• br cAMP cGMP effector systems in human platelets PKA PKG

  2021-12-23

  

  cAMP/cGMP effector systems in human platelets (PKA, PKG, PDEs) In eukaryotic cells, the effects of intracellular cAMP are mediated by two types of cAMP-dependent protein kinases (PKA type I and II) and cAMP-regulated guanine nucleotide exchange factors (EPAC/cAMP-GEF) which activate the RAS GTPas

• br Discussion Regulation of redox

  2021-12-23

  

  Discussion Regulation of redox homeostasis is critical in the maintenance of normal cell functions, and both glutathione S-transferase and peroxiredoxin enzymes are important contributors to this process. There are numerous reports of aberrant expression patterns of GSTP linked with cancer and wi

• br Author contributions br Acknowledgements

  2021-12-23

  

  Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa

• Variants of NEIL were also analysed

  2021-12-23

  

  Variants of NEIL1 were also analysed in Primary sclerosing cholangitis (PSC) and cholangiocarcinoma (CCA) patients by Forsbring et al. to identify effect of variants on these diseases. Four variants were identified i.e., one earlier validated (G83D) and three novel (E181K, H275, R339W). E181K was fo

• UNC 0646 Introduction l Glutamate is a major

  2021-12-23

  

  Introduction l-Glutamate is a major excitatory neurotransmitter in the mammalian central nervous system (CNS) that contributes not only to fast synaptic neurotransmission, but also to complex physiological processes like memory, learning, plasticity, and neuronal cell death [30], [81]. Glutamate is

• Two excellent GSMs with clear pharmacological effect across

  2021-12-23

  

  Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas

• Iodination of commercially available with excess ICl in AcOH

  2021-12-23

  

  Iodination of commercially available with excess ICl in AcOH gave a quantitative yield of , which was cyclized with benzyl thioamides to give the 2-benzyl-9,10-dihydro-4-1-thia-3,4-diaza-benzo[]azulenes . Coupling of the iodides with heterocycles including imidazoles, triazoles, or zinc cyanide us

• uPAR promotes cell associated proteolysis by binding

  2021-12-22

  

  uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot

• br Results The RAS MEK ERK pathway is a

  2021-12-22

  

  Results The RAS/MEK/ERK pathway is a potential target of FGFR signaling. Indicative for its activation is the presence of double phosphorylated (activated) ERK (dpERK), which is generated in a series of phosphorylation events downstream of FGFR (op. cit. (Lemmon and Schlessinger, 2010)). Followin

• We reveal that the four well

  2021-12-22

  

  We reveal that the four well known vertebrate families of KAT enzymes (GNAT, MYST, P300/CBP, Basal transcription factor/nuclear receptor co-activator) seem to be conserved (Karmodiya et al., 2014; Roth et al., 2001; Sheikh & Akhtar, 2018) in the mangrove rivulus, together with Camello, a potential n

• The overall response rate to afatinib

  2021-12-22

  

  The 13% overall response rate to afatinib is comparable to a 19% response rate reported by Peters et al. [20] in a separate retrospective series investigating the use of afatinib in more heavily pretreated patients with HER2-mutant lung adenocarcinomas. Our 13% response rate is also comparable to an

• P Benzoxaborole substituted macrocyclic compounds based

  2021-12-22

  

  P4-Benzoxaborole-substituted macrocyclic compounds based on ITMN-191 scaffold were prepared using a general scheme as shown in . ITMN-191 was prepared by following a patent procedure. The P4 BOC group was removed by treatment with TFA in dichloromethane to give amine . The coupling of the amine to 6

• br FXR Agonists Azepinol b indole

  2021-12-22

  

  FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in

• Selective pharmacological inhibition of tonic currents indic

  2021-12-22

  

  Selective pharmacological inhibition of tonic currents indicated that the effects of gp120 are predominantly mediated by α5-containing GABAARs. The other dominant subtype that contributes to tonic current in the hippocampus, the δ-containing GABAAR, was unaffected by gp120 treatment. Additionally, i

• br Significant efforts are currently focused on non dopamine

  2021-12-22

  

  Significant efforts are currently focused on non-dopaminergic strategies to address the unmet medical needs in schizophrenia, and targeting -methyl--aspartate (NMDA) rgs protein hypofunction has garnered a great deal of attention., , Elevation of synaptic glycine levels near NMDA-containing syna

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