• To develop novel EPAC inhibitors

  2021-06-28

  

  To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock

• More than thirty enzymes with PLA

  2021-06-28

  

  More than thirty enzymes with PLA2 activity have been described and, based on sequence similarities, they are currently classified in 16 groups, each containing several sub-groups [16]. However, based on biochemical features these enzymes are frequently grouped into six major families: secreted phos

• br Enzyme catalysis A biochemically spontaneous process

  2021-06-28

  

  Enzyme catalysis A biochemically spontaneous process proceeds in a direction where free Quercitrin of the system decreases. However, every spontaneous or energetically favorable reaction needs to overcome an energy barrier known as the activation energy barrier because of the formation of an unst

• Our finding that activating DDR variants are a cause of

  2021-06-28

  

  Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho

• Similar to EGFR another receptor tyrosine kinase RTK

  2021-06-28

  

  Similar to EGFR, another receptor tyrosine kinase (RTK), fibroblast growth factor receptor 4 (FGFR4), is gaining attention in the lung cancer setting. The protein expression of this receptor has been recently associated with a negative impact on lung cancer prognosis, supporting the idea that FGFR4

• br E intracellular localization br Regulation of E by other

  2021-06-28

  

  E1 intracellular localization Regulation of E1 by other post-translational modifications Concluding remarks Acknowledgments We apologize to those whose work was not included because of space considerations or whose papers were unintentionally omitted. We thank Dr Peter Bullock (Tufts Uni

• Historically covalent drugs have had great success e g

  2021-06-28

  

  Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form

• Tailoring pharmacological treatment to the genetic backgroun

  2021-06-28

  

  Tailoring pharmacological treatment to the genetic background of a person can enhance therapeutic response (), increase compliance (), and decrease drug toxicity (, , ). Because cocaine addiction has a strong genetic basis, with the vulnerability to develop an addiction estimated to be as high as 72

• Why then is leading strand

  2021-06-28

  

  Why then is leading-strand DNA synthesis reduced relative to lagging-strand synthesis in rad53-1 mutant TGX-221 under replication stress? To gain insight into this question, we first determined whether the firing of late origins in rad53-1 mutant cells contributes to compromised leading-strand synt

• br Concluding remarks br Introduction Hypertrophic pachymeni

  2021-06-28

  

  Concluding remarks Introduction Hypertrophic pachymeningitis (HP) is a neurologic disorder characterized by diffuse or focal thickening of the intracranial or spinal dura mater, presenting with intracranial hypertension, cranial nerve palsy and spinal cord dysfunction (Kupersmith et al., 2004;

• After repeated intermittent exposure to

  2021-06-28

  

  After repeated, intermittent exposure to a psychostimulant an augmentation of drug response to motor activity is commonly observed, a phenomenon known as behavioral sensitization (Kalivas and Stewart, 1991, Steketee and Kalivas, 2011). On the other hand, several reports have pointed out that stress

• br ET Antagonist for the Future

  2021-06-25

  

  ET Antagonist for the Future: Macitentan and Atresentan Macitentan is an insurmountable antagonist, resulting from structure-activity studies to improve the efficacy and tolerability of bosentan, and gained approval in the United States in 2013 for the treatment of PAH. Actelion describes the com

• In terms of its protease activity MME has a

  2021-06-25

  

  In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other Calmidazolium chloride australia of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target an

• ionomycin Nimodipine administration also inhibited the eIF A

  2021-06-25

  

  Nimodipine administration also inhibited the eIF2α/ATF4 singnaling which is a crucial evolutionarily conserved adaptive pathway during cellular stresses including hypoxia and ischemia (Evans et al., 2016; Manwani and McCullough, 2013). While, the eIF2a/ATF4 pathway, activated by different forms of s

• Introduction Excessive exposure to ultraviolet UV irradiatio

  2021-06-25

  

  Introduction Excessive exposure to ultraviolet (UV) irradiation from the sun injures human skin, which might lead to premature aging and skin pathologies [1], [2]. Chronic exposure to UV (especially ultraviolet-B, UVB) irradiation could profoundly affect the skin epidermis, interfering with the ker

15788 records 605/1053 page Previous Next First page 上5页 601602603604605 下5页 Last page