Identification of a Potent Phosphoinositide 3‐Kinase Pan Inhibitor Displaying a Strategic Carboxylic Acid Group and Development of Its Prodrugs
Sign Up to like & getrecommendations! Published in 2017 at "Chemmedchem"
DOI: 10.1002/cmdc.201700340
Abstract: Activation of the phosphoinositide 3‐kinase (PI3K) pathway is a key signaling event in cancer, inflammation, and other proliferative diseases. PI3K inhibitors are already approved for some specific clinical indications, but their systemic on‐target toxicity limits… read more here.
Keywords: inhibitor; kinase; phosphoinositide kinase; pan ... See more keywords
Identification of a potent and selective gametocytocidal antimalarial agent from the stem barks of Lophira lanceolata.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103321
Abstract: Bioassay-guided fractionation of the organic extract obtained from stem barks of the African plant Lophira lanceolata has led to the isolation of seven biflavonoids, including the new α'-chlorolophirone E (5) and 5'-chlorolophirone D (6). Among… read more here.
Keywords: agent; potent selective; stem barks; lophira lanceolata ... See more keywords
Identification of a potent heme oxygenase-2 (HO-2) inhibitor by targeting the secondary hydrophobic pocket of the HO-2 western region.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.104310
Abstract: The enzymatic family of heme oxygenase (HO) is accountable for heme breakdown. Among the two isoforms characterized to date, HO-2 is poorly investigated due to the lack of potent HO-2 chemical modulators and the greater… read more here.
Keywords: heme oxygenase; identification potent; western region; potent heme ... See more keywords
Computational identification of potent inhibitors for Streptomycin 3″-adenylyltransferase of Serratia marcescens.
Sign Up to like & getrecommendations! Published in 2017 at "Microbial pathogenesis"
DOI: 10.1016/j.micpath.2016.12.015
Abstract: Serratia marcescens is an opportunistic pathogen responsible for the respiratory and urinary tract infections in humans. The antibiotic resistance mechanism of S. marcescens is mediated through aminoglycoside modification enzyme that transfer adenyl group from substrate to… read more here.
Keywords: streptomycin adenylyltransferase; serratia marcescens; structure; identification potent ... See more keywords
HTS by NMR for the Identification of Potent and Selective Inhibitors of Metalloenzymes.
Sign Up to like & getrecommendations! Published in 2018 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.7b00483
Abstract: We have recently proposed a novel drug discovery approach based on biophysical screening of focused positional scanning libraries in which each element of the library contained a common binding moiety for the given target or… read more here.
Keywords: potent selective; nmr identification; hts nmr; selective inhibitors ... See more keywords
Identification of Potent Bioassay Guided Terpenoid and Glycoside Root Fractions of Astragalus candolleanus against Clinically Significant Bacterial Strains
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Microbiology"
DOI: 10.1155/2022/4584799
Abstract: Antibiotic resistance represents one of the biggest challenges, and there is an urgent need for plant-based antimicrobial agents that enable managing this crisis effectively. In this work, we aimed to investigate the antibacterial activity of… read more here.
Keywords: root; identification potent; guided terpenoid; potent bioassay ... See more keywords
Identification of a potent NAFLD drug candidate for controlling T2DM-mediated inflammation and secondary damage in vitro and in vivo
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.943879
Abstract: Accumulation of glucose/sugar results in the formation of reactive di-carbonyl compounds such as MGO and GO that interact with several amino acids and proteins to form toxic advanced glycation end products (AGEs). Induction of AGEs… read more here.
Keywords: inflammation; identification potent; mgo age; age ... See more keywords