Histidine N([tau])-cyclized macrocycles as a new genre of polo-like kinase 1 polo-box domain-binding inhibitors
Abstract not provided
Hymel, David↗
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Search indexed NASA NTRS and DOE OSTI research on propulsion, heat transfer, battery materials and energy systems. Follow report and document links to the original sources.
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Serendipitous discovery of aryl boronic acids as [beta]-lactamase inhibitors
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Yang, Shu-Wei↗
Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa
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Fang, Tianan↗
Targeting the TS dimer interface in bifunctional Cryptosporidium hominis TS-DHFR from parasitic protozoa: Virtual screening identifies novel TS allosteric inhibitors
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99 GENERAL AND MISCELLANEOUS↗
Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp3 character and an exquisite selectivity profile
Not Available
Bigi-Botterill, Simone V.↗
Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model
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Barberis, Claude↗
Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious
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Calvo, Veronica↗
Development of BET inhibitors as potential treatments for cancer: A search for structural diversity
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Hill, Matthew D.↗
Structural and biophysical characterization of the Burkholderia pseudomallei IspF inhibitor L-trypto
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Blain, Joy M.↗
Development of BRD4 inhibitors as anti-inflammatory agents and antidotes for arsenicals
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Yatchanga, Marina Fosso↗
Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors
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Caldwell, Timothy M.↗
Tetrazole-based inhibitors of the bacterial enzyme N -succinyl- L,L -2,6-diaminopimelic acid desuccinylase as potential antibiotics
Based on a hit from a high-throughput screen, a series of phenyltetrazole amides was synthesized and assayed for inhibitory potency against DapE from Haemophilus influenzae (HiDapE). The inhibitory potency was modest but confirmed, with the most potent analog containing an aminothiazole moiety displaying an IC 50 = 50.2 ± 5.0 μM. Finally, docking reveals a potential binding mode wherein the amide carbonyl bridges both zinc atoms in the active site, and the tetrazole forms key hydrogen bonds with Arg330.
60 APPLIED LIFE SCIENCES↗
Structure–activity relationship study of small-molecule inhibitor of Atg12-Atg3 protein–protein interaction
Not Available
Skach, Krystof (ORCID:0000000275586961)↗
The Plasma Membrane as a Competitive Inhibitor and Positive Allosteric Modulator of KRas4B Signaling
Not Available
59 BASIC BIOLOGICAL SCIENCES↗
Development of substituted benzimidazoles as inhibitors of human aldehyde dehydrogenase 1A isoenzymes
Not provided.
Biochemistry & Molecular Biology↗