• Several enzymes in serine and glycine

  2024-08-26

  

  Several enzymes in serine and glycine metabolism have been proposed as biomarkers for cancer stage and prognosis. Phosphoglycerate dehydrogenase (PHGDH), phosphoserine phosphatase (PSPH), and serine hydroxymethyltransferase (SHMT) levels are high in TNBC and low in luminal-A breast cancers (Kim et a

• Heat shock protein Hsp is a molecular chaperone

  2024-08-26

  

  Heat shock protein 90 (Hsp90) is a molecular chaperone that plays a central role in regulating the maturation, activation and stability of numerous “client proteins” that drive the development and progression of many cancers. Therefore, inhibition of Hsp90 would result in degradation of the client p

• br AHR expression in cancer Perhaps the

  2024-08-26

  

  AHR expression in cancer Perhaps the earliest indicator that the AHR might play an ongoing role in tumorigenesis, independent of its role in generating mutations, was the demonstration that non-genotoxic 2,3,7,8-tetrachlorodibenzo(p)dioxin (TCDD) is a carcinogen in animals and humans [7]. Althoug

• In the late s Solvay

  2024-08-26

  

  In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the

• BMS-626529 Children with ADA SCID commonly suffer from a var

  2024-08-26

  

  Children with ADA-SCID commonly suffer from a variety of opportunistic infections, including viral, fungal, and mycobacterial infections. Due to defects in BMS-626529 and IG production, they are also susceptible to infection with encapsulated bacteria such as Haemophilus influenzae, Streptococcus p

• Sperm total motility and hyperactivated motility are

  2024-08-26

  

  Sperm total motility and hyperactivated motility are mediated by PLD-dependent bioactive polymerization [20]. Reduction of PIP2 synthesis inhibited actin polymerization and motility, and increasing PIP2 synthesis enhanced these activities. Furthermore, sperm demonstrating low motility contained low

• Targeting the BCR is the ideal strategy to

  2024-08-26

  

  Targeting the BCR is the ideal strategy to identify the antigen reactive B cells. However, there is concern that B cells could be activated when BCR are bound and cross-linked by antigens, a possibility that is obviously negative for the treatment of autoimmune disease. Proby et al. (2000) tried to

• It is already established in the literature that

  2024-08-26

  

  It is already established in the literature that products synthesized by 5-LO, such as lipoxin A4, can activate PPARγ in a setting of experimental stroke [43]. Interestingly, experiments using 5-LO knockout mice in an endotoxemia model to mimic septic conditions, demonstrated reduced multiple organ

• The first rationally designed dual mPGES LO inhibitor

  2024-08-26

  

  The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic CC-115 receptor - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been sy

• Finasteride has been shown to

  2024-08-26

  

  Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a

• Many metalloenzyme inhibitors consist of two chemical

  2024-08-26

  

  Many metalloenzyme inhibitors consist of two chemical components: the MBG, the portion of the inhibitor designed to bind to the metal, and the scaffold, the portion of the inhibitor recognized by the amino Thieno-GTP residues that form the substrate-binding site of the metalloenzyme. The MGB is oft

• As mentioned above variation of

  2024-08-26

  

  As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to N6-Methyl-dATP (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () having comparabl

• Small kinase inhibitors have been developed to block AXL by

  2024-08-26

  

  Small kinase inhibitors have been developed to block AXL by interacting with the kinase cytoplasmic ATP binding site. Up to date, no AXL selective kinase inhibitors are marketed. As depicted in , some marketed kinase inhibitors such as Bosutinib and Cabozantinib or kinase inhibitors in clinical pha

• br ASK in Huntington s disease and other polyglutamine disea

  2024-08-23

  

  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 Conclusion In conclusion the arginase from P

  2024-08-23

  

  Conclusion In conclusion, the arginase from P. aeruginosa IH2 was purified with electrophoretic homogeneity. Purified enzyme was homo-dimer and showed significant activity and catalytic stability near to the pH of circulating system and temperature of human body. The prolonged serum and proteolyt

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