• Akt Inhibitor IV One possible pitfall of using EPAC activato

  2019-09-12

  

  One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le

• In studies directed toward the development of

  2019-09-11

  

  In studies directed toward the development of sequence-specific major-groove binding small Golgicide A [11], we desired a non-intercalating molecular scaffold that could direct attached moieties into the major groove. As an initial step toward this goal, we wished to study the DNA binding mode and

• This hydrophobic biphenyl tail gave good

  2019-09-11

  

  This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC MK-3207 HCl was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent binding interactions which were

• The following is the supplementary data related

  2019-09-11

  

  The following is the supplementary data related to this article. Funding This work was supported by departmental funding to Prof. Mühl. Funding derived from the State of Hessia to the Institute of General Pharmacology and Toxicology at the pharmazentrum frankfurt (Head: Prof. Josef Pfeilschifter

• br Results br Discussion The

  2019-09-11

  

  Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i

• Till date several predictive models have been developed by d

  2019-09-11

  

  Till date, several predictive models have been developed by different research groups to speed up the process of library selection and drug optimization (Walters et al., 1999, Caldwell, 2000, Plewczynski et al., 2006, Wang and Ramnarayan, 1999, Pogorelcnik et al., 2015, Greenbaum et al., 2002, Sadow

• An AmDH is engineered by mutating two conserved amino

  2019-09-11

  

  An AmDH is engineered by mutating two conserved amino IL-10, human recombinant protein residues in the active site of an amino acid dehydrogenase (AADH). Starting from the leucine dehydrogenase (LeuDH) from Bacillus stearothermophilus, substituting a serine and leucine at the K68 and N261 positions,

• Introduction Cysteinyl leukotrienes CysLTs LTC

  2019-09-11

  

  Introduction Cysteinyl leukotrienes (CysLTs), LTC4, LTD4 and LTE4, are 5-lipoxygenase pathway metabolites of arachidonic CHIR-124 and deeply involved in bronchial asthma via activation of CysLT1 receptors [1], [2]. Specific CysLT1 receptor antagonists, including pranlukast [3], [4] and montelukast

• More recently it was discovered that BChE hydrolyzes the

  2019-09-11

  

  More recently, it was discovered that BChE hydrolyzes the neuropeptide gut hormone, ghrelin [25], [26], [27], [28]. Nonetheless, because the enzyme reaction is very slow, those who first reported this finding were initially reluctant to attribute a real physiological role for that phenomenon. Our ow

• Previous studies have documented that

  2019-09-11

  

  Previous studies have documented that SCFAs may elicit effects on lipid metabolism via de novo synthesis and transport. Acetate is not only used as an energy source, but is also constituted as a substrate for the cholesterol synthesis in the liver through acetyl-CoA, thus affecting plasma cholestero

• We have previously reported the

  2019-09-11

  

  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

• We have previously reported the

  2019-09-11

  

  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

• Studies of LRRK tagged with green fluorescent protein reveal

  2019-09-10

  

  Studies of LRRK2 tagged with green fluorescent protein revealed the presence of monomeric LRRK2 in the Pioglitazone of living cells, while LRRK2 oligomers were found in the proximity of the plasma membrane, suggesting that both oligomerization status and compartmentalization of LRRK2 defines its fu

• The binding pattern of was

  2019-09-10

  

  The binding pattern of 1 was analysed by flexible molecular docking. The Thyroid Hormone Receptor Antagonist (1-850) and inserted into the narrow ATP binding site of CK2 (Fig. 2). As shown the aliphatic chain of 1 was located at the edge of the pocket and established van der Waals interactions with

• In SLO permeabilized human sperm the AR elicited

  2019-09-10

  

  In SLO-permeabilized human sperm, the AR elicited by calcium, persistently active Arf6 [41] and Rab3A, 8-pCPT-2′-O-Me-cAMP [8], diacylglycerol and a non-hydrolyzable analog [35], is sensitive to the PLC blocker U73122. Furthermore, 8-pCPT-2′-O-Me-cAMP elicits a calcium signal in non-permeabilized sp

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