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A potential weakness of the
2019-09-26

A potential weakness of the present study is that it involved population controls rather than family controls, which are a better way of controlling the effects of population stratification (e.g. ethnic group differences in allele frequencies). On the other hand, general population samples do have t
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A An optimized BEI SEIscore
2019-09-26

(A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compare
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Sodium Danshensu clinical Resistance to SP is linked to poin
2019-09-26

Resistance to SP is linked to point mutations that accumulate at several sites in the dihydrofolate reductase (dhfr) and dihydropteroate synthase (dhps) Sodium Danshensu clinical of P. falciparum (Roper et al., 2003). These mutations have been identified in codons 16, 51, 59, 108, and 164 in the dh
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angiotensin ii Proteases as multifunctional enzymes play key
2019-09-26

Proteases, as multifunctional enzymes, play key roles in controlling a wide variety of cellular and extracellular processes in plants and animals, including protein degradation and processing, germination, complement activation, inflammation, responses to environmental stimuli, senescence and so on
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In addition to an action via P
2019-09-26

In addition to an action via P2Y receptors, extracellular UDP activates GPCRs for cysteinyl leukotrienes (CysLT1, CysLT2; Mellor et al., 2001, 2003). GPR17 has been reported to function as a receptor for cysteinyl leukotrienes and uracil nucleotides (Boda et al., 2011; Fumagalli et al., 2011; but se
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Alvocidib flavopiridol is a piperidine chromenone http
2019-09-26

Alvocidib (flavopiridol) is a piperidine-chromenone derivative (Fig. 6D) that is not FDA approved, but is in clinical trials for breast, endometrial, and several other cancers and hematological malignancies (Table 4) [[100], [101], [102], [103], [104]]. This drug targets CDK9 (IC50 = 3.2 nM) and CDK
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RO5185426 Since its inception ADEPT approach has been
2019-09-26

Since its inception, ADEPT approach has been widely reported by many groups using a variety of enzymes and prodrugs (see reviews) [12], [14]. Both mammalian and non-mammalian enzymes have been utilised. Of the mammalian variety, human β-glucuronidase in combination with many prodrugs [17], [18] and
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As a support chitosan presents interesting characteristics t
2019-09-26

As a support, chitosan presents interesting characteristics that reinforce its great potential for enzyme immobilization [18,19]. Firstly, it is produced from renewable natural sources in addition to being biodegradable and water insoluble [20,21]. Also, the main peculiarity in the chitosan structur
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The role of ETB clearing receptors has been
2019-09-26

The role of ETB clearing receptors has been studied in detail in endothelial cell–specific ETB knock-out mice. In these animals, clearance of an intravenous 4μ8C of labeled ET-1 was reduced significantly compared with wild-type controls. Importantly, functioning ETB were retained on all other cell
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The elastase induced injury model has
2019-09-26

The elastase-induced injury model has been shown to produce airspace enlargement, and increases in lung volume and compliance that are similar to those observed in human patients (Hantos et al., 2008, Hamakawa et al., 2011). Thus, this model, which has been used to study emphysema, should be adequat
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br Discussion The present study found cholinesterase activit
2019-09-25

Discussion The present study found cholinesterase activity in Saccostrea sp. to vary significantly among three tissue types (digestive gland, gills, adductor muscle) and to respond differentially to four toxicants, three of which were non-organophosphates. Furthermore, a comparison of enzyme acti
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Compounds and possessed relatively low clogP values and tend
2019-09-25

Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.
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In contrast to SQLE HMGCR
2019-09-25

In contrast to SQLE, HMGCR could be efficiently degraded in ML-291 kinase lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with our recen
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UBA belongs to the non canonical E
2019-09-25

UBA5 belongs to the non-canonical E1 enzymes that lack a defined Cys domain but have the active-site Cys within the adenylation domain [24]. Similar to other E1 enzymes, UBA5\'s adenylation domain comprises an eight-stranded beta sheet that is surrounded by helices [21]. Moreover, like the ancestral
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The present review also summarizes the efforts that
2019-09-25

The present review also summarizes the efforts that have been made to find new c-FMS inhibitors under clinical trial as given in the Table 1. These inhibitors may reduce the burdens of potency and side effects that have faced the scientists globally. ABT-869 41 was manufactured in Abbott laboratorie
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