• Similar to GPR A activation

  2022-03-22

  

  Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic neomycin sulfate receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et al., 2008, Gold et al., 196

• The expression of heat shock proteins HSPs can

  2022-03-22

  

  The expression of heat-shock proteins (HSPs) can be upregulated by viral infection, nutritional deficiency, TNF-α and oxidative stress in Paeonol [44], [45] HSPs are classified in six families (including the HSP10, HSP40, HSP60, HSP70, HSP90 and HSP100 families). HSP90 [46] for example provides a na

• In addition to vertebrate species GnRH has been identified

  2022-03-22

  

  In addition to vertebrate species, GnRH has been identified in invertebrates, such as in the Protochordate Ciona intestinalis (Powell et al., 1996; Adams et al., 2003), the decapods mollusk Octopus vulgaris (Iwakoshi et al., 2002), the gastropod mollusk, the sea hare Aplysia californica (Zhang et al

• Introduction The West syndrome or epilepsy with epileptic

  2022-03-22

  

  Introduction The West syndrome or epilepsy with epileptic spasms (ES) is an epileptic encephalopathy in early infancy with probable seizure-related developmental regression. According to the United Kingdom Infantile Spams Study (UKISS), common causes of infantile spasms include hypoxic-ischemic enc

• Unfortunately the approved drugs suffer from failure in

  2022-03-21

  

  Unfortunately, the approved drugs suffer from failure in many cases [5,6]. Several mutations occur in the binding site of NS3/4A protease, which affect drug binding and cause drug resistance [13]. It is a big challenge and needs more efforts to be done. This is the reason why research is still conce

• We are pursuing a hit to lead medicinal

  2022-03-21

  

  We are pursuing a hit-to-lead medicinal chemistry campaign to optimize inhibitors of the HBV RNaseH. Here, we report the activity of seven new HIDs and nine new HPDs, with significant improvements in in vitro potency and cytotoxicity profiles for the HPD compounds. Materials and methods Result

• In this precancerous condition though cancer develops from t

  2022-03-21

  

  In this precancerous condition, though cancer develops from the epithelium, the subepithelial connective tissue also play crucial biological role in pathogenesis and progression to malignancy. In this context it may be noted that some recent reports addressed the problem of the mechanical interactio

• Compared with the tetrazole derivative the potency of analog

  2022-03-21

  

  Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, su

• Reduction of the hydrolysis of ATP is

  2022-03-21

  

  Reduction of the hydrolysis of ATP is an important strategy to reduce ischemia/reperfusion injury. Increased intracellular concentrations of solutes secondary to ATP depletion are known to result in osmotic swelling that may be sufficient to cause sarcolemmal rupture. Cinaciguat activates sGC direct

• Racemic protein crystallography has been

  2022-03-21

  

  Racemic protein crystallography has been proven to be a powerful technique for crystallizing proteins , , , , . The structures of many difficult-to-crystallize peptides/proteins of different sizes were resolved by the racemic protein crystallography combined with the protein chemical synthesis , , ,

• br Conclusion The following is the

  2022-03-21

  

  Conclusion The following is the supplementary data related to this article. Conflict of interest Funding Acknowledgements Peroxiredoxin VI (Prdx6) is a dual-functioning antioxidant enzyme that acts to protect biological membranes against damage caused by lipid peroxidation , . The enz

• In addition to their functional activation of GPR

  2022-03-21

  

  In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic Probucol to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner, whereas unlab

• The occurrence of MDR in cancer patients undergoing

  2022-03-21

  

  The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer Epothilone D in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems including the

• br Acknowledgements br Introduction Obesity is a growing pan

  2022-03-21

  

  Acknowledgements Introduction Obesity is a growing pandemic, which becomes a global public health problem. The evidence has been readily available and mounting, demonstrating that obesity increases incidences of chronic comorbidities, such as non-alcoholic fatty liver diseases, diabetes, cardi

• GK allosteric activators validate the importance of GK from

  2022-03-21

  

  GK allosteric activators validate the importance of GK from a therapeutic perspective, but the nature of allosteric activation of GK remains unclear. The GK allosteric activator site, the pocket where GKAs bind, is ~20 Å remote from the active site (Fig. 1A). The allosteric site is the locus of many

15755 records 471/1051 page Previous Next First page 上5页 471472473474475 下5页 Last page