• Our own search towards aryl imidazole

  2022-01-10

  

  Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,

• More direct evidence of a role for Hat

  2022-01-10

  

  More direct evidence of a role for Hat1 in the acetylation of newly synthesized histone H4 has come from a number of recent studies that have shown that Hat1 is responsible for at least a portion of the acetylation that occurs on histone H4 lysines 5 and 12 in the pool of cytosolic histones. In chic

• RS testing has been extensively validated in patients with

  2022-01-10

  

  RS testing has been extensively validated in patients with early stage, ER+, HER2− patients. TAILORx, a randomized controlled trial to evaluate the role of adjuvant chemotherapy by RS, found no recurrence or survival benefit to the addition of chemotherapy to endocrine therapy in patients with inter

• ICLs represent of all generated DNA adducts for

  2022-01-10

  

  ICLs represent ICL Inducers in Cancer Therapy Nitrogen mustards with aromatic substituents (chlorambucil, melphalan) or a bioactivatable phosphoramide group (cyclophosphamide) were one of the first identified DNA crosslinkers. These agents are still used in combined schemes for the therapy of chr

• There is increased awareness of HBV reactivation in chronic

  2022-01-10

  

  There is increased awareness of HBV reactivation in chronic HCV/HBV co-infected patients treated with DAAs [1], [2]. The recent emergence of this adverse event of DAA therapy is due to the exclusion of HBV co-infected subjects from registration clinical trials evaluating the safety of these treatmen

• Cysteine Cys residues are frequently found to be highly cons

  2022-01-10

  

  Cysteine (Cys) residues are frequently found to be highly conserved within functional, regulatory, catalytic, or binding sites of proteins. Thiol or thiolate chemistry imparts active sites with unique properties like nucleophilicity, high affinity metal binding, and disulfide bond assisted multimeri

• Ras small GTPases are critical molecular switches

  2022-01-10

  

  Ras small GTPases are critical molecular switches that connect extracellular signals to intracellular signaling pathways initiated by membrane receptors, such as growth factor receptors and G protein-coupled receptors (Simanshu et al., 2017). When shifting between active GTP-bound and inactive GDP-b

• JNJ-38877605 In the H NMR spectrum two pairs of doublet reso

  2022-01-10

  

  In the 1H NMR spectrum two pairs of doublet resonances arising from the protons in the aromatic moiety of the two diastereoisomers can be readily observed around 7.5–7.6 ppm. These resonances can be used to detect and quantify the two diastereoisomers. From the results presented in Fig. 1A it can be

• br Myelin and metabolism In addition

  2022-01-10

  

  Myelin and metabolism In addition to promoting efficient NAD/NADH Quantitation Colorimetric Kit propagation, myelin is also critical for trophic and metabolic support of axons [56]. To provide metabolites to axons accurately, glia must ‘know’ the metabolic requirements of axons. Could electrical

• Acarbose and voglibose the classic glucosidase inhibitors we

  2022-01-07

  

  Acarbose and voglibose, the classic α-glucosidase inhibitors, were clinically used to inhibit α-glucosidase activity for the treatment of type 2 diabetes. However, the intake of these drugs may cause some undesirable gastrointestinal side effects and weight gain (Xu et al., 2015). The synthetic drug

• br Clinical trials testing GLP mimetics in AD or

  2022-01-07

  

  Clinical trials testing GLP-1 mimetics in AD or PD patients GIP analogues show good neuroprotective effects in animal models of AD and PD Glucose-dependent insulinotropic polypeptide (GIP) is a 42-amino neuronal nitric oxide synthase incretin growth factor which activates pancreatic islets to

• ANP (1-11), rat The eradication of agonist activity

  2022-01-07

  

  The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary ANP (1-11), rat as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagoniz

• Our own search towards aryl imidazole derived GSMs led

  2022-01-07

  

  Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,

• br Conflicts of interests br Acknowledgements

  2022-01-07

  

  Conflicts of interests Acknowledgements We thank Drs. T. Tomita and T. Iwatsubo (Tokyo University, Tokyo, Japan) for anti-presenilin 1-CTF antiserum, Dr. A. Takashima (Gakushuin University, Tokyo, Japan) for anti-Pen-2 antiserum and the laboratory members for helpful comments and discussion. M

• br Introduction The mammalian skin forms the largest organ o

  2022-01-07

  

  Introduction The mammalian skin forms the largest organ of the body and includes a network of cutaneous nerves, cells of the immune system, and mediators of the neuro-endocrine axis (Theoharides et al., 2016). Analogous to the hypothalamic-pituitary-adrenal axis, neuropeptides and their receptors

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