• The most significant finding was the inhibition

  2020-01-03

  

  The most significant finding was the inhibition of EROD and BFCOD activity by CLO. Inhibition of EROD and BFCOD were reversible, as pre-incubation did not enhance CLO inhibitory potency, and no reductions in IC50 values were observed. We further characterized the kinetic pattern of inhibition using

• Three kinase inhibitors dasatinib type I imatinib

  2020-01-02

  

  Three kinase inhibitors dasatinib (type I), imatinib (type II) and nilotinib (type II), identified initially as inhibitors of tyrosine kinase BCR-ABL, were found to target DDRs in a chemical proteomic profiling study (Bantscheff et al., 2007, Hantschel et al., 2008). These tyrosine kinase inhibitors

• Like all other cellular processes ubiquitination is also tig

  2020-01-02

  

  Like all other cellular processes, ubiquitination is also tightly regulated; more so, as myriads of pathways are controlled via this conjugation and dysregulation of ubiquitination has been implicated in various diseases including cancer [16], [17]. Quite a few of such regulatory mechanisms that con

• Against this backdrop we set out

  2020-01-02

  

  Against this backdrop, we set out to identify synthetic and endogenous ligands that bind directly to and regulate the activity of Nurr1. Owing to the pivotal role Nurr1 plays in producing and processing dopamine, and the need for neurons to tightly regulate dopamine levels, we postulated that the re

• ATRX belongs to the switch sucrose non fermenting

  2020-01-02

  

  ATRX belongs to the switch/sucrose non-fermenting (SWI/SNF) chromatin remodeling family, mutations in which cause syndromal mental retardation and downregulation of α-globin expression (Gibbons et al., 1995). Most of these mutations are located in two highly conserved regions of the ATRX protein: a

• br Author Contributions br Acknowledgments

  2020-01-02

  

  Author Contributions Acknowledgments Introduction Many anticancer agents bind covalently to DNA, introduce bulky adducts, and inhibit DNA metabolic processes including repair, replication and transcription.1., 2., 3. Frequently, the first enzymes to encounter DNA adducts are DNA helicases.

• br Enzymes involved in microbial steroid degradation are gen

  2020-01-02

  

  Enzymes involved in microbial steroid degradation are generally not expressed constitutively, but they are upregulated depending on which steroid substrates are present [17,81]. Thus, a cell-free extract prepared from testosterone-adapted C. testosteroni ATCC 11996 cells displayed a 1(2)-dehydroge

• Pulmonary fibroblasts can regulate the wound

  2020-01-02

  

  Pulmonary fibroblasts can regulate the wound healing process by secreting and processing extracellular matrix (ECM), chemokines, and cytokines. However, persistent and atypical fibroblast proliferation can result in ECM accumulation and may trigger the onset or development of pulmonary fibrosis [[17

• The IL family consists of nine related molecules IL

  2020-01-02

  

  The IL-10 family consists of nine related molecules: IL-10, IL-19, IL-20, IL-22, IL-24, IL-26, IL-28α, IL-28β, and IL-29 [34]. These molecules have a somewhat conserved primary structure and contain a core of hydrophobic HET0016 and two pairs of disulfide bonds in the chain, giving them a similar s

• CYP A is involved in the metabolism

  2020-01-02

  

  CYP3A is involved in the metabolism of approximately 50% of all drugs that are currently prescribed to patients [1], [15], [16]. Marked interindividual variabilitity of the catalytic function for metabolizing CYP3A substrates has been demonstrated with variability exceeding 20-fold [1]. Levonorgestr

• CPG a metalloenzyme derived from sp was the

  2020-01-02

  

  CPG2, a metalloenzyme derived from sp., was the elected enzyme for the first pilot-scale clinical trial of ADEPT. This enzyme has no mammalian homologue and activates glutamic Natural Product Library receptor prodrug derivatives of several nitrogen mustards alkylating agents., , , , , A bond clea

• In conclusion this study provides the first investigation of

  2020-01-02

  

  In conclusion, this study provides the first investigation of role of ACC receptors in parasitic nematodes. While research using C. elegans to evaluate anthelmintic targets is an excellent tool to provide relevant information, research on similar targets in parasitic nematode can provide key informa

• How does an increase in E affinity for the RING

  2019-12-31

  

  How does an increase in E2 affinity for the RING domain favor higher activity and polyubiquitination by the E2? Binding of the RING domain to the E2 positions the donor Ub in the E2~Ub conjugate in a closed complex [16], [17], [18] that increases the reactivity of the thioester [60]. A higher affini

• br Materials and Methods br Acknowledgements Authors would l

  2019-12-31

  

  Materials and Methods Acknowledgements Authors would like to thank Mr. Pritam Naskar and Mr. Dibya Mukherjee for their help. Authors also acknowledge the help of Mr. Barun Mahata and Dr. Kaushik Biswas, Division of Molecular Medicine, Bose Institute, for human cDNA samples. P.A.B. and A.B.D. w

• br Results and discussion br Conclusion We have constructed

  2019-12-31

  

  Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz

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