• br Acknowledgements We thank Dr Tai Yuan Yu

  2019-12-03

  

  Acknowledgements We thank Dr. Tai-Yuan Yu and Miss Chun-Ping Chang for helping with the drug/DNA sequence specificity study. We also thank the Chemical Synthesis Core and the Pathology Core Laboratory of IBMS for synthesizing SL-1 and for performing the pathology analysis, respectively, and the T

• A An optimized BEI SEIscore based on the trends

  2019-12-03

  

  (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

• The homologous DDRs are composed of an N terminal

  2019-12-03

  

  The homologous DDRs are composed of an N-terminal discoidin homology domain, followed by a sequence of ∼220 amino acids unique to the DDRs, a transmembrane domain, a large juxtamembrane domain, and a conserved cytoplasmic tyrosine kinase domain. In a previous study, we demonstrated that DDR activati

• In the PTEN loss mouse model deletion

  2019-12-03

  

  In the PTEN loss mouse model, deletion of ATG7 gene not only caused an autophagy-deficient phenotype, but also postponed the progression of inoculated prostate tumor [22]. On the basis of these experimental facts, these ATG7 and PTEN related genes were then compared with the 3020 BCR-associated gene

• In conclusion our data demonstrated

  2019-12-03

  

  In conclusion, our data demonstrated that montelukast and pranlukast non-competitively blocked P2Y signaling in several cell systems, but in a relatively nonsubtype-specific manner. The functional antagonism was especially evident at heterologously expressed P2Y1 and P2Y6 receptors, at which IC50 va

• br Acknowledgments br Introduction Hypertensive retinopathy

  2019-12-02

  

  Acknowledgments Introduction Hypertensive retinopathy is a disease of the retinal microvasculature associated with elevated blood pressure (Fraser-Bell et al., 2017). Narrowing of retinal arterioles occurs in the early stage of the disease, and with persistent hypertension further vascular pat

• br Mechanisms of acquired resistance to

  2019-12-02

  

  Mechanisms of acquired resistance to 1st and 2nd generation EGFR inhibitors After treatment with first or second generation EGFR TKIs, virtually all patients after approximately 12 months develop acquired resistance (AR). Different mechanisms of AR to EGFR TKIs have been reported to date and may

• br Experimental Procedures br Author Contributions br

  2019-12-02

  

  Experimental Procedures Author Contributions Acknowledgments Introduction Oxysterols came to prominence in the late 1970\'s with the oxysterol hypothesis which proposed that the suppressive effect of cholesterol on its own synthesis is mediated through oxysterols not by cholesterol itsel

• The murine subfamily members including and

  2019-12-02

  

  The murine subfamily members including , , , and have been identified and their encoded proteins showed deubiquitinating enzymatic activity , , , . It has been demonstrated that is an immediate-early gene induced by IL-3 in B-lymphocytes and is an IL-2 specific immediate-early gene in T-lymphocytes

• Acknowledgments We acknowledge the Danish Council for Indepe

  2019-12-02

  

  Acknowledgments We acknowledge the Danish Council for Independent Research (Grant no. 11-105250) and the Carlsberg Foundation (Grant no. 2011-01-0567) for funding this work. Introduction DNA is vital as a biological target to design diagnostic agents as well as therapeutic drugs. The recognitio

• Introduction The term myeloproliferative disorders was first

  2019-12-02

  

  Introduction The term “myeloproliferative disorders” was first proposed by William Dameshek in 1951. With the discovery of the Philadelphia chromosome, myeloproliferative disorders were classified into two groups: BCR-ABL positive chronic myeloid leukemia (CML) and BCR-ABL negative chronic myelopro

• In agreement with the study on porcine

  2019-12-02

  

  In agreement with the study on porcine microsomes (Ekstrand et al., 2015), our results indicated a somewhat higher degree of inhibition of CYP2E1 activity in the male pools compared to females. Nevertheless, the degree of this NVP-BEP800 inhibition did not reach 50%, indicating that quercetin is unl

• Iberin Moreover a ligand for fusin has recently been found

  2019-12-02

  

  Moreover, a ligand for fusin has recently been found: the lymphocyte chemoattractant stromal-derived factor-1 (SDF-1) binds to CHO Iberin transfected with fusin and promotes secondary messenger production (Bleul et al., 1996; Oberlin et al., 1996). A new name, CXCR-4, has been proposed for the recep

• CUDC-907 The results of bisaryl ether linker study are shown

  2019-12-02

  

  The results of bisaryl ether linker study are shown in . It was found that the methylene linker () moderately improved the binding to the DP receptor. The increased binding potency was also diminished in the presence of plasma, possibly due to higher plasma protein binding. Other linkers, such as th

• Several highly selective COX inhibitors coxibs

  2019-12-02

  

  Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d

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