Targeting autophagy-related protein kinases for potential therapeutic purpose
Publication date: Available online 18 October 2019Source: Acta Pharmaceutica Sinica BAuthor(s): Honggang Xiang, Jifa Zhang, Congcong Lin, Lan Zhang, Bo Liu, Liang OuyangAbstractAutophagy, defined as a scavenging process of protein aggregates and damaged organelles mediated by lysosomes, plays a significant role in the quality control of macromolecules and organelles. Since protein kinases are integral to the autophagy process, it is critically important to understand the role of kinases in autophagic regulation. At present, intervention of autophagic processes by small-molecule modulators targeting specific kinases has becoming a reasonable and prevalent strategy for treating several varieties of human disease, especially cancer. In this review, we describe the role of some autophagy-related kinase targets and kinase-mediated phosphorylation mechanisms in autophagy regulation. We also summarize the small-molecule kinase inhibitors/activators of these targets, highlighting the opportunities of these new therapeutic agents.Graphical abstractThis review elaborates in detail the role of some autophagy-related kinase targets and phosphorylation in autophagy regulation, and further summarizes the application of small-molecule kinase inhibitors/activators for autophagy inhibition and induction. Understanding how these autophagy-related kinases regulate autophagy machinery is critical for the potential therapeutic application of autophagy.
What impact do antibiotic-related changes of the gut microbiome have on efficacy of immune-checkpoint inhibitors?Annals of Oncology
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Men with early stage prostate cancer did not show benefits from a vegetable-rich diet.
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Publication date: Available online 19 January 2020Source: Food Research InternationalAuthor(s): Caiyu Lei, Xiangyi Tang, He Li, Hualei Chen, Shujuan YuAbstractThe grape seed extract (GSE) hybridized with medium-chain saturated fatty acids (decanoic acid) exhibited higher lipophilicity, antioxidant activity, and anti-proliferative activity than its parents. The chemical structures of individual hybridized GSE derivatives were identified as 3'-O-decanoyl catechin, 3′-O-decanoyl epicatechin, 3', 5'-2-O-decanoyl epigallocatechin, and 3', 4', 3'', 5''-4-O-decanoyl epicatechin gallate by HPLC-MS2 and 1H and 13C NMR. For gr...
Women whose periods stop before the age of 40 are at greater risk of diabetes, heart disease, strokes, asthma and breast cancer, the study found. The UK menopause average is 51.
Publication date: 15 April 2020Source: Journal of Molecular Structure, Volume 1206Author(s): Imre Huber, Zsuzsanna Rozmer, Zoltán Gyöngyi, Ferenc Budán, Péter Horváth, Eszter Kiss, Pál PerjésiAbstractThe chemical susceptibility of the β-diketone linker between the two aromatic rings in the structure of curcumin to hydrolysis and metabolism has made it crucial to investigate structurally modified analogs of curcumin without such shortcomings. The synthesis of twenty cyclic C5-curcuminoids is described in this study in order to gain more insight into their anticancer struct...