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CPG a metalloenzyme derived from sp was the elected enzyme
2019-09-23

CPG2, a metalloenzyme derived from sp., was the elected enzyme for the first pilot-scale clinical trial of ADEPT. This enzyme has no mammalian homologue and activates glutamic silybin prodrug derivatives of several nitrogen mustards alkylating agents., , , , , A bond cleavable by CPG2 is essentia
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We have previously reported the characterization of A a nove
2019-09-23

We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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br Results br Discussion The nitric oxide cyclic guanosine m
2019-09-23

Results Discussion The nitric oxide-cyclic guanosine monophosphate pathway plays an important role in normal EF, and oral PDE-5Is were developed in the late 90s after the discovery that ED occurs when there is a problem with this pathway. Since then, several PDF-5Is with different pharmacokine
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Not all of the biological activities exhibited by progestoge
2019-09-23

Not all of the biological activities exhibited by progestogens (Table 1) are mediated via binding to SRs. For example, the anti-estrogenic action of progestogens in the doxorubicin hydrochloride and is due to the progestogen-bound PR suppressing ER gene expression, and consequently the ability of t
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The ADME profile of AAT was very promising with high
2019-09-23

The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in .
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Enhanced responses to varying concentrations
2019-09-23

Enhanced responses to varying concentrations of bronchoconstrictors, such as MCh, and airway obstruction are characteristic of metforman and common to other clinical states, including chronic obstructive pulmonary disease, lung transplantation, and infection- or chemical agent-induced airway inflam
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br E E backside interaction The E possesses an important
2019-09-23

E3–E2 backside interaction The E2 possesses an important regulatory interface which is termed its backside as it is opposite to the catalytic cleft that bears the active-site cysteine forming the thioester with SUMOD. This backside site interacts noncovalently with a scaffold SUMOB and was origin
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The crystal structure of full length
2019-09-21

The crystal structure of full-length CHK is still unsolved. However, the close homology between CHK and Csk suggests that these kinases share a similar structure. Therefore, the engagement of the CHK SH2–kinase linker with the αC-helix could control the activity of the CHK kinase domain. Sequence al
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(+)-MK 801 br Introduction Breast cancer is the most common
2019-09-21

Introduction Breast cancer is the most common cancer in women and one of the leading causes of death worldwide. Estrogen receptor alpha (ERα, “wild-type” estrogen receptor), encoded by the estrogen receptor1 (ESR1) gene, is expressed in approximately 70% of all breast cancers. Hormonal therapy ha
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We then analyzed Ki proliferation index as a categorical
2019-09-21

We then analyzed Ki-67 proliferation index as a categorical variable by using 15%, essentially the median Ki-67 value in the entire study group (see above), to delineate low and high proliferation subgroups. By Fisher\'s exact test, both the type 1 versus non-type 1 EWS-FLI1 comparison (P = 0.047; T
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The glycolytic pathway is a catabolic route
2019-09-21

The glycolytic pathway is a catabolic route that ends with the synthesis of pyruvate (Pyr). In Arabidopsis embryos, the conversion of phosphoenolpyruvate (PEP) to Pyr, catalyzed by pyruvate kinase (PK), is mainly located in the plastids [10], [11]. The preceding reaction is catalyzed by enolase (ENO
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For statistical analysis the Statistical
2019-09-21

For statistical analysis, the Statistical Package for Social Sciences (SPSS) was used (version 21.0; SPSSInc., Chicago, IL). Chi-square (x2) exact test was used for the comparison of categorical data, whereas Wilcoxon and Mann–Whitney U tests were used for the analysis of nonparametric variables bas
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The human MARCH family comprises
2019-09-21

The human MARCH family comprises eleven members (termed MARCH-1 to 11), of which nine are transmembrane proteins. In this review, we focus on the role of the membrane-spanning MARCH proteins and how their transmembrane regions can mediate interactions with their target proteins. Therefore, the cytos
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br Anti inflammatory effects of MTX In addition to
2019-09-21

Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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DDR expression is upregulated in the glomeruli and
2019-09-21

DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident (±)-J 113397 is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. In favo
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