• br Results and discussion br Conclusion We have

  2019-09-23

  

  Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz

• Our finding that one enzyme acts both as a

  2019-09-23

  

  Our finding that one enzyme acts both as a primase and a DNAP poses evolutionary and mechanistic questions. In particular, why do cellular organisms require two enzymes to fulfill de novo DNA synthesis? The inability of cellular replicases to perform as primases might be dictated by the challenges a

• During the past three decades platinum based DNA

  2019-09-23

  

  During the past three decades, platinum-based DNA-alkylating agents have been employed in the treatment of various cancers [14]. Oxaliplatin is currently used as a first-line treatment for colorectal cancer (CRC) [15]. Unfortunately, a large portion of CRC patients receiving oxaliplatin-based chemot

• The promoter regions of all

  2019-09-23

  

  The promoter regions of all MdDGKs examined here included many hormone-responsive and stress-responsive elements, such as ABRE, MBS, TC-rich repeats, HSE, and LTR. Despite assumptions about how those promoters might control expression in response to environment stimuli, we found several exceptions.

• The DDR gene located on chromosome region p

  2019-09-23

  

  The DDR1 gene, located on chromosome region 6p21.33, encodes a transmembrane tyrosine kinase receptor involved in melanocyte anchoring through binding to collagen IV (Silva de Castro et al., 2010). So far, only three studies have been conducted on the association between DDR1 polymorphism and the ri

• Another important mediator in fear learning is the

  2019-09-23

  

  Another important mediator in fear learning is the neuropeptide corticotropin-releasing factor (CRF). For example, local repeated administration of CRF into the basolateral amygdala potentiates the acquisition of cue-conditioned fear (Bijlsma et al., 2011) and CRF1 receptor antagonists effectively b

• We further correlated OPRK and OPRM methylation levels with

  2019-09-23

  

  We further correlated OPRK1 and OPRM1 methylation levels with individual characteristics in Xinjiang Han and Uygur controls. Partial correlation analyses showed that OPRK1 methylation was positively correlated with age in Uygur male controls (r=0.72, p=0.001, adjusted by body mass index (BMI), gluco

• 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

• 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

• 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

• 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

• 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 .

• 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

• 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

• 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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