EMBO Mol Med 2014 02 10;6(2):169-82. Epub 2014 Jan 10.
Department of Radiology, Oncology and Pathology, Sapienza University of Rome, Rome, Italy.
Bioorg Med Chem 2021 Feb 14;35:116073. Epub 2021 Feb 14.
Jiangsu Key Laboratory of Pesticide Science, College of Sciences, Nanjing Agricultural University, Nanjing 210095, China. Electronic address:
Streptochlorin is a small molecule of indole alkaloid isolated from marine Streptomyces sp., it is a promising lead compound due to its potent bioactivity in preventing many phytopathogens in our previous study, but further structural modifications are required to improve its antifungal activity. Our work in this paper focused on the replacement of oxazole ring in streptochlorin with the imidazole ring, to discover novel analogues. Read More
Antimicrob Agents Chemother 2021 Feb 8. Epub 2021 Feb 8.
Center for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA
Global infections by non-tuberculous mycobacteria (NTM) are steadily rising. New drugs are needed to treat NTM infections, but the NTM drug pipeline remains poorly populated and focused on repurposing or reformulating approved antibiotics. We sought to accelerate NTM drug discovery by testing advanced compounds with established activity against 3-aminomethyl 4-halogen benzoxaboroles, a novel class of leucyl-tRNA synthetase inhibitors, were recently discovered as active against Here, we report that the benzoxaborole EC/11770 is not only a potent anti-tubercular agent but is active against the and complexes. Read More
Nat Commun 2021 01 4;12(1):45. Epub 2021 Jan 4.
Department of Biochemistry and Molecular Pharmacology, UMass Medical School, 364 Plantation Street, Worcester, MA, 01605, USA.
Citrullination is a post-translational modification (PTM) of arginine that is crucial for several physiological processes, including gene regulation and neutrophil extracellular trap formation. Despite recent advances, studies of protein citrullination remain challenging due to the difficulty of accessing proteins homogeneously citrullinated at a specific site. Herein, we report a technology that enables the site-specific incorporation of citrulline (Cit) into proteins in mammalian cells. Read More
Am J Med Genet A 2021 03 10;185(3):866-870. Epub 2020 Dec 10.
Center for Medical Genetics, Keio University School of Medicine, Tokyo, Japan.
Infantile liver failure syndrome type 1 (ILFS1) is a recently recognized autosomal recessive disorder caused by deleterious mutations in the leucyl-tRNA synthetase 1 gene (LARS1). The LARS1 enzyme is responsible for incorporation of the amino acid leucine during protein polypeptide synthesis. Individuals with LARS1 mutations typically show liver failure from infancy to early childhood during periods of illness or other physiological stress. Read More
Eur J Med Chem 2021 Feb 16;211:113021. Epub 2020 Nov 16.
Medicinal Chemistry, Rega Institute for Medical Research, Department of Pharmaceutical and Pharmacological Sciences, KU Leuven, Herestraat 49 - Box 1030, 3000, Leuven, Belgium. Electronic address:
Leucyl-tRNA synthetase (LeuRS) is a clinically validated target for the development of antimicrobials. This enzyme catalyzes the formation of charged tRNA molecules, an essential substrate for protein translation. In the first step of catalysis LeuRS activates leucine using ATP, forming a leucyl-adenylate intermediate. Read More