ATP inhib News - LARVOL Sigma

|||||||||| Journal: Dehydrocurvularin is a potent antineoplastic agent irreversibly blocking ATP-citrate lyase: evidence from chemoproteomics. (Pubmed Central) - Apr 16, 2019
Natural-product macrolide 10,11-dehydrocurvularin (DCV) was revealed to be a potent irreversible inhibitor of ATP-citrate lyase (ACLY) via classical chemoproteomic profiling, which mechanistically illuminates the anti-cancer mode of action of DCV and its analogues.

|||||||||| Journal: The inhibitors of soluble adenylate cyclase 2-OHE, KH7, and bithionol compromise mitochondrial ATP production by distinct mechanisms. (Pubmed Central) - Apr 7, 2019
These findings were corroborated by investigating energy metabolism in acute brain slices from mice. Since all three sAC inhibitors are shown to curb mitochondrial ATP production and affect energy metabolism, caution should be exercised when employed to study the physiological roles of sAC or for validating sAC as a drug target.

|||||||||| metformin / generics
Journal: Mitochondria-targeted drugs stimulate mitophagy and abrogate colon cancer cell proliferation. (Pubmed Central) - Apr 7, 2019
...3-Carboxyl proxyl nitroxide (Mito-CP) and Mito-Metformin, two mitochondria-targeted compounds, depleted intracellular ATP levels and persistently inhibited ATP-linked oxygen consumption in both KRAS WT and KRAS variant-containing colon cancer cells and had only limited effects on nontransformed intestinal epithelial cells...This is the first demonstration that drugs selectively targeting mitochondria induce mitophagy in cancer cells. Targeting bioenergetic metabolism with mitochondria-targeted drugs to stimulate mitophagy provides an attractive approach for therapeutic intervention in KRAS wild-type and overactive mutant expressing colon cancer.

|||||||||| Journal: Structure of the Î³-Îµ complex of cyanobacterial F-ATPase reveals a suppression mechanism of theÂ Î³ subunit on ATP-hydrolysis in phototrophs. (Pubmed Central) - Apr 5, 2019
In addition, we found that truncating the Î²-hairpin insertion structure resulted in a marked impairment of the interaction with theÂ Îµ subunit, which binds to the opposite side of the Î³ subunit from the Î²-hairpin structure. Combined with structural analyses, our work provides experimental evidence supporting the molecular principle of how the insertion region of the Î³ subunit suppresses F rotation during ATP hydrolysis.

|||||||||| Journal: Dichloroacetate, an inhibitor of pyruvate dehydrogenase kinases, inhibits platelet aggregation and arterial thrombosis. (Pubmed Central) - Apr 5, 2019
Wild-type mice pretreated with DCA were less susceptible to thrombosis in the FeCl-induced carotid and laser injury-induced mesenteric artery thrombosis models (P < .05 vs vehicle control), without altering hemostasis. Targeting metabolic plasticity with DCA may be explored as a novel strategy to inhibit platelet function.

|||||||||| Journal: ATP-competitive DNA gyrase and topoisomerase IV inhibitors as antibacterial agents. (Pubmed Central) - Apr 5, 2019
Other common issues, such as low solubility, high protein binding, development of off-target resistance (e.g., via bacterial efflux pumps), are related to the structures of the inhibitors themselves, which is thus a main focus of design strategies. With some now in early clinical development, there is reasonable expectation that novel ATP-competitive inhibitors of GyrB/ParE(GrlB) will reach the market in the near future.

|||||||||| doxorubicin hydrochloride / generics
Journal: The P-glycoprotein inhibitor diltiazem-like 8-(4-chlorophenyl)-5-methyl-8-[(2Z)-pent-2-en-1-yloxy]-8H-[1,2,4]oxadiazolo[3,4-c][1,4]thiazin-3-one inhibits esterase activity and H3 histone acetylation. (Pubmed Central) - Mar 28, 2019
...The compound 8-(4-chlorophenyl)-5-methyl-8-[(2Z)-pent-2-en-1-yloxy]-8H-[1,2,4]oxadiazolo[3,4-c][1,4]thiazin-3-one namely 2c, is structurally related to the myocardial-calcium-channel-modulator diltiazem and is considered one of the most efficient P-glycoprotein inhibitors, able to induce apoptosis at low concentrations of doxorubicin in multidrug resistant ovarian cells...2c also inhibits cell esterase activity, acetylcholine esterase activity inÂ vitro and cell histone H3 acetylation according to its structural homology with some known HAT inhibitors. The results obtained provide new knowledge on the biological activities of 2c and represent useful information when it is used as an inhibitor of drug resistance.

|||||||||| Journal: Grifolic acid induces GH3 adenoma cell death by inhibiting ATP production through a GPR120-independent mechanism. (Pubmed Central) - Mar 27, 2019
The results obtained provide new knowledge on the biological activities of 2c and represent useful information when it is used as an inhibitor of drug resistance. Grifolic acid induces GH3 cell death by decreasing MMP and inhibiting ATP production, which may be due to the inhibition of NADH production through a GPR120-independent mechanism.

|||||||||| Nexletol (bempedoic acid) / Esperion Therap, Otsuka
Clinical, Journal: Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol. (Pubmed Central) - Mar 27, 2019
P3
In this 52-week trial, bempedoic acid added to maximally tolerated statin therapy did not lead to a higher incidence of overall adverse events than placebo and led to significantly lower LDL cholesterol levels. (Funded by Esperion Therapeutics; CLEAR Harmony ClinicalTrials.gov number, NCT02666664.).



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