• dinaciclib In the nineties we knew

  2023-10-19

  

  In the nineties we knew that (-)baclofen was the stereo-selective ligand for the GABAB receptor which had been recognised by Norman Bowery as a receptor for GABA, which was different from the GABAA receptor (Hill and Bowery, 1981). GABAB receptor antagonists were also synthesised and made available

• br ASK in Huntington s disease

  2023-10-19

  

  ASK1 in Huntington's disease and other polyglutamine diseases The polyglutamine (polyQ) diseases are a group of inherited neurodegenerative disorders caused by the expansion of cytosine-adenine-guanine (CAG) trinucleotide repeats in the coding regions of specific genes, leading to the production

• br Experimental section br Acknowledgments br Introduction A

  2023-10-19

  

  Experimental section Acknowledgments Introduction Adipose is a major endocrine organ which releases a range of bioactive agents [1]. Selected adipose depots have been established as sites of sex steroid metabolism [1]. Subcutaneous and visceral adipose express high levels of aromatase, cap

• br Introduction Diabetes mellitus DM

  2023-10-18

  

  Introduction Diabetes mellitus (DM) is a chronic metabolic disorder characterized by elevated levels of glucose in the blood. Type 1 diabetes is characterized by insufficient insulin production and needs a daily administration of insulin. Actually, no prevention is known for Type 1 diabetes. Type

• Gratifyingly compound also demonstrated improved physicochem

  2023-10-18

  

  Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and

• br ABCA modulates intracellular sphingolipid metabolism in t

  2023-10-18

  

  ABCA2 modulates intracellular sphingolipid metabolism in the LE/LY Recycling of plasma membrane lipids that occurs by constitutive endocytosis and vesicularization of complex glycolipids, complex sphingolipids and cholesterol as well as free cholesterol liberated from LDL after receptor-mediated

• Application of the broad acting HTR antagonist methiothepin

  2023-10-18

  

  Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L

• Tacrine an aminoacridine derivative Fig A was the first AChE

  2023-10-18

  

  Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t

• Caffeic acid dihydroxycinnamic acid is a natural

  2023-10-18

  

  Caffeic Fmoc-Gly-OH (3,4-dihydroxycinnamic acid) is a natural compound that inhibits 5-LO and exerts potent anti-inflammatory and antioxidant properties. Recently, Takeda et al. reported that caffeic acid provided neuroprotective and anti-depressive activities [23]. Sertraline, a selective serotonin

• Previously we reported that EL Kras mice

  2023-10-18

  

  Previously, we reported that EL-Kras mice-fed diets rich in omega-6 FAs demonstrated increased pancreatic mast cell infiltration [16]. Significantly, increased infiltration of mast cells into the tumor microenvironment correlates with a poor prognosis [15]. Soucek et al.[25] demonstrated that mast c

• br Acknowledgements We thank Dr Stefan Schulte Merker

  2023-10-18

  

  Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific

• Our research is the first to report

  2023-10-18

  

  Our research is the first to report that administration of HMW-HA is an effective strategy to defend against PM2.5-induced disruption of pulmonary epithelial barrier and lung injury, and addresses that HMW-HA restricts PM2.5-induced epithelial apoptosis through reducing oxidative stress and followin

• Antioxidative enzymes such as SOD and CAT

  2023-10-18

  

  Antioxidative enzymes such as SOD and CAT play prominent roles in protecting against oxidative stress and extending food freshness due to their ability in scavenging active oxygen species for maintaining cell membrane integrity. Evidence shows that activities of SOD and CAT are positively affected b

• It remains unclear to what extent UCP and UCP are

  2023-10-17

  

  It remains unclear to what extent UCP2 and UCP3 are subject to the same acute molecular regulation as UCP1 (and the extent to which they share the same mechanism of uncoupling). Although they lack sequence homology in a matrix-localised region reportedly critical for fatty 5 03 activation of UCP1 [

• With wide spread use of

  2023-10-17

  

  With wide-spread use of corticosteroids to combat inflammation and allergies, even children are susceptible to corticosteroid-induced muscle wasting. Although non-steroidal SGRMs that spare muscle and bone, but have significant anti-inflammatory effects, have been preclinically developed and tested,

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