• Recently several Pt IV complexes as prodrugs

  2021-02-19

  

  Recently, several Pt(IV) complexes as prodrugs have been designed and studied to enhance anti-tumor efficacy of traditional Pt(II) drugs, improving their cellular uptake and blood-circulation time [26], [27], [28], [29]. Compared with their Pt(II) counterparts, six-coordinated Pt(IV) complexes with

• br Conflicts of interest br

  2021-02-19

  

  Conflicts of interest Author contributions Acknowledgements This work was supported by the University of Brescia (ex 60%) and Siderurgica Leonessa research funds to AF. RR was supported by Associazione Italiana per la Ricerca sul Cancro - AIRC (MFAG 18459 grant). We are grateful to Umberto

• br Oxidoreductase like MEM for prodrug activation br Future

  2021-02-18

  

  Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2

• To study the effect of DDR inhibition

  2021-02-18

  

  To study the effect of DDR inhibition by imatinib, nilotinib and dasatinib in a cellular environment we generated DDR1 and DDR2 expressing HEK293 cell lines by stable transfection. Of the five DDR1 splice variants we focused on the 1b variant whose over-expression has been associated with pulmonary

• Initially the E uses ATP to activate the

  2021-02-18

  

  Initially, the E1 uses ATP to activate the C-terminal glycine residue of ubiquitin prior to ligation. In the first step of E1 activation, the E1 catalyzes the adenylation of ubiquitin and pyrophosphate (PPi) release. In the second step, the E1 releases adenosine monophosphate (AMP) and a thioester b

• Inhibition of DHODH is reflected by

  2021-02-16

  

  Inhibition of DHODH is reflected by an antiproliferative effect on peripheral blood mononuclear N1-Methylpseudo-UTP mg (PBMCs), which can be measured by the inhibitory effect on their phytohemagglutinin (PHA) stimulated growth. The test was performed as described in the reference. Data for few selec

• Collagen compaction and alignment are

  2021-02-16

  

  Collagen compaction and alignment are generated by cell-mediated contractile forces (Stopak and Harris, 1982). The transmission of actomyosin forces to collagen has been mainly attributed to integrins and the activation of the Rho-ROCK pathway (Clark et al., 2007, Kural and Billiar, 2013, Provenzano

• AVL-292 DDR was originally cloned by the group of Michele

  2021-02-16

  

  DDR1 was originally cloned by the group of Michele de Luca, at the time named TrkE. The Genoa-based research team identified the skin, and the keratinocytes in particular, as a major site of DDR1-binding activity [20]. DDR1 is also expressed in kidney, liver and lung (Fig. 2). The functional role of

• The IP R is a

  2021-02-16

  

  The IP3R is a ubiquitously expressed Ca2+-release channel from the ER, activated by IP3, produced upon cellular stimulation by hormones, growth factors or neurotransmitters. Three genes are coding for the IP3R and their gene products (IP3R1, IP3R2, IP3R3) assemble in functional homo- or heterotetram

• CXCL mediated cell migration is facilitated

  2021-02-16

  

  CXCL16 mediated cell migration is facilitated by the interaction of soluble CXCL16 with CXCR6, expressed predominantly on the cell surface of CD4+ Th1 cells, cancer infiltrating lymphocytes and platelets (Borst et al., 2012, Kim et al., 2001, Liao et al., 1997, Wilbanks et al., 2001). CXCR6 is invol

• The estrogenic activity of steroids with a C methyl group

  2021-02-15

  

  The estrogenic activity of steroids with a C19 methyl group may provide a selective advantage in estrogen physiology that is not provided by E2. In this regard, 5α-androstanediol has been proposed to be a second physiological estrogen in fetal mouse ixabepilone based on the timing of ERβ synthesis

• To study systemic potential of the selected compounds as

  2021-02-15

  

  To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,

• In conclusion substrate enabled effective detection of L ala

  2021-02-15

  

  In conclusion, substrate enabled effective detection of L-alanylaminopeptidase activity in all Gram-negative bacteria tested here. The chromogenic substrate showed high sensitivity at a relatively low concentration (50 mgL), with no diffusion of the coloured chelate into the surrounding agar. Lack

• Regarding eicosanoid production iPLA VIA appears in general

  2021-02-15

  

  Regarding eicosanoid production, iPLA2-VIA appears, in general terms, not to play a major role in mediating this response in innate immunity and inflammation, as evidenced by the large number of studies highlighting the lack of effect of selective inhibition of the enzyme in stimulus-induced AA rele

• The loss of secondary mutation T M mutation after

  2021-02-12

  

  The loss of secondary mutation T790M mutation after AR and SCLC transformation was also reported for Rociletinib. Piotrowska et al. using the MGH NGS platform recently reported in 13 biopsies among 12 EGFR T790M+ patients progressing after treatment with Rociletinib the loss of EGFR T790M mutation

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