Prolyl-tRNA synthetase inhibition promotes cell death in SK-MEL-2Â cells through GCN2-ATF4 pathway activation.
Sign Up to like & getrecommendations! Published in 2017 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2017.01.045
Abstract: Protein translation is highly activated in cancer tissues through oncogenic mutations and amplifications, and this can support survival and aberrant proliferation. Therefore, blocking translation could be a promising way to block cancer progression. The process… read more here.
Keywords: death; prolyl trna; gcn2 atf4; atf4 pathway ... See more keywords
Structure-Guided Design of Halofuginone Derivatives as ATP-Aided Inhibitors Against Bacterial Prolyl-tRNA Synthetase.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01496
Abstract: Aminoacyl-tRNA synthetases (aaRSs) are promising antimicrobial targets due to their essential roles in protein translation, and expanding their inhibitory mechanisms will provide new opportunities for drug discovery. We report here that halofuginone (HF), an herb-derived… read more here.
Keywords: structure; guided design; prolyl trna; atp aided ... See more keywords
Late-Breaking Basic Science Abstracts From the American Heart Association’s Scientific Sessions 2017
Sign Up to like & getrecommendations! Published in 2017 at "Circulation Research"
DOI: 10.1161/res.0000000000000184
Abstract: ### 24036 ### Inhibition Of Prolyl-tRNA Synthetase As A Novel Mediator Of Cardiac Fibrosis Joon Seok Park1, Caroline H Lee1, Sungjin Yoon1, Jong Hyun Kim2, Sunghoon Kim2, Bongyong Lee1; 1Daewoong Pharmaceutical Co., Ltd., Yongin, Korea,… read more here.
Keywords: prs; fibrosis; prolyl trna; cardiac fibrosis ... See more keywords
Discovery and pharmacological characterization of a new class of prolyl-tRNA synthetase inhibitor for anti-fibrosis therapy
Sign Up to like & getrecommendations! Published in 2017 at "PLoS ONE"
DOI: 10.1371/journal.pone.0186587
Abstract: Scleroderma has clinical characteristics including skin and other tissue fibrosis, but there is an unmet need for anti-fibrotic therapy. Halofuginone (HF) is a well-known anti-fibrosis agent in preclinical and clinical studies which exerts its effect… read more here.
Keywords: new class; fibrosis; prolyl trna; trna synthetase ... See more keywords
Double drugging of prolyl-tRNA synthetase provides a new paradigm for anti-infective drug development
Sign Up to like & getrecommendations! Published in 2022 at "PLoS Pathogens"
DOI: 10.1371/journal.ppat.1010363
Abstract: Toxoplasmosis is caused by Toxoplasma gondii and in immunocompromised patients it may lead to seizures, encephalitis or death. The conserved enzyme prolyl-tRNA synthetase (PRS) is a validated druggable target in Toxoplasma gondii but the traditional… read more here.
Keywords: prolyl trna; drug development; drug; trna synthetase ... See more keywords
Control of fibrosis with enhanced safety via asymmetric inhibition of prolyl-tRNA synthetase 1.
Sign Up to like & getrecommendations! Published in 2023 at "EMBO molecular medicine"
DOI: 10.15252/emmm.202216940
Abstract: Prolyl-tRNA synthetase 1 (PARS1) has attracted much interest in controlling pathologic accumulation of collagen containing high amounts of proline in fibrotic diseases. However, there are concerns about its catalytic inhibition for potential adverse effects on… read more here.
Keywords: safety; trna synthetase; enhanced safety; prolyl trna ... See more keywords
Adenosine-Mimicking Derivatives of 3-Aminopyrazine-2-Carboxamide: Towards Inhibitors of Prolyl-tRNA Synthetase with Antimycobacterial Activity
Sign Up to like & getrecommendations! Published in 2022 at "Biomolecules"
DOI: 10.3390/biom12111561
Abstract: Multidrug-resistant tuberculosis (MDR-TB) poses a significant threat to mankind and as such earned its place on the WHO list of priority pathogens. New antimycobacterials with a mechanism of action different to currently used agents are… read more here.
Keywords: trna synthetase; prolyl trna; activity; adenosine mimicking ... See more keywords