and the role of open science
Published in Beilstein journal of organic chemistry (02-06-2020)“…Helminths, including cestodes, nematodes and trematodes, are a huge global health burden, infecting hundreds of millions of people. In many cases, existing…”
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Simvastatin activates single skeletal RyR1 channels but exerts more complex regulation of the cardiac RyR2 isoform
Published in British journal of pharmacology (01-03-2018)“…Background and Purpose Statins are amongst the most widely prescribed drugs for those at risk of cardiovascular disease, lowering cholesterol levels by…”
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From arylamine N-acetyltransferase to folate-dependent acetyl CoA hydrolase: impact of folic acid on the activity of (HUMAN)NAT1 and its homologue (MOUSE)NAT2
Published in PloS one (13-05-2014)“…Acetyl Coenzyme A-dependent N-, O- and N,O-acetylation of aromatic amines and hydrazines by arylamine N-acetyltransferases is well characterised. Here, we…”
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An automated high-throughput system for phenotypic screening of chemical libraries on C. elegans and parasitic nematodes
Published in International journal for parasitology -- drugs and drug resistance (01-04-2018)“…Parasitic nematodes infect hundreds of millions of people and farmed livestock. Further, plant parasitic nematodes result in major crop damage. The pipeline of…”
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Synthesis of SMT022357 enantiomers and in vivo evaluation in a Duchenne muscular dystrophy mouse model
Published in Tetrahedron (10-01-2020)“…Following on from ezutromid, the first-in-class benzoxazole utrophin modulator that progressed to Phase 2 clinical trials for the treatment of Duchenne…”
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Identification and Preliminary Structure-Activity Relationship Studies of 1,5-Dihydrobenzo[ e ][1,4]oxazepin-2(3 H )-ones That Induce Differentiation of Acute Myeloid Leukemia Cells In Vitro
Published in Molecules (Basel, Switzerland) (02-11-2021)“…Acute myeloid leukemia (AML) is the most aggressive type of blood cancer, and there is a continued need for new treatments that are well tolerated and improve…”
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2,4-Diaminothieno[3,2-d]pyrimidines, a new class of anthelmintic with activity against adult and egg stages of whipworm
Published in PLoS neglected tropical diseases (11-07-2018)“…The human whipworm Trichuris trichiura is a parasite that infects around 500 million people globally, with consequences including damage to physical growth and…”
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Dihydrobenz[e][1,4]oxazepin-2(3H)-ones, a new anthelmintic chemotype immobilising whipworm and reducing infectivity in vivo
Published in PLoS neglected tropical diseases (01-02-2017)“…Trichuris trichiura is a human parasitic whipworm infecting around 500 million people globally, damaging the physical growth and educational performance of…”
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An Oxidation and Ring Contraction Approach to the Synthesis of (±)-1-Deoxynojirimycin and (±)-1-Deoxyaltronojirimycin
Published in Organic letters (01-01-2010)“…A reaction sequence involving the chemoselective olefinic oxidation of N(1)-benzyl-2,7-dihydro-1H-azepine with m-CPBA in the presence of HBF4 and BnOH followed…”
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