• Our previous work has demonstrated that two glutamate residu

  2021-03-10

  

  Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi

• Subgroup analysis showed that patients with

  2021-03-09

  

  Subgroup analysis showed that patients with relatively lower CrCl levels (>50–80 mL/min) were more likely to initiate treatment on a lower dose (17% for all DPP-4 inhibitors; 22% excluding linagliptin). Nevertheless, even in patients with higher CrCl value (>80–120 mL/min and >120 mL/min), at least

• The quaternary structure of many

  2021-03-09

  

  The quaternary structure of many of the family B members (i.e., secretin, glucagon, glucagon-like peptide and pilocarpine hydrochloride receptors) have been actively studied and it has been demonstrated that they can form homodimers/oligomers (Gao et al., 2009; Ng & Chow, 2015; Ng, Lee, & Chow, 201

• Ramiprilat In light of the overall

  2021-03-09

  

  In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The

• br Rationale and Conventional Use of Alkylating Agents and P

  2021-03-09

  

  Rationale and Conventional Use of Alkylating Agents and Platinum Derivatives in Clinical Practice After the attack on Bari Harbor in 1943 revealed the effects of mustard gas on bone marrow depletion and the first therapeutic outcomes in lymphoma, alkylating agents gradually became a gold standard

• br Conclusion New series of thiazolo d pyridazine

  2021-03-09

  

  Conclusion New series of thiazolo[4,5-d]pyridazine and imidazo[2′,1′:2,3]thiazolo[4,5-d]pyridazine were designed and synthesized using thiazole as scaffold based on its previously observed activity as DHFR inhibitor. Compounds 13 and 43 (Fig. 9) proved to be the most active DHFR inhibitors with I

• Table shows the clinical data of recipients

  2021-03-09

  

  Table 2 shows the clinical data of 23 recipients with CYP3A5*1 allele classified by the presence or absence of CYP3A phenoconversion. Phenoconversion of CYP3A was observed in 10 recipients with CYP3A5*1 allele. No significant differences in eGFR, ALT and total bilirubin were observed between recipie

• fgfr1 br Conflict of interest br Acknowledgments Dr Hauger

  2021-03-09

  

  Conflict of interest Acknowledgments Dr. Hauger was supported by a BLR&D Merit Review grant from the Department of Veterans Affairs, Veterans Health Administration, Office of Research and Development. Dr. Hauger also received support from the VA Center of Excellence for Stress and Mental Healt

• Employing distinct genetic and pharmacological approaches Di

  2021-03-09

  

  Employing distinct genetic and pharmacological approaches, Divakaruni et al. now demonstrate that macrophages still acquire their IL-4-elicited phenotype in the absence of CPT1a (considered the main isoform in leukocytes) or CPT2, and highlight that the increased LC-FAO in M(IL-4) cells is less cruc

• Mass spectrometry has previously been used to

  2021-03-09

  

  Mass spectrometry has previously been used to examine the presence of Hyp in recombinant collagen, using hydrolysates to identify the individual imino acid, equivalent to an amino Hydroxyfasudil analysis [33], and also by analysis of mass changes to tryptic peptides [34]. The present study, however,

• NB-598 Maleate br Allosteric inhibitors In general

  2021-03-09

  

  Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d

• Our earlier experimental studies showed neutral i e non

  2021-03-09

  

  Our earlier experimental studies showed "neutral", i.e. non-proliferative, effects of progesterone but a large increase in proliferation using certain progestins; however, this was only in the presence of PGRMC1 [[13], [14], [15], [16], [17], [18], [19]]. The next step was to investigate whether thi

• In rodent models the loss of estrogens

  2021-03-09

  

  In rodent models, the loss of estrogens through ovariectomy has been shown to promote the development of intracranial aneurysms. Conversely, the administration of an Protease Inhibitor Cocktail (100X in DMSO, EDTA plus) receptor beta agonist restores its protective effect, but is abolished with the

• Several questions remain to be

  2021-03-09

  

  Several questions remain to be addressed. The hormones and metabolites that modulate expression of EERγ in the steps leading to maturation need to be identified to learn more about physiological and pathophysiological regulation of EERγ in β cells. Considering that ERRγ repressed cell cycle genes in

• capmatinib br Conflict of interest br Acknowledgements This

  2021-03-09

  

  Conflict of interest Acknowledgements This work was supported by the Basic Science Research Program through the National Research Foundation (NRF) funded by the Ministry of Science, ICT & Future Planning (2013R1A1A1076117) and also by the Priority Research Centers Program through the NRF funde

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