• br STAR Methods br Acknowledgments We thank Prof Y

  2022-01-18

  

  STAR★Methods Acknowledgments We thank Prof. Y. Tomari at the University of Tokyo for experimental advice and K. Hanada for technical assistance. This research was supported by Grants-in-Aid for Scientific Research on Innovative Areas “Nascent Chain Biology” (JP15H01548 and JP17H05677 to T.I. a

• The compounds f and a e were found to

  2022-01-18

  

  The compounds 8f and 9a–e were found to be potent inhibitors of both isoforms of GSK-3 as characterized by IC50 values in the low nanomolar range. In addition, all of them showed good selectivities against other kinases. Substituents in the ortho- and para-positions of structure 8 and 9 lead to pote

• R R MNF is a unique bitopic agent

  2022-01-18

  

  (R,R′)-MNF is a unique bitopic agent with selective and potent β2AR agonistic and GPR55 inhibitory properties [10], [11] that are independently associated with the drug's anti-mitotic and anti-tumorigenic actions. In 1321N1, U118MG, and melanoma cell lines, (R,R′)-MNF activation of the β2AR decrease

• The atherosclerosis development requires additional pro infl

  2022-01-18

  

  The atherosclerosis development requires additional pro-inflammatory response in the vascular tissue, promoting increased levels of adhesion molecules such as VCAM-1 (vascular cell adhesion molecule-1) and ICAM-1 (intercellular adhesion molecule-1). Cytokines such as TNF-α and IL-1β are able to upre

• Additionally OsGly I overexpressing transgenic rice plants

  2022-01-18

  

  Additionally, OsGly I-overexpressing transgenic rice plants had higher grain yields than WT (Table 2). Although there were no significant differences in the number of effective panicles per plant, panicle length, grain numbers per panicle, or 1000-grain weight between WT and transgenic plants, the s

• A general synthesis of the tetrazole is shown in

  2022-01-18

  

  A general synthesis of the tetrazole is shown in . First, a magnesium-halogen exchange reaction quenched with DMF afforded benzo[]thiophene-5-carbaldehyde , which was further decorated with a bromine at the 3-position (). A Suzuki reaction with -tolylboronic reductase enzyme followed by reduction

• Some aspects of intercellular Ca wave

  2022-01-18

  

  Some aspects of intercellular Ca2+ wave spread are similar to the phenomenon of spreading depression and associated with migraine headache [57]. These depolarization waves, followed by electrical inhibition, are evoked by transient hypoxia and other types of csf-1r injury and spread slowly across t

• In summary the SAR of a series of phenylpropanoic acid

  2022-01-18

  

  In summary, the SAR of a series of phenylpropanoic acid-free fatty BINA receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust efficacy in

• br Materials and methods br Acknowledgments We are grateful

  2022-01-18

  

  Materials and methods Acknowledgments We are grateful for financial support from the National Natural Science Foundation of China (Grants No. 81661148046 and 81773762, China) and the “Personalized Medicines—Molecular Signature-based Drug Discovery and Development”, Strategic Priority Research

• Because AM had limited efficacy on rodent GPR

  2022-01-18

  

  Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to

• br Materials and methods br Results br Discussion Several st

  2022-01-18

  

  Materials and methods Results Discussion Several studies highlighted an improvement of glycaemic control in diabetic patients receiving sunitinib, while the underlying mechanism remained still elusive [3], [4], [5], [6], [8]. The present study gives evidence that sunitinib directly and spec

• br Acknowledgements We thank Dr Bhushan Nagar and Dr Albert

  2022-01-18

  

  Acknowledgements We thank Dr. Bhushan Nagar and Dr. Albert Berghuis for access to the X-ray diffraction machine at McGill University. We also thank Dr. Manon Couture and Dr. Steve Charette at Université Laval for access to scientific equipment. Funding for this research was provided by Discovery

• The current lack of effective treatments for primary

  2022-01-18

  

  The current lack of effective treatments for primary or metastatic UM leaves a large therapeutic gap for patients and clinicians underscoring an urgent need for the identification of additional pharmacological targets for therapeutic intervention. As YAP-targeting strategies have remained elusive th

• br The inhibitory effect of ATP B knockdown on lysosomal

  2022-01-17

  

  The inhibitory effect of ATP7B knockdown on lysosomal exocytosis is likely mediated by the resulting oxidative stress induced by Cu, as exposure to oxidative stress induced by tert-Butyl hydroperoxide (TBHP) inhibited β-hex exocytosis as well, indicating that oxidative stress inhibits lysosomal ex

• The molecular mechanism of gliotransmitter release is not

  2022-01-17

  

  The molecular mechanism of gliotransmitter release is not fully understood until now, and previous studies have emphasized that the elevation of [Ca2+]i triggers vesicular 1 646 of glutamate. Parpura et al. reported that the essential role of Ca2+ release from internal stores in glutamate release.

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