Tubulin colchicine site binding agent LL01 displays potent antitumor efficiency both in vitro and in vivo with suitable drug-like properties
Sign Up to like & getrecommendations! Published in 2019 at "Investigational New Drugs"
DOI: 10.1007/s10637-019-00753-z
Abstract: Through rational drug design, we previously identified an indenoprazole derivative, 2-(6-ethoxy-3-(3-ethoxyphenylamino)-1-methyl-1,4-dihydroindeno[1,2- c ]pyrazol-7-yloxy)acetamide (LL01), as a potent tubulin polymerization inhibitor targeting the tubulin colchicine binding site. In this study, we further demonstrated that LL01 was… read more here.
Keywords: site binding; drug; ll01; tubulin colchicine ... See more keywords
Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00403
Abstract: The dysregulated Hippo pathway and, consequently, hyperactivity of the transcriptional YAP/TAZ-TEAD complexes is associated with diseases such as cancer. Prevention of YAP/TAZ-TEAD triggered gene transcription is an attractive strategy for therapeutic intervention. The deeply buried… read more here.
Keywords: msc 4106; site; binding fragment; optimization ... See more keywords
Quantifying cooperative multisite binding in the hub protein LC8 through Bayesian inference
Sign Up to like & getrecommendations! Published in 2022 at "PLOS Computational Biology"
DOI: 10.1101/2022.06.29.498022
Abstract: Multistep protein-protein interactions underlie most biological processes, but their characterization through methods such as isothermal titration calorimetry (ITC) is largely confined to simple models that provide little information on the intermediate, individual steps. In this… read more here.
Keywords: itc; protein lc8; hub protein; protein ... See more keywords