• In conclusion we have demonstrated that

  2024-01-11

  

  In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi

• A high throughput small molecule

  2024-01-11

  

  A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found dacomitinib to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was per

• Molecular simulation has proven useful

  2024-01-10

  

  Molecular simulation has proven useful in describing the dynamics and energetics of NMDA receptor LBD cleft closure and the potentiating role of glycans (Yao et al., 2013, Dai and Zhou, 2013, Dai and Zhou, 2015, Dai and Zhou, 2016, Dutta et al., 2015, Omotuyi and Ueda, 2015, Sinitskiy and Pande, 201

• VEGFR inhibition using sunitinib does

  2024-01-10

  

  VEGFR2 inhibition using sunitinib does not result in tumor growth reduction or in a further decrease in vessel density in NDRG1 overexpressing glioma rendering these tumors intrinsically resistant to antiangiogenic treatment. Intrinsic resistance to antiangiogenic therapy is defined as a non-respons

• (+)-Apogossypol It was reported that oral administration of

  2024-01-10

  

  It was reported that oral administration of CSZ to C57BL/6J mice significantly improved spatial learning and memory, and prevented Aβ-induced immunoresponse in Aβ25-35-injected mice. However, post-treatment with CSZ after Aβ25-35 administration, when Aβ was already accumulated, did not prevent Aβ-in

• Perhaps the first evidence of AMPKs therapeutic ability in

  2024-01-10

  

  Perhaps the first evidence of AMPKs therapeutic ability in DM1 came from Thomas Cooper’s laboratory where they demonstrated that insulin-independent glucose uptake was unaffected in human DM1 muscle Sulfo-NHS-Biotin treated with MET, an AMPK activator and first-line therapy for type 2 diabetes mell

• Histochemical analyses using antibody or cDNA probes reveal

  2024-01-10

  

  Histochemical analyses using antibody or cDNA probes reveal the precise cellular location of the 12S-lipoxygenases in tissues of interest. An immunohistochemical study in various rat tissues showed specific expression of the leukocyte-type 12S-lipoxygenase in macrophages in lung and spleen [27]. In

• br Special report Financial and personal benefits of early d

  2024-01-10

  

  Special report – Financial and personal benefits of early diagnosis Acknowledgments The Alzheimer’s Association acknowledges the contributions of Joseph Gaugler, Ph.D., Bryan James, Ph.D., Tricia Johnson, Ph.D., Allison Marin, Ph.D., and Jennifer Weuve, M.P.H., Sc.D., in the preparation of 201

• Aldose reductase ALR EC the first enzyme in the polyol

  2024-01-10

  

  Aldose reductase (ALR2, EC1.1.1.21), the first enzyme in the polyol pathway, is a monomeric oxidoreductase that catalyses the NADPH-dependent reduction of a wide variety of carbonyl compounds, especially glucose. In this metabolism pathway, glucose is firstly reduced to sorbitol catalyzed by ALR2 wi

• Lithocholic Acid receptor Acetaminophen N acetyl p aminophen

  2024-01-10

  

  Acetaminophen (N-acetyl-p-aminophenol, AAP) (Fig. 1) is a medically important, low cost, readily available and commonly used over the counter analgesic and antipyretic drug [18,19]. Acetaminophen monotherapy is efficient and is safer than Aspirin and Ibuprofen [20]. The efficacy and tolerability in

• To date more than different mutations in the gene have

  2024-01-09

  

  To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su

• Regarding androgens it is known that they are also essential

  2024-01-09

  

  Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco

• retinoid x receptor On another hand pyrazoles are widely

  2024-01-09

  

  On another hand, pyrazoles, are widely found as the core structure in a large variety of compounds of great biological and pharmaceutical value exhibiting anti-HCV [11], antitumor [12], cytotoxic[13], and antioxidant activities [14]. Finally, 1,2,3-triazoles have attracted the interest of medicinal

• HT modulates cortical and hippocampal pyramidal cell functio

  2024-01-09

  

  5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal WWL 70 as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et al., 2015,

• br Funding br Introduction l Dihydroxyphenylalanine l DOPA i

  2024-01-09

  

  Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side

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