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MMV s distinct mode of inhibition addresses key impediments
2022-01-13

MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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Neither E nor Z FPP synthase
2022-01-13

Neither E- nor Z-FPP synthase catalyzed the reaction between 8-THPOGPP and IPP. However, a mutant E-FPP synthase (Y81S) produced 12-THPOFPP from the substrates 8-THPOGPP and IPP, and wild-type E-FPP synthase catalyzed the reaction betweeen 8-AcOGPP and IPP producing 12-AcOFPP. Mutant E-FPP synthase
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Microglia after activation can show prominently pro
2022-01-13

Microglia after activation can show prominently pro-inflammatory but also anti-inflammatory characteristics [46]. Although the ageing process is not a pathological process, many of the age-associated changes resemble those observed under pathological conditions. An increase number of pro-inflammator
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In addition the interplay of
2022-01-13

In addition the interplay of membrane curvature induced tension at the fusion pore and LDN-212854 synthesis induced tension across the PM seems to be a worthwhile target for investigation. The roles of dynamin and myosin II and especially their spatial and temporal dynamics during activity warrant
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br Characterization of quantal exocytosis by amperometry A s
2022-01-13

Characterization of quantal exocytosis by amperometry A secretory vesicle experiences four phases during exocytosis: (i) cargo packaging & translocation, (ii) vesicle docking & priming; (iii) fusion pore formation; (iv) fusion pore expansion and cargo secretion (Fig. 1a). The release of monoamine
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br Conclusion In conclusion our results demonstrate that
2022-01-13

Conclusion In conclusion, our results demonstrate that incubation of both LAD and SCA rat coronary arteries rapidly increases the ETB receptor-mediated contraction as well as upregulation of ETB receptor protein levels. These findings may have important experimental implications in tissue bath ex
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Introduction Post translational modifications to the N
2022-01-13

Introduction Post-translational modifications to the N-terminal tails of the histone proteins play crucial roles in genome regulation [1]. These modifications (e.g. acetylation, methylation, phosphorylation) are deposited by so-called ‘writer’ enzymes and dynamically removed by the action of ‘erase
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br Prostaglandins meet Hippo The
2022-01-13

Prostaglandins meet Hippo The prostaglandins lie at the crossroads between inflammation, regeneration and tumorigenesis (Figure 3). Prostaglandins are synthesized from archidonic due to by Cox1 and Cox2 enzymes [40, 41] and in the gut, prostaglandin E2 (PGE2) protects against DSS-induced coliti
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br STAR Methods br Acknowledgments We thank the TCGA
2022-01-13

STAR★Methods Acknowledgments We thank the TCGA PanCanAtlas Analysis Working Group. This study was supported in part by grants from the NIH (CA175486 and CA209851 to H.L., CA217842 to G.B.M., and CCSG grant CA016672); a grant from the Cancer Prevention and Research Institute of Texas (RP140462
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br Disp Cleavage and Membrane Trafficking Knowledge
2022-01-13

Disp Cleavage and Membrane Trafficking Knowledge of how Disp is regulated in Shh-producing Oligomycin Complex to control ligand deployment has, until recently, remained limited. Early studies examining Disp function in Madin–Darby Canine Kidney (MDCK) cells and Drosophila tissue suggested that i
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Metallothioneins MTs that are intracellular proteins respons
2022-01-13

Metallothioneins (MTs) that are intracellular proteins responsible for the maintenance of metal homeostasis are involved in arsenic toxicity (Kita et al., 2006). Four major MT isoforms have been reported so far, MT1, MT2A, MT3 and MT4. The synthesis of MT1 and MT2A isoforms in mammal cells can be in
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hbv br Biochemical properties and post translational
2022-01-13

Biochemical properties and post-translational modification of GCAPs GCAPs are hydrophobic proteins that are likely permanently bound to their GC target under physiological conditions [5]. They interact with the photoreceptor GCs through the intracellular domains (reviewed in [17]). GCAP1 has been
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Although it has been observed
2022-01-13

Although it has been observed in numerous studies and by many investigators that intraplatelet cGMP elevation results in platelet inhibition, there are a few papers which proposed a platelet stimulatory role for cGMP when elevated in response to NO donors or PDE5 inhibitors in mouse and human platel
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br Membrane Fusion Requires Rab GTPases Tethers and SNAREs b
2022-01-13

Membrane Fusion Requires Rab-GTPases, Tethers, and SNAREs Regulation and Function of Rab5 Following endocytosis in metazoan cells, the Rab5-specific GEF Rabex5 binds to ubiquitinated cargo proteins, such as cell surface receptors or metabolite transporters, and subsequently activates Rab5 on e
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br Declaration of interest br Acknowledgments br This work
2022-01-13

Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A
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