Search Results - "Mamo, Mulugeta"
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Yield stability and adaptability of lowland sorghum (Sorghum bicolor (L.) Moench) in moisture-deficit areas of Northeast Ethiopia
Published in Cogent food & agriculture (2020)“…Genotype-environment interaction (GxE) is a common phenomenon in sorghum. The effect of GxE can be reduced by identifying stable genotypes across environments…”
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Assessment of type II diabetes mellitus drug therapy in diabetes clinic of a tertiary care teaching hospital in Addis Ababa
Published in Archives of pharmacy practice (01-07-2014)“…Prevalence of type II diabetes mellitus(T2DM) is substantially increasing in Ethiopia but there are no studies on its drug therapy. To assess drug therapy for…”
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Facilitating unambiguous NMR assignments and enabling higher probe density through selective labeling of all methyl containing amino acids
Published in Journal of biomolecular NMR (01-05-2016)“…The deuteration of proteins and selective labeling of side chain methyl groups has greatly enhanced the molecular weight range of proteins and protein…”
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Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic
Published in Journal of medicinal chemistry (12-03-2020)“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
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Rationally Designed PI3Kα Mutants to Mimic ATR and Their Use to Understand Binding Specificity of ATR Inhibitors
Published in Journal of molecular biology (02-06-2017)“…ATR, a protein kinase in the PIKK family, plays a critical role in the cell DNA-damage response and is an attractive anticancer drug target. Several potent and…”
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Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based Drug Design
Published in Journal of medicinal chemistry (27-12-2018)“…A HTS campaign identified compound 1, an excellent hit-like molecule to initiate medicinal chemistry efforts to optimize a dual ROCK1 and ROCK2 inhibitor…”
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Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity
Published in Journal of medicinal chemistry (26-04-2018)“…In the preceding manuscript [Moreau et al. 2018, 10.1021/acs.jmedchem.7b01691 ] we described a successful fragment-based lead discovery (FBLD) strategy for…”
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Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria
Published in Journal of medicinal chemistry (26-04-2018)“…The discovery and development of new antibiotics capable of curing infections due to multidrug-resistant and pandrug-resistant Gram-negative bacteria are a…”
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Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers
Published in Journal of medicinal chemistry (22-06-2017)“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
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Cryptosporidium PI(4)K inhibitor EDI048 is a gut-restricted parasiticidal agent to treat paediatric enteric cryptosporidiosis
Published in Nature microbiology (08-10-2024)“…Diarrhoeal disease caused by Cryptosporidium is a major cause of morbidity and mortality in young and malnourished children from low- and middle-income…”
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Design of Aminobenzothiazole Inhibitors of Rho Kinases 1 and 2 by Using Protein Kinase A as a Structure Surrogate
Published in Chembiochem : a European journal of chemical biology (16-03-2018)“…We describe the design, synthesis, and structure–activity relationships (SARs) of a series of 2‐aminobenzothiazole inhibitors of Rho kinases (ROCKs) 1 and 2,…”
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Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo
Published in Molecular cancer therapeutics (01-06-2005)“…The Akt kinases are central nodes in signal transduction pathways that are important for cellular transformation and tumor progression. We report the…”
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Design and synthesis of pyridine–pyrazolopyridine-based inhibitors of protein kinase B/Akt
Published in Bioorganic & medicinal chemistry (15-03-2007)“…We have designed and synthesized a series of potent pyridine–pyrazolopyridine-based inhibitors of protein kinase B/Akt. The best compound in this series showed…”
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Syntheses of Potent, Selective, and Orally Bioavailable Indazole-Pyridine Series of Protein Kinase B/Akt Inhibitors with Reduced Hypotension
Published in Journal of medicinal chemistry (28-06-2007)“…Compound 7 was identified as a potent (IC50 = 14 nM), selective, and orally bioavailable (F = 70% in mouse) inhibitor of protein kinase B/Akt. While promising…”
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P1-Substituted Symmetry-Based Human Immunodeficiency Virus Protease Inhibitors with Potent Antiviral Activity against Drug-Resistant Viruses
Published in Journal of medicinal chemistry (27-10-2011)“…Because there is currently no cure for HIV infection, patients must remain on long-term drug therapy, leading to concerns over potential drug side effects and…”
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2-Pyridyl P1′-Substituted Symmetry-Based Human Immunodeficiency Virus Protease Inhibitors (A-792611 and A-790742) with Potential for Convenient Dosing and Reduced Side Effects
Published in Journal of medicinal chemistry (23-04-2009)“…A series of symmetry-based HIV protease inhibitors was designed and synthesized. Modification of the core regiochemistry and stereochemistry significantly…”
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