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Derivatives of M that possess either an alkyne or an
2024-01-09
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these Venlafaxine to maintain 5-HTR antagonist properties as (+)-M100907 was demonstra
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At present drugs that specifically
2024-01-09
At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi
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br Materials and Methods br Author Contributions br
2024-01-09
Materials and Methods Author Contributions Conflicts of Interest Acknowledgments This study was funded by the NIH Common Fund (UH2TR000943) through the Office of Strategic Coordination/Office of the NIH Director, an NCI/NIH grant (1R21CA199050), the MD Anderson Cancer Center support gran
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br Increased blood ATX and
2024-01-09
Increased blood ATX and LPA in liver fibrosis Although previous in vitro findings have suggested a link between LPA and liver fibrosis in vivo, whether LPA plays a primary role in the pathogenesis of liver fibrosis has remained uncertain. No phenotypic changes in livers of LPA receptor-deficient
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Autophagy is finalized through the coordinated positioning
2024-01-09
Autophagy is finalized through the coordinated positioning and fusion of autophagosomes with lysosomes, during which an array of common and specific membrane traffic-associated proteins is mobilized. Among these proteins, small GTPases, like Rab7, Rab34, or Arl8, and their UNC 0631 synthesis protei
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Pyrimidine is the important pharmacology
2024-01-09
Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the ezh2 inhibitor core as
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Chromatin proteins play important roles in gene expression a
2024-01-09
Chromatin proteins play important roles in gene expression and DNA repair. The importance of chromatin composition on gene expression is exemplified by X-inactivation, where one of the two X chromosomes in female mammalian Clonidine HCl is transcriptionally silenced by heterochromatin , , , . In th
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Limitations of this study include the use of HL cardiomyocyt
2024-01-09
Limitations of this study include the use of HL-1 cardiomyocytes, which show different characteristics than primary cardiomyocytes [56]. Furthermore, sustained TAC in Ampkα1-deficient mice did not favorably influence cardiac function [33]. It must be kept in mind that global Ampkα1-deficiency may af
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There are increasing repeated reports of amphotericin
2024-01-09
There are increasing repeated reports of amphotericin B-resistance in pathogenic fungi including Candida spp. [35], [36]. Nolte et al. characterized some fluconazole and amphotericin B-resistant Candida albicans isolates from leukemia patients [37]. Fan-Havard et al. (1991) have shown multi-antifung
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Rizatriptan Benzoate Recently two distinct small molecule in
2024-01-09
Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Rizatriptan Benzoate with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces
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br Functions essentially consisting in
2024-01-08
Functions essentially consisting in transport of substrates across plasma membranes Direct activation of neurotransmitter transporters elicits responses in neurons As previously mentioned (Section 2.1), nerve terminals handling classical transmitters possess transporters able to (re)capture se
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Among the enzymes involved in
2024-01-08
Among the enzymes involved in adenosine metabolism, adenosine kinase plays an important role in regulating formation and release of endogenous adenosine in cardiomyocytes as well as vascular endothelial cells Decking et al., 1997, Kowaluk et al., 1998, Smolenski et al., 1994. Inhibition of adenosine
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Princen Panier specifically address the
2024-01-08
Princen, 2012, Panier, 2013 specifically address the issue of ACE using the commercial database AMADEUS. However, both studies focus only on corporate leverage and the ACE in Belgium. Due to the lack of a counterfactual, these authors consider firms in other European countries, e.g., France, as a co
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The small fishers with little or no quota who
2024-01-08
The small fishers with little or no quota who remained relied on quota leasing arrangements to continue their fishing operations. Such arrangements had relatively high transaction costs and by early 2000 it appeared that the demise of the small fisher was imminent [2]. The introduction in 2001 of t
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LO is a soluble kDa enzyme composed
2024-01-08
5-LO is a soluble 78 kDa enzyme, composed of an α-helix-rich catalytic domain and a regulatory β-sheet-rich C2-like domain. Depending on the cell type, 5-LO may be located in the cytosol, in the nucleoplasm, or in both compartments (Werz, 2002). Upon cell stimulation by agents that elevate intracell
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