• Our recent discovery M P H R A S

  2021-08-11

  

  Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w

• The three dimensional crystal structure of Ca

  2021-08-11

  

  The three-dimensional crystal structure of Ca2+ loaded CaM reveals a dumbbell-shaped molecule with two roughly globular lobes, the N- and C-terminal lobes linked by a long solvent-exposed helix, which has been shown by NMR to be non-helical in its central part and flexible in solution [13]. Each glo

• A small subset of compounds

  2021-08-11

  

  A small subset of compounds composed the 5-[1,2,4]triazino[5,6-]indole cluster (). This series of compounds was characterised by a central heterocyclic core with an R1 alkyl amine chain, required for potency (. , , and ), with preference for morpholine over piperidine (. ). The scaffold can be subst

• It has been shown that DAPK induces

  2021-08-10

  

  It has been shown that DAPK induces cell death through an increase in DAPK catalytic activity and subsequent phosphorylation of target proteins (Shang et al., 2005, Yamamoto et al., 2002), but its multidomain structure enables also a close physical interaction with other proteins (Bialik and Kimchi,

• In the present study it was

  2021-08-10

  

  In the present study, it was found that HepG2, H4IIE and LMH cells were inclined to remove S-metalaxyl and lead to decrease of ERs of metalaxyl, while L8824 cells were inclined to attenuate R-metalaxyl and resulted in an inverse shift of ER. These findings indicate the enantioselective accumulation

• 4-iodo-SAHA This work aimed to investigate whether the incre

  2021-08-10

  

  This work aimed to investigate whether the increase in liver lipid depots, observed in the fetuses from rats fed a saturated-fat-rich diet, persists later in life in the offspring (a) at 21days of age immediately after weaning and (b) at 140days of age, after healthy nourishing. Furthermore, we want

• To characterize Ea and S

  2021-08-10

  

  To characterize Ea and γ·S, DC/AC electrical parameters will be determined from MIL standard measurements in a temperature range of −55 to +200°C. It is therefore necessary also to characterize the junction temperatures and hot points by infra-red or electrical method. The accelerated aging, represe

• br Disclosure and conflicts of interest br Acknowledgements

  2021-08-10

  

  Disclosure and conflicts of interest Acknowledgements This research was supported by grant (BT/PR/11293/BRB/10/849/2008) from Department of Biotechnology (DBT), Government of India and a DST YOS Chair Professorship to PB. The mass spectrometry facility is supported by an institutional program

• Two isoforms of intracellular ER ER

  2021-08-10

  

  Two isoforms of intracellular ER, ERα, and ERβ, after binding to estrogens and translocate to the nucleus, activate some transcription factors and signaling pathways. The deregulation of estrogenic pathways can elevate transcriptional activity contributed to the development of cancer. Expression of

• br Genomic and non genomic signaling crosstalk

  2021-08-10

  

  Genomic and non-genomic signaling crosstalk As exemplified in the previous sections, it is evident that the mechanisms of action of estrogen in the various cell targets represent a combination of complex multifactorial processes. Besides the independent genomic and non-genomic pathways described

• Recent advances in microarray and next generation

  2021-08-10

  

  Recent advances in microarray [32] and next-generation sequencing [33] based technologies have led to tremendous increases in information about the molecular mechanisms that are responsible for malignant transformation of rare and poorly understood soft tissue sarcomas. However, data interpretation

• In a study performed simultaneously by another group EWS

  2021-08-10

  

  In a study performed simultaneously by another group, EWS-FLI-1 introduction into unsorted murine bone marrow-derived GSK J4 resulted in tumors with various phenotypes including one that is consistent with that of Ewing sarcoma [68]. The tumors expressed markers associated with Ewing sarcoma and di

• The effect of transformation of the linker Y between the

  2021-08-10

  

  The effect of transformation of the linker Y between the carboxylic hpdp residue and the phenyl moiety of 2b was also investigated, and is illustrated in Table 5. Analogs 2b, 16, and 17, possessing conformationally restricted carboxylic acid residues, tended to show stronger antagonist activity tha

• To identify and characterize new possible

  2021-08-10

  

  To identify and characterize new possible molecular targets, the mechanisms of various kinds of TCDD toxicities that occur by abnormal regulation in the downstream of AhR signals have been studied (Yoshioka et al., 2011). Experimental evidence has revealed that prostanoids (i.e., prostaglandins and

• The contribution of local ETA and

  2021-08-10

  

  The contribution of local ETA and ETB receptors towards heat hyperalgesia induced by inoculation of XC tumor AZD 8055 in the paw of mice has been demonstrated by Baamonde and colleagues (Baamonde et al., 2004). Furthermore, using neuropathic and inflammatory nociception models, several studies have

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