• A variety of quinazoline or fused pyrimidine substituted dia

  2024-03-08

  

  A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and

• Because of the formation of phosphoenzyme intermediates

  2024-03-08

  

  Because of the formation of phosphoenzyme intermediates, the enzymatic K-7174 of P-ATPases can be divided into steps that include a kinase activity, by which an aspartate residue on the enzyme is phosphorylated, and a phosphatase activity, by which the phosphoenzyme is dephosphorylated. Another comm

• Although the LB domains of mGlu receptors have not been

  2024-03-08

  

  Although the LB2 domains of mGlu receptors have not been shown to form an extensive interface during activation, they do draw closer to each other, as demonstrated in crystal structures (Kunishima et al., 2000, Muto et al., 2007, Tsuchiya et al., 2002) and by FRET analysis (Doumazane et al., 2013, V

• We have shown that an extensive region in

  2024-03-07

  

  We have shown that an extensive region in SERBP1 (amino acids 354 to 474, using co-ordinates based on the full-length isoform, Figs. 1a and 2) is necessary for it to interact with RACK1; since this region has substantial homology to the corresponding region of HABP1 (Fig. 3) it is a reasonable hypot

• br Concluding remarks br Conflict of interest br

  2024-03-07

  

  Concluding remarks Conflict of interest Acknowledgment This work was supported by the H.E.B. Endowed Chair in Marine Science (to P.T.) and University of Texas Marine Science Institute endowment-supported scholarships (to A.C). Introduction Disorders of sex development (DSD) are defined

• With regard to participation of the

  2024-03-07

  

  With regard to participation of the 12S-lipoxygenase in diabetes mellitus, inconsistent results have been obtained. Earlier studies demonstrated that the leukocyte-type 12S-lipoxygenase is specifically expressed in pancreatic b-cells and is involved in regulating glucose-stimulated insulin secretion

• br Conflict of interest statement br Introduction

  2024-03-07

  

  Conflict of interest statement Introduction The global prevalence of Alzheimer's disease (AD) is expected to increase to 106 million in 2050 from 30 million in 2010 (Brookmeyer et al., 2007), which will further impose a significant economic burden on health systems and society as a whole (Broo

• Polycyclic aromatic hydrocarbons PAHs are abundant

  2024-03-07

  

  Polycyclic aromatic hydrocarbons (PAHs) are abundant environmental contaminants that are produced by the incomplete combustion of organic matter, combustion engines, residential heating, Calmidazolium chloride burning, and industrial activities (Gelboin, 1980; Phillips, 1999, Phillips, 2002). Some

• The central problem in amnesia developing following impairme

  2024-03-07

  

  The central problem in amnesia developing following impairment of long-term memory consolidation or reconsolidation is a question of the underlying mechanisms, whether it is caused by impairment of retrieval or memory storage mechanisms [3,8,9,[15], [16], [17], [18]]. To answer this question, severa

• br AMPK structure and mechanism of action AMPK is

  2024-03-07

  

  AMPK: structure and mechanism of action AMPK is a metabolic master switch that regulates downstream signals based on shifts in the surrounding energy reservoir [6]. It is expressed in a number of tissues, including the kidney, the liver, the skeletal muscle, the adipose tissue, and the hypothalam

• br Introduction In myasthenia gravis MG autoantibodies

  2024-03-07

  

  Introduction In myasthenia gravis (MG), autoantibodies against the native AChR conformation cause loss of AChR at the neuromuscular junction and fatigable muscle weakness (Newsom-Davis et al., 1993). The AChR is a pentameric transmembrane protein, with two splice forms of the α-subunit, P3A− and

• br Conclusion There have been multiple clinical trials and p

  2024-03-07

  

  Conclusion There have been multiple clinical trials and pre-clinical studies that have tested the utility of 5ARIs in treating prostate disease, as summarized in Fig. 1. Inhibiting androgen action through the use of finasteride and dutasteride has been established as a valuable resource for physi

• An AXL decoy receptor with enhanced GAS binding properties

  2024-03-07

  

  An AXL decoy receptor with enhanced GAS6-binding properties, MYD1, was engineered as a therapeutic tool to disrupt GAS6/AXL signaling in vivo (Kariolis et al., 2014). MYD1 was shown to block metastasis of human ovarian cancer SKF38393 HCl synthesis and a murine breast cancer cell line in grafting a

• br Author contributions br Conflicts of interest The authors

  2024-03-06

  

  Author contributions Conflicts of interest The authors declare no competing financial interests. Acknowledgement This work was supported by grants from the Deutsche Forschungsgemeinschaft (Sonderforschungsbereich/Transregio 166–Project C1 and grant CA 1014/1-1 to D.C.) and the IZKF Würzbur

• Most human diseases e g cancer diabetes

  2024-03-06

  

  Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te

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