• The interface between the E ligase and the

  2021-05-05

  

  The interface between the E3 ligase and the E2 enzyme can vary, and ZNF451 and SP-RING ligases stabilize this interaction via noncovalent binding to a scaffold SUMO (SUMOB) on the backside of the E2 (Cappadocia et al., 2015; Eisenhardt et al., 2015; Streich & Lima, 2016). By contrast, RanBP2 does no

• gpr119 agonist Everolimus treatment showed an increase in th

  2021-05-05

  

  Everolimus treatment showed an increase in the number of plaques and a reduction in plaque size, depending on concentration and treatment time (Fig. 1, Fig. 2). Everolimus-pretreated gpr119 agonist adsorbed less virus with more plaque formation in the initial phase of infection (Fig. 3). The abilit

• Hedamycin isolated from Streptomyces griseoruber belongs to

  2021-05-05

  

  Hedamycin, isolated from Streptomyces griseoruber, belongs to the highly cytotoxic pluramycin class of egfr inhibitor (Figure 3(c)). It consists of a planar anthrapyrantrione chromophore attached to two amino sugar rings at one end and a bisepoxide-containing side-chain at the other end (Figure 3(c

• br Introduction Although not fully understood the molecular

  2021-05-05

  

  Introduction Although not fully understood, the molecular toxicology of sulfur mustard (bis(2-chloroethyl)sulfide, SM; CAS–Nr. 505-60-2), an alkylating warfare agent, has been attributed to DNA alkylation [1], [2], [3]. The same principle holds true for other alkylating compounds such as nitrogen

• br Fragment based drug discovery FBDD is a powerful method

  2021-05-05

  

  Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical Pentamidine space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It

• br Acknowledgements br Introduction Chemokines are a superfa

  2021-05-05

  

  Acknowledgements Introduction Chemokines are a superfamily of chemotactic cytokines that play important roles in regulating cell migration and activation under inflammatory conditions (Nomiyama et al., 2008; Peatman and Liu, 2007; Zlotnik and Yoshie, 2000), such as angiogenesis (Arenberg et al

• In the course of carbohydrate metabolism pyruvate the end

  2021-04-30

  

  In the course of carbohydrate metabolism, pyruvate, the end product of glycolysis, is converted to acetyl-CoA, which fuels the citrate cycle for further generation of energy. In the case of elevated levels of acetyl-CoA, acetyl-CoA is converted into malonyl-CoA by the action of acetyl-CoA carboxylas

• In some pancreatic and non pancreatic tissues the chloride

  2021-04-30

  

  In some pancreatic and non-pancreatic tissues, the chloride and calcium channels are heavily regulated by phosphorylation by protein kinases, such as PKC, cyclic AMP-dependent protein kinase (PKA), PKCaMKII, PI3K and protein tyrosine kinases [7,36,37]. Since the interaction of triterpenes with recep

• br Introduction Receptor tyrosine kinases RTKs are criticall

  2021-04-30

  

  Introduction Receptor tyrosine kinases (RTKs) are critically involved in the development and progression of human cancers and are therefore useful targets for anti-cancer therapies [1]. The Eph receptors represent the largest subfamily of receptor protein kinases and interact with ligands called

• For most enolases fluoride acts as an inhibitor while Mg

  2021-04-30

  

  For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby

• The isomeric phenyloxazole not only exhibited increased pote

  2021-04-30

  

  The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand rosavin synthesis (as seen in compound pairs – and –) decre

• In this study we implicate SCFFBXO E ligase as a

  2021-04-30

  

  In this study, we implicate SCFFBXO3 E3 ligase as a critical modulator of inflammation in atherosclerosis and demonstrate the efficacy of a small molecule FBXO3 inhibitor in suppressing inflammatory responses important in atherosclerosis. Specifically, individuals carrying a hypofunctioning genetic

• Till date several predictive models

  2021-04-30

  

  Till date, several predictive models have been developed by different research groups to speed up the process of library selection and drug optimization (Walters et al., 1999, Caldwell, 2000, Plewczynski et al., 2006, Wang and Ramnarayan, 1999, Pogorelcnik et al., 2015, Greenbaum et al., 2002, Sadow

• An AmDH is engineered by

  2021-04-30

  

  An AmDH is engineered by mutating two conserved amino np e residues in the active site of an amino acid dehydrogenase (AADH). Starting from the leucine dehydrogenase (LeuDH) from Bacillus stearothermophilus, substituting a serine and leucine at the K68 and N261 positions, respectively, resulted in

• Interestingly genome wide association studies have linked th

  2021-04-30

  

  Interestingly, genome-wide association studies have linked the chromosomal region harboring RDHE2 (SDR16C5) and seven other genes to stature and growth in cattle, humans, and pigs [30], [31], [32], [33], [34], [35], [36], [37], and beak deformity in chickens [38]. The most recent study specifically

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