• Recently several Pt IV complexes as prodrugs have been desig

  2021-08-27

  

  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 Criteria for ER targeted fluorescent probes br Survey of

  2021-08-27

  

  Criteria for ER-targeted fluorescent probes Survey of fluorescent probes Proposed approach to high affinity fluorescent steroidal ER probes Our proposed approach to the development of a new generation of fluorescent estrogen receptor imaging agents employs many of the elements present in th

• It is of interest that an

  2021-08-27

  

  It is of interest that an initial maternal experience in virgin mice produces both changes in subsequent maternal behavior as well as possible changes in neural gene expression. Stolzenberg et al. (2012) proposed that experience-based changes in maternal responsiveness may be mediated by chromatin m

• The mechanisms by which coregulators control the actions of

  2021-08-27

  

  The mechanisms by which coregulators control the actions of estrogen receptors are still a topic of ongoing research. From studies in cancer cells, we have learned that a large group of coregulators have specific structural motifs that than affect their contact with ER ligand-binding domains (Heery,

• br Conflicts of interest br Author

  2021-08-27

  

  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

• Accumulating evidence suggests that certain

  2021-08-27

  

  Accumulating evidence suggests that certain abnormal emotional traits, such as impulsive aggression and cluster B personality, are associated with suicidal behaviors (Currier and Mann, 2008, Mann et al., 2009, Rujescu et al., 2007, Turecki, 2005). Impulsive aggression appeared to be associated with

• br E mediated E discharge E ligases

  2021-08-26

  

  E3-mediated E2 discharge E3 ligases simultaneously interact with the substrate and the SUMOD charged E2 enzyme to catalyze the discharge of the thioester-bound SUMOD from the E2 to the substrate. E3 interaction with SUMOD via a SIM results in a closed conformation which is highly reactive and lea

• Twin studies have shown that P

  2021-08-26

  

  Twin studies have shown that P has moderate heritability. Zuckerman (1989) reviewed the earlier studies of P or related traits and found a median heritability of 0.51. However, twin studies using an Eysenckian P scale have tended to estimate somewhat lower heritabilities than this, in the range 0.36

• It is currently believed that acute morphine administration

  2021-08-26

  

  It is currently believed that acute morphine administration can impair learning and memory (Friswell et al., 2008). Chronic morphine treatment can also impair access to and retention of spatial memory (Spain and Newsom, 1991, Zheng et al., 2002). Using the Morris water maze experiment, we have previ

• We have reported previously that

  2021-08-26

  

  We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHOD

• Tacrolimus Dihydrofolate reductase DHFR is an excellent mole

  2021-08-26

  

  Dihydrofolate reductase (DHFR) is an excellent molecular target for this study because it has been and is currently studied by using different molecular modeling techniques [6], [7], [8], [9]. Kerrigan et al. have reported an interesting review about recent progress in molecular dynamics simulations

• Elevated production of cysLTs in asthma and rhinitis in

  2021-08-26

  

  Elevated production of cysLTs in Epothilone D and rhinitis in general and aspirin-sensitive disease in particular10, 11, 26, 27 has been implicated in causing epithelial cell activation and excessive mucus secretion, which characterize these diseases.2, 28 It is of particular interest, therefore, th

• LY364947 br Materials and methods br

  2021-08-26

  

  Materials and methods Results Discussion In this study, we developed a new CysLT1 and CysLT2 receptors-mediated LY364947 guinea pig model for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. Unlike human CysLT2 receptors, which are equally stimulated by both LTC4 and LTD4[

• br Acknowledgements We thank Jeffrey D Konowalchuk and John

  2021-08-26

  

  Acknowledgements We thank Jeffrey D. Konowalchuk and John Sony Robbins for their technical assistance. This work was supported by Natural Sciences and Engineering Research Council of Canada (NSERC) grants to DRB (RGPIN-2013-355303) and MB (RGPIN-2014-96395). AMR was supported by NSERC Vanier Doct

• br Conclusion The preclinical data reported

  2021-08-26

  

  Conclusion The preclinical data reported in this study shows that LAS191859 is a potent and safe CRTh2 antagonist, with a long receptor residence time that provides a sustained in vivo efficacy. This property is reflected in the prolonged duration of action of LAS191859 in in vitro and in vivo fu

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