Derivatization of Microcystins Can Increase Target Inhibition while Reducing Cellular Uptake
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Natural Products"
DOI: 10.1021/acs.jnatprod.4c00688
Abstract: Microcystins, a large family of nonribosomal cyclic heptapeptides known for their hepatotoxicity, are among the best-studied cyanobacterial toxins. Recently, they have been discussed as leads for the development of anticancer drug substances. Their main mode-of-action… read more here.
Keywords: phosphatase inhibition; inhibition; target inhibition; transportability ... See more keywords
Abstract 4031: In vivo studies demonstrate differences in target inhibition and anticancer efficacy between NXP900 and dasatinib in ovarian clear cell carcinoma model
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-4031
Abstract: Background: NXP900 (formerly known as eCF506) is a novel SRC/YES1 family kinase (SFK) inhibitor that locks SRC into its native closed conformation (= type 1.5), thereby inhibiting both kinase activity and complex formation with protein… read more here.
Keywords: cell; inhibition; efficacy; model ... See more keywords
USP13: Multiple Functions and Target Inhibition
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Cell and Developmental Biology"
DOI: 10.3389/fcell.2022.875124
Abstract: As a deubiquitination (DUB) enzyme, ubiquitin-specific protease 13 (USP13) is involved in a myriad of cellular processes, such as mitochondrial energy metabolism, autophagy, DNA damage response, and endoplasmic reticulum-associated degradation (ERAD), by regulating the deubiquitination… read more here.
Keywords: usp13 multiple; development; biology; functions target ... See more keywords
USP30: Structure, Emerging Physiological Role, and Target Inhibition
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.851654
Abstract: Ubiquitin-specific protease 30 (USP30) is a deubiquitinating enzyme (DUB) belonging to the USP subfamily, which was found localized in the mitochondrial outer membrane and peroxisomes owing to its unique transmembrane domain. Structural study revealed that… read more here.
Keywords: emerging physiological; structure; role; physiological role ... See more keywords