• br Conclusion br Conflict of interest

  2022-01-15

  

  Conclusion Conflict of interest References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements Introduction Free fatty acids (FFAs) are essential nutrients that contribute to various cellular functio

• Recently the novel fatty acid receptor GPR also called FFAR

  2022-01-15

  

  Recently, the novel fatty TCEP receptor, GPR120 (also called FFAR4), has been shown to be implicated in diverse physiological homeostasis, such as insulin sensitization, anti-inflammation and regulation of appetite (Hirasawa et al., 2005, Oh et al., 2010). Notably, it is abundantly expressed in WAT

• Rapid action of E on GnRH neurons has been known

  2022-01-15

  

  Rapid action of E2 on GnRH neurons has been known for some time. E2 hyperpolarizes guinea pig GnRH neurons, alters cAMP production in GT1-cells and stimulates or inhibits [Ca2+]i oscillations within 15 min (Lagrange et al., 1995; Navarro et al., 2003; Temple et al., 2004; Romanò et al., 2008). Impor

• Hepatic drug metabolizing enzymes and transporters expressio

  2022-01-15

  

  Hepatic drug-metabolizing caspase pathway and transporters expression were regulated by nuclear receptors [19], [20], [21]. The effects of HFD-induced fatty liver on drug metabolizing enzymes in mice were recently studied, and the results provided a systematic evaluation of the changes of nuclear r

• Various strategies have been pursued in the search for GIPR

  2022-01-15

  

  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 biotin 100 mg substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modifications such as e.g

• High lipophilicity of seems to cause poor PK profiles First

  2022-01-14

  

  High lipophilicity of seems to cause poor PK profiles. First we replaced the phenyl ring of compound with various hetero aromatic rings to reduce lipophilicity, (). The synthesis of pyridine derivative was shown in . (2′,6′-Dimethylbiphenyl-3-yl)methanol () was reacted with 2,5-dibromopyridine i

• Interestingly the subcellular localization of FBPase in

  2022-01-14

  

  Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule Fenoprofen Calcium receptor reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our re

• We then explored the possible mechanisms by

  2022-01-14

  

  We then explored the possible mechanisms by which integrin α5β1 was involved in the PHEV proliferation process. Normally, the virus activates integrin and induces its downstream protein activation to promote its own invasion and proliferation. Human papillomavirus type 16 (HPV16) binds to heparan su

• Following the discovery of diketo compounds S

  2022-01-14

  

  Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent WAY-100635 maleate salt based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV i

• SH-4-54 Intestinal epithelium renewal is tightly controlled

  2022-01-14

  

  Intestinal epithelium renewal is tightly controlled by Hedgehog genes. Three Hedgehog genes are highly conserved in mouse and human, including Sonic hedgehog (Shh), Indian hedgehog (Ihh), and Desert hedgehog (Dhh) [13]. Hedgehogs bind to Patched (PTCH) [[14], [15], [16]], which unlike conventional r

• Currently the computational chemical biology has been applie

  2022-01-14

  

  Currently, the computational chemical biology has been applied in hepatitis B antiviral drug discovery research [18]. Tan et al. explored oxime ethers as HBV inhibitors by docking and screening [19]. Allen et al. clarified the resistance of HBV to the nucleoside drug lamivudine [20]. The results sug

• Epiberberine br Conclusion br Disclosure of interest br Ackn

  2022-01-14

  

  Conclusion Disclosure of interest Acknowledgement Introduction Vitamin B6 has long been recognized as a cofactor for many enzymes, especially those involved in amino Epiberberine metabolism. Apart from its role as coenzyme, recent studies are unveiling a new role of vitamin B6 as a chemo

• br Brief overview of GSK inhibitors

  2022-01-14

  

  Brief overview of GSK-3 inhibitors We will briefly summarize some of the key aspects about GSK-3 inhibitors. Additional details of GSK-3 inhibitors in clinical trials have been recently reviewed [5]. GSK-3 is a complicated target as it is involved in many biological processes from neurology, dia

• RO5185426 GPR is present primarily in the pancreas and the

  2022-01-14

  

  GPR119 is present primarily in the pancreas and the intestine. Activation of GPR119 increases insulin, GLP-1, GIP and PYY secretion. GPR119 agonists stimulate insulin release in a glucose-dependent manner. The glucose dependent insulin secretion (GIDS) mechanism makes GPR119 an attractive target for

• Armed with this knowledge we looked

  2022-01-14

  

  Armed with this knowledge, we looked at ways to reduce the log of through nitrogen incorporation while still maintaining potency via installation of ortho substituents such as chloro, methyl, bromo, and thiomethyl (). In general, pyridine analogs were less active ( vs ; vs ; vs ) than their simpl

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