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Pazopanib Hydrochloride With the identification of small
2022-07-29

With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met
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Binding of FGFs to FGFRs leads to receptor dimerization resu
2022-07-29

Binding of FGFs to FGFRs leads to receptor dimerization, resulting in the transphosphorylation of a tyrosine in the activation loop of the kinase domain. Subsequently, the activated FGFRs phosphorylate their intracellular receptor substrates, particularly FGFR substrate 2 (FRS2) and phospholipase Cγ
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All of the abovementioned effects of PUFAs signal their invo
2022-07-29

All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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HMP Linker Whether ferroptosis specific inhibitor could prom
2022-07-29

Whether ferroptosis specific inhibitor could promotes spinal cord repair is a question worth to explore. A potent and stable ferroptosis specific inhibitor is essential for in vivo study. Ferrostatin-1 (Fer-1), the first generation of ferroptosis inhibitor, was shown actively suppressing ferroptosis
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br Venous thromboembolism VTE is
2022-07-29

Venous thromboembolism (VTE) is a rare but potentially life-threatening complication of total joint arthroplasty (TJA) . With modern chemoprophylaxis, the incidence of VTE after primary total hip (THA) or total knee (TKA) arthroplasty is commonly estimated between 0.5% and 1%, and VTE is now consi
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Murine models of AML were used
2022-07-29

Murine models of AML were used to identify differentially expressed proteins following treatment with the EZH2 inhibitor, DZnep. Sandow and coworkers demonstrated that inhibition of EZH2 induces leukemia UNC 0631 sale arrest through regulation of cyclin-dependent kinases and increased expression of
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Similarly towards the acylsulfamoyl benzoxaboroles the boron
2022-07-28

Similarly, towards the 5-acylsulfamoyl benzoxaboroles, the boronate intermediate was prepared according to , while the boronate , an intermediate towards 4-acylsulfamoyl benzoxaboroles, was prepared according to . The sulfonamides and used in the synthesis were made from the starting sulfonyl chl
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In first wave first generation drugs telaprevir and
2022-07-28

In 2013, first-wave, first-generation drugs telaprevir and boceprevir was the first protease inhibitors (PIs) incorporated in Brazilian Clinical Guidelines for the treatment of patients infected with HCV perifosine sale 1. Based on this 2013 Clinical Guideline, telaprevir could be used for both naïv
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br Conclusions br Conflicts of Interest br Introduction Myal
2022-07-27

Conclusions Conflicts of Interest Introduction Myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS) is a chronic multisystem illness of unconfirmed cause. ME/CFS has largely been diagnosed from Fukuda CFS criteria and/or the Canadian ME/CFS criteria. The Institute of Medicine in 2015
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His brother individual B II
2022-07-27

His brother, individual B.II-4, is 11 months old. He was born at term with intrauterine growth retardation. His birth weight was 2.2 kg (T (p. Arg176Trp) variant in SLC45A1 (GenBank: NM_001080397.1). This variant is very rare (MAF = 0.00001660 in the ExAC Browser) and predicted to be damaging by Pol
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There are two ways to transport FFAs into cells First
2022-07-27

There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty AKT inhibitor VIII transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36 is re
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br Future perspectives A plethora of reports from in
2022-07-27

Future perspectives A plethora of reports from in vivo and in vitro human and animal studies have demonstrated the potential role of FGFR signalling in human carcinogenesis, whether it be in an oncogenic or tumour suppressive capacity. It is still not well understood how FGFRs can act as tumour s
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Species specificity of small molecular GPR agonists
2022-07-27

Species specificity of small molecular GPR40 agonists have been reported by Takeda scientist. In the binding pocket of TM5, a Leu186 in human GPR40/FFA1 is replaced with Phe in rat, resulting in dramatic inter-species GPR40 activity discrepancy in certain scaffolds of small molecular GPR40 agonists.
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br RESULTS br DISCUSSION In
2022-07-26

RESULTS DISCUSSION In this study, we found impaired apoptosis in the peripheral blood of RA patients when compared with peripheral blood from normal controls. Our previous studies have shown that the number of CD4 + T GS967 increased while regulatory T (Treg) cells diminished in the periphera
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In the FARM motifs of GGPPSs hydrophobic amino
2022-07-26

In the FARM motifs of GGPPSs, hydrophobic c-di-AMP australia are replaced by aliphatic amino acids, which are more flexible residues and allow the entrance of longer substrates into the pocket (Wang and Ohnuma, 2000). It has been reported that the lepidopteran Manduca sexta CA possesses GGPP syntha
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