• Compounds and were tested for pharmacodynamic

  2022-08-22

  

  Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a

• As early as glucagon was shown to increase

  2022-08-22

  

  As early as 1957, glucagon was shown to increase FSLLRY-NH2 expenditure in rodents in both pair-feeding studies and through directly increasing oxygen consumption [23], [24]. This has more recently been confirmed in man, through indirect calorimetry during glucagon infusions [25], [26], [27]. This c

• Introduction High mobility group box HMGB is a nuclear prote

  2022-08-19

  

  Introduction High mobility group box 1 (HMGB1) is a nuclear protein that plays a fundamental role in the regulation of DNA-associated events such as DNA repair, transcription, and replication. HMGB1 can be translocated to the cytosol, plasma membrane, and extracellular space in response to various

• The inhibitory activities of the compounds with the modifica

  2022-08-19

  

  The inhibitory activities of the compounds with the modification of the amino group against human liver FBPase are summarized in . Replacement of the amino group of with hydrophobic substituent such as a methyl group () led to a substantial loss of activity (IC=995nM). Similarly, replacement with h

• Recently considerable effort has been invested in developing

  2022-08-19

  

  Recently, considerable effort has been invested in developing FDPS inhibitors based on alternative scaffolds (including nonbisphosphonates) that allow other tissue types and parasite-derived forms of FDPS , to be targeted. There are several limits in analyzing inhibitors of FDPS activity: the most w

• In the course of an

  2022-08-19

  

  In the course of an internal FAAH, program,, , , , , , , , , , , , , many very similar compounds were profiled in vivo with particular interest paid to their ability to penetrate the BBB. The compounds profiled were heteroaryl piperazinyl and piperadinyl ureas; a class of compounds, reported on pr

• There are limited studies on antibody responses against HIV

  2022-08-19

  

  There are limited studies on antibody responses against HIV-1 integrase antigen. According to previous studies, almost 5 percent of individuals infected with HIV never raise anti-integrase sglt-2 (Rikhtegaran Tehrani et al., 2015; Chang et al., 1985). If this rate is identical in individuals infect

• A pyrimidine class of compounds

  2022-08-19

  

  A pyrimidine class of compounds is of enormous interest within anti-HIV drug discovery process for several decades, as pyrimidine based DABOs class [7], DAPYs class [8] are well known as NNRTIs as well as NRTIs. However, the overall role of a pyrimidine class of heterocycles in anti-HIV drug discove

• Introduction Histone is the core component of chromatin

  2022-08-19

  

  Introduction Histone is the core component of chromatin and histone modification is one of the key mechanisms of epigenetic regulation (Bannister and Kouzarides, 2011). Amino NG,NG-dimethyl-L-Arginine hydrochloride sale residues on histone tails can be modified under different mechanisms including

• VE-821 Evidence indicates that astrocytes play

  2022-08-19

  

  Evidence indicates that astrocytes play a role in the modulation of NMDAR activity in the CA1 (Henneberger et al., 2010; Papouin et al., 2017a, Papouin et al., 2017b; Robin et al., 2018). Therefore, we sought to examine whether astrocytes are involved in the H1 receptor antagonist/inverse agonist-in

• microRNAs miRNAs of approximately nucleotides play vital rol

  2022-08-19

  

  microRNAs (miRNAs) of approximately 22 nucleotides play vital roles in cancer development and progression by regulating translational repression or decay of target messenger RNAs (mRNAs) through their binding to the 3′-untranslated regions (3′-UTRs) of target mRNAs with imprecise or precise compleme

• Most studies of HIF have focused on

  2022-08-19

  

  Most studies of HIF-1α have focused on its transcriptional activity-dependent functions. However, our results indicate that the oxidative stress-related effects of mtHIF-1α occur independently of its translocation to the nucleus and do not require its transcriptional activity. In fact, several studi

• Introduction In the s nitric oxide NO was

  2022-08-19

  

  Introduction In the 1980s, nitric oxide (NO) was first characterized as critical to both innate immunity and endogenous signaling in animals [[1], [2], [3], [4], [5]]. NO was the first gaseous signaling molecule synthesized by animals to have its biochemical signaling pathway fully described [2]. P

• The differential tissue and ligand dependent signaling descr

  2022-08-19

  

  The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va

• An alternative approach to improving pharmacokinetic

  2022-08-18

  

  An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unli

15597 records 379/1040 page Previous Next First page 上5页 376377378379380 下5页 Last page