• During the course of our optimization of the diarylsulfonami

  2021-11-16

  

  During the course of our optimization of the diarylsulfonamide chemotype as FFA4 agonists, we identified xanthene as a potent and selective antagonist of FFA4 (). Xanthene was able to block the agonist induced intracellular Ca response elicited by both linoleic CP-809101 hydrochloride and compoun

• estrogen related receptor br Introduction The fibroblast gro

  2021-11-16

  

  Introduction The fibroblast growth factor receptor (FGFR) pathway is an important oncogenic driver in malignant cancer. It controls cellular processes such as cell proliferation, differentiation, migration, estrogen related receptor progression, metabolism, and survival. In non–small-cell lung c

• Active compounds and were further tested and

  2021-11-16

  

  Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of

• In the adult normal spinal cord

  2021-11-16

  

  In the adult normal spinal cord, the resident cells mainly include neurons, astrocytes, oligodendroglia and microglia (Lecca et al., 2012, Miyagi et al., 2012). After SCI, the lesion microenvironment is complex, which includes the functional changes of CNS resident cells and the infiltration of leuk

• br Acknowledgments br Introduction Liver disease

  2021-11-16

  

  Acknowledgments Introduction Liver disease is one of the leading causes of death worldwide. Death from any type of acute or chronic liver injury results when sufficient healthy hepatic parenchyma cannot be regenerated to perform vital liver-specific functions. Although the regenerative capabil

• Miconazole Among the GSK inhibitors available in market lith

  2021-11-15

  

  Among the GSK-3 inhibitors available in market, lithium is probably the only example and the oldest one. Some molecules, both natural and synthetic, such as maleimide derivatives, staurosporine (from the bacterium Streptomyces storosporeus), indole derivatives such as indirubin (used since long in t

• In summary we have developed an efficient synthetic route to

  2021-11-15

  

  In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ-

• Studies of human and mouse GPR as ascertained

  2021-11-15

  

  Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infla

• Various strategies have been pursued in the search

  2021-11-15

  

  Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino Baicalin substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modifications such as e.g. Pro

• The lack of inhibition of K efflux in

  2021-11-15

  

  The lack of inhibition of K+ efflux in normal red cells reported by Fathallah et al. [16] was attributed by the authors to a lower level (about half) of membrane PKCα activity. In our experiments, single channel recording probably overcame this difficulty because of its molecular detection level. O

• In conclusion a novel series

  2021-11-15

  

  In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen SP 141 had a remarkable effect on the GPR40 agonistic activity. Com

• As a part of our continuing efforts towards

  2021-11-15

  

  As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here

• In this study according to the critical pharmacophore

  2021-11-15

  

  In this study, according to the critical pharmacophore T31, Y113 and R140 of FBPase, using the strategy of pharmacophore-based virtual screening, a series of novel scaffold inhibitor targeted the AMP binding site of FBPase were screened, their inhibitory activities against FBPase were further tested

• br Introduction Lysine acetylation is an important post

  2021-11-15

  

  Introduction Lysine acetylation is an important post-translational modification that is found on numerous cellular proteins, including both histone and non-histone proteins [1], [2]. Dynamic acetylation and deacetylation is regulated by enzymes called histone acetyltransferases (HATs) as writers

• SB-505124 hydrochloride synthesis Most studies of HIF have f

  2021-11-15

  

  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

15499 records 502/1034 page Previous Next First page 上5页 501502503504505 下5页 Last page