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Substrate affinity and specificity can be enhanced by
2022-03-23
Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of Voreloxin bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognition of short
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br Conclusions br Acknowledgments This work was
2022-03-23
Conclusions Acknowledgments This work was financially supported partly by Shanghai Pujiang Talent Project (No.: 08PJ14017), the National Natural Science Foundation of China (Nos.: 20771029 and 91013001) and Shanghai Leading Academic Discipline Project (No. B108). Soluble guanylate cyclase (
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Main Text There are over
2022-03-23
Main Text There are over 200 small GTPases that play critical roles in diverse fundamental cellular processes such as signal transduction, (±)-Bay K 8644 dynamics, and intracellular trafficking. Most of the GTPases act as switch-like molecules by cycling between the guanosine triphosphate (GTP)-bo
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br Conclusion and future perspectives The nicotinic acid
2022-03-23
Conclusion and future perspectives The nicotinic C598-0466 mg receptor GPR109A and its close relatives GPR109B and GPR81 are primarily expressed in adipocytes and are coupled to Gi-type G proteins. Recently, the ketone body β-hydroxy-butyrate, the β-oxidation intermediate 3-hydroxy octanoic acid
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Finally a potentially effective therapeutic approach
2022-03-23
Finally, a potentially effective therapeutic approach is to target the LDH enzymes that mediate bidirectional conversion of pyruvate into lactate. In particular, because LDHA is the predominant isoform expressed in glycolytic tumours, an array of LDHA-targeting compounds have been proposed and valid
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It was noted elsewhere that several
2022-03-22
It was noted elsewhere that several of the variants (i.e., Indel19 and SNP63) that make up the risk haplotypes had unusually large differences in allele frequencies between Africans and non-Africans, as compared with a set of likely neutral loci (Fullerton et al. 2002). This finding was interpreted
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Levofloxacin Given that inactivation of GLO by
2022-03-22
Given that inactivation of GLO1 by 4BAB is an active site directed mechanism, as the transition state analogue CHG protects GLO1 against inactivation by 4BAB (Figs. 2D and S6b), we next set out to determine the amino Levofloxacin that is covalently modified by 4BAB. From the X-ray crystallographic
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N Cadherin facilitated gap junction formation between embryo
2022-03-22
N-Cadherin facilitated gap junction formation between embryonic lens 4-Hydroxytamoxifen by stabilizing membrane appositions (Frenzel and Johnson, 1996). Cx43 has been found to be delivered to N-Cadherin-positive membrane HeLa cells (Shaw et al., 2007), and N-Cadherin determine the localization of C
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The highest metabolic stability observed for compound k
2022-03-22
The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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Analysis of published albumin X
2022-03-22
Analysis of published albumin X-ray structures had suggested that an allosteric link may exist, but could not establish whether Zn2+ prevented FFA binding or vice versa. This question was answered through competition experiments monitored by isothermal titration calorimetry (ITC; Fig. 3) for BSA [55
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The G protein coupled receptor GPR also called FFAR
2022-03-22
The G protein-coupled receptor, GPR40 (also called FFAR1) responds to medium and long chain unsaturated fatty acids, resulting in increase of insulin secretion during elevated glucose levels. The glucose dependency of insulin secretion makes this receptor a very good target for developing therapies
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Ferulenol The first FPR ligand described is
2022-03-22
The first FPR1 ligand described is the fMLF peptide, which binds with high affinity (in the nM range) to and activates FPR1. Formylated peptides derived from Listeria monocytogenes also selectively activate FPR1 [10] (Table 1). Formylation of peptides also occurs in mitochondria. Thus, the release o
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br Disp Mediated Hh Membrane Recycling
2022-03-21
Disp-Mediated Hh Membrane Recycling Due to its cholesterol modification, Drosophila Hh enriches on sphingolipid-rich apical membranes of polarized epithelial A-1210477 mg 33., 38., 39.. Genetic studies examining Hh release from wing imaginal disc epithelia suggest that Hh must be endocytosed fro
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Carbon monoxide another key product
2022-03-21
Carbon monoxide, another key product from the breakdown of heme by HO-1, also plays an important role in the vasculature. Like NO, CO is endogenously derived from the endothelium [68] and can weakly activate sGC by binding to its heme moiety [69]. CO was found to have vasodepressor activity in rats
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It has been known for some time
2022-03-21
It has been known for some time that an oral salt load given to mammals induces a much greater natriuresis than the intravenous administration of an equivalent amount of saline (Carey et al., 1976, Singer et al., 1998). In addition, oral administration of salt to rats has been reported to augmented
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