• Further modifications on the position

  2020-04-06

  

  Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po

• br Significance Ubl post translational modifications are

  2020-04-06

  

  Significance Ubl post-translational modifications are potential targets for developing novel therapeutics for life-threatening diseases, such as c-Myc- and KRas-driven cancers that lack targeted therapy. However, only a few drugs are available to target these modifications. This lack of drugs hig

• Dipeptidyl peptidase inhibitors DPP is or

  2020-04-06

  

  Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit dna repair pathways secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good eff

• Electron transport via DHODH activity will allow

  2020-04-06

  

  Electron transport via DHODH activity will allow the generation of mitochondrial ROS without the consumption of α-ketoglutarate or NADH. Glutamine-dependent flux through the TCA cycle and oxidative phosphorylation can also enable generation of mitochondrial ROS (Weinberg et al., 2010). The latter pr

• Carprofen The crystal structure of the B subtilis Maf

  2020-04-06

  

  The crystal structure of the B. subtilis Maf (BSU28050) was published in 2000, and, to date, it represents the only experimental work with a purified Maf protein (Minasov et al., 2000). The structure revealed a structural fold similar to that found in ITPases and YjjX proteins, which are nucleotide

• In our preliminary evaluation of this series we

  2020-04-06

  

  In our preliminary evaluation of this series, we were surprised to discover that integrin inhibitor was found to bind CSF-1R in a classical DFG-in binding mode (a). Dramatic conformational differences in the juxtamembrane domain and activation loops are apparent when this DFG-in structure is compa

• br Acknowledgments This research was supported by grants

  2020-04-06

  

  Acknowledgments This research was supported by grants from the Ministerio de Ciencia e Innovación (Grants SAF/FEDER 2010-17907; 2013-49076-P), Spain, Red de trastornos adictivos (RETICS RD12/0028//0003, Instituto de Salud Carlos III, Spain) and Fundación Séneca (15405/PI/10, Región de Murcia, Spa

• endothelin receptor Another option is to use the thiol group

  2020-04-06

  

  Another option is to use the thiol groups of cysteine residues, which can be modified by use of PEG-maleimide and vinyl sulfone. However, changes in PEGylation interactions or reaction conditions can result in changes in the functional properties of the therapeutic proteins [[50], [51], [52]]. A st

• br Materials and methods br Results br Discussion In this

  2020-04-06

  

  Materials and methods Results Discussion In this study, we first showed that fluxametamide, a novel isoxazoline insecticide, inhibits agonist responses in two types of LGCCs, the M. domestica GABACl and GluCl, with higher potency in the former channel versus the latter one (Fig. 3). In addi

• br Materials and methods br Results br Discussion Human Chk

  2020-04-06

  

  Materials and methods Results Discussion Human Chk, a member of the Csk-family, was initially cloned from two different megakaryocytic cell lines [2], [3]. Structural comparison of human Chk with human Csk shows that human Chk has the additional N-terminal unique domain [2], [3], [25]. Chk

• br Results br Discussion The nitric oxide cyclic

  2020-04-06

  

  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

• The glycolytic pathway is a

  2020-04-06

  

  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

• Rose Bengal br Transparency document br Acknowledgements We

  2020-04-06

  

  Transparency document Acknowledgements We thank Prof. Barbara Brodsky for valuable comments and discussion. We thank the support of the Tufts start-up fund and the Knez Family Faculty Investment Fund for Y.-S. L, and the Tufts Summer Scholar program for E.C. Introduction Discoidin domain r

• br Materials and methods br Results br

  2020-04-06

  

  Materials and methods Results Discussion Studies have suggested that the Hh signaling pathway, which plays as an essential autocrine viability factor for MFBs [10], [11], is a potential therapeutic target for liver fibrosis. Previously reported works have proven the effectiveness of the Hh

• Thienoguanosine There have been two reports

  2020-04-03

  

  There have been two reports of tumor shrinkage in response to dasatinib treatment in lung SCC patients harboring the DDR2 kinase domain S768R mutation., In the first case described by Hammerman et al. a combination of erlotinib (an epithelial growth factor receptor inhibitor) and dasatinib was admin

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