• For the SAR study human haspin kinase inhibitory

  2022-04-22

  

  For the SAR study, human haspin kinase inhibitory activity of the various compounds was evaluated using the same assay utilized for the HTS, except in the presence of varying test compound concentrations. DYRK2 kinase inhibitory activity was measured by P-incorporation into Woodtide peptide substrat

• The number of small molecule GSK inhibitors is continuously

  2022-04-22

  

  The number of small molecule GSK-3 inhibitors is continuously rising and many have been tested in animals. These studies have provided additional support for specific roles of GSK-3 in neuronal functions under both normal and pathological conditions. Inhibition of GSK-3 has profound effect on neurop

• Historically pharmacological investigations have been carrie

  2022-04-22

  

  Historically, pharmacological investigations have been carried out by first identifying a biological response to a ligand, and then subsequently using that ligand to identify the receptor(s) responsible for the response (Wilson et al., 1998). However, this approach needed revision with the discovery

• Several studies have found that GPR possesses a distinct

  2022-04-22

  

  Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected PF-4708671 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Ri

• Quinacrine hydrochloride hydrate In order for cytokines to e

  2022-04-22

  

  In order for cytokines to exert any effect on the NSC population, they must first bind to specific receptors on the cell surface. Numerous pro- and anti-inflammatory cytokines are able to exert effects on the NSC population, including IL-1β through IL-1R1 and IL-1R2, TNFα through TNFR1 and TNFR2, IL

• In addition to gonadotropes GnRHRs have also

  2022-04-22

  

  In addition to gonadotropes, GnRHRs have also been detected on somatotropes, lactotropes, thyrotropes, melanotropes, somatolactin (SL) cells, and/or corticotropes using immunohistochemical, radioligand-binding, or mRNA expression approaches across species; including fishes, rats, and humans (La Rosa

• The first hypothesis better fertility in heifers that

  2022-04-22

  

  The first hypothesis, better fertility in heifers that had CL at day 0, was clearly supported by our results. Heifers with a CL had over 60% P/AI compared to ∼50% in heifers without CL. These results are consistent with several other studies reporting that cycling heifers have greater fertility than

• Introduction Substantial body of evidence supports the

  2022-04-22

  

  Introduction Substantial body of evidence supports the notion that GABA, the dominant inhibitory neurotransmitter in the hypothalamus of mammals, affects GnRH release by two classes of membrane receptors: GABAA (GABAAR) [1] and GABAB (GABAB R) [2]. Studies in rodents and sheep have documented that

• The differentially expressed proteins during somatic embryog

  2022-04-22

  

  The differentially expressed proteins during somatic embryogenesis are described as the proteins that are induced by oxidative stress and respond to higher cell division activity including ascorbate peroxidase, dehydroascorbate reductase, glutathione transferase and mitochondrial manganese superoxid

• Which is the preferred dimer configuration the one correspon

  2022-04-22

  

  Which is the preferred dimer configuration, the one corresponding to the active state or the one corresponding to the desensitized state? Umbrella sampling simulations of a pair of GluA2 LBDs, using distances at the top (proximal to the ATD) and the bottom (proximal to the TMD), indicate that the de

• In this study for the first time the

  2022-04-22

  

  In this study, for the first time: 1) the electrochemical glutamate oxidase-based biosensor was optimized for the determination of low micromolar glutamate concentrations; 2) the algorithm of the analysis of exocytotic and transporter–mediated glutamate release was developed; 3) the comparative anal

• Acknowledgments br Introduction The gut derived hormone oxyn

  2022-04-21

  

  Acknowledgments Introduction The gut-derived hormone oxyntomodulin (OXM) is a naturally occurring dual agonist of both the glucagon receptor (GCGr) and glucagons-like peptide 1 receptor (GLP-1r). Structurally OXM is the 29 mibefradil of glucagon with a C-terminal octapeptide tail. Administratio

• br Conclusions Temporally controlled disruption of Gcgr

  2022-04-21

  

  Conclusions Temporally-controlled disruption of Gcgr reveals a lack meaningful contribution to the improvement of glycemic control in insulinopenic conditions attributable to the intrinsic loss of GCGR signaling. On the other hand, these data highlight the importance of compensatory systems, incl

• br Materials and methods br Results br

  2022-04-21

  

  Materials and methods Results Discussion The global pandemic of T2DM has mandated a search for new types of therapeutic agent and several long-acting analogs of naturally occurring incretins, particularly derivatives of GLP-1, have already been adopted in clinical practice [29]. This study

• Some clinical reports have suggested that

  2022-04-21

  

  Some clinical reports have suggested that galanin has a role in the neurobiology of mood disorders [[6], [7], [8], [9], [10]]. In behavioral studies, contradictory results have been reported [11,12]. For example, systemic administration of non-selective galanin receptor agonists, such as galmic [13]

15853 records 430/1057 page Previous Next First page 上5页 426427428429430 下5页 Last page