Progress and challenges in aminoacyl-tRNA synthetase-based therapeutics

CS Francklyn, P Mullen - Journal of Biological Chemistry, 2019 - ASBMB
Aminoacyl-tRNA synthetases (ARSs) are universal enzymes that catalyze the attachment of
amino acids to the 3′ ends of their cognate tRNAs. The resulting aminoacylated tRNAs are …

Aminoacyl-tRNA synthetases as valuable targets for antimicrobial drug discovery

L Pang, SD Weeks, A Van Aerschot - International Journal of Molecular …, 2021 - mdpi.com
Aminoacyl-tRNA synthetases (aaRSs) catalyze the esterification of tRNA with a cognate
amino acid and are essential enzymes in all three kingdoms of life. Due to their important …

[HTML][HTML] Structural simplification: an efficient strategy in lead optimization

S Wang, G Dong, C Sheng - Acta Pharmaceutica Sinica B, 2019 - Elsevier
The trend toward designing large hydrophobic molecules for lead optimization is often
associated with poor drug-likeness and high attrition rates in drug discovery and …

Recent development of aminoacyl-tRNA synthetase inhibitors for human diseases: a future perspective

SH Kim, S Bae, M Song - Biomolecules, 2020 - mdpi.com
Aminoacyl-tRNA synthetases (ARSs) are essential enzymes that ligate amino acids to
tRNAs and translate the genetic code during protein synthesis. Their function in pathogen …

Recent development of leucyl-tRNA synthetase inhibitors as antimicrobial agents

P Zhang, S Ma - Medchemcomm, 2019 - pubs.rsc.org
Aminoacyl-tRNA synthetases (aaRSs) widely exist in organisms and mediate protein
synthesis. Inhibiting these synthetases can lead to the termination of protein synthesis and …

Discovery of novel tRNA-amino acid dual-site inhibitors against threonyl-tRNA synthetase by fragment-based target hopping

J Guo, B Chen, Y Yu, B Cheng, Y Cheng, Y Ju… - European Journal of …, 2020 - Elsevier
Threonyl-tRNA synthetase (ThrRS) is a key member of the aminoacyl-tRNA synthetase
(aaRS) family that plays essential roles in protein biosynthesis, and ThrRS inhibitors have …

Synthesis and structure-activity studies of novel anhydrohexitol-based leucyl-tRNA synthetase inhibitors

D De Ruysscher, L Pang, SMG Lenders… - European Journal of …, 2021 - Elsevier
Leucyl-tRNA synthetase (LeuRS) is a clinically validated target for the development of
antimicrobials. This enzyme catalyzes the formation of charged tRNA Leu molecules, an …

Structural basis of cysteine ligase MshC inhibition by cysteinyl-sulfonamides

L Pang, S Lenders, EM Osipov, SD Weeks… - International journal of …, 2022 - mdpi.com
Mycothiol (MSH), the major cellular thiol in Mycobacterium tuberculosis (Mtb), plays an
essential role in the resistance of Mtb to various antibiotics and oxidative stresses. MshC …

Synthesis and biochemical evaluation of noncyclic nucleotide exchange proteins directly activated by cAMP 1 (EPAC1) regulators

P Wang, U Luchowska-Stanska… - Journal of medicinal …, 2020 - ACS Publications
Exchange proteins directly activated by cAMP (EPAC) play a central role in various
biological functions, and activation of the EPAC1 protein has shown potential benefits for the …

Novel benzene sulfonamide-piperazine hybrid compounds: design, synthesis, antioxidant, enzyme inhibition activities and docking, ADME profiling studies

K Buran, Y İnan, AI Uba, G Zengin - Zeitschrift für Naturforschung C, 2024 - degruyter.com
Benzene sulfonamides are an important biological substituent for several activities. In this
study, hybridization of benzene sulfonamide with piperazine derivatives were investigated …