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Dihydrofolate reductase DHFR is an
2021-01-22

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
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Collagen compaction and alignment are generated by cell medi
2021-01-22

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
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Henderson et al reported that allergen induced airway remode
2021-01-22

Henderson et al. [20] reported that allergen-induced airway remodeling was blocked by the CysLT1 receptor antagonist montelukast. The development of epithelial thickening and mucus accumulation at relatively small bronchi was also suppressed by montelukast. The CysLT2 receptor antagonist BayCysLT2R
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DDI is one of the main problems with
2021-01-22

DDI is one of the main problems with serious clinical consequences in clinical settings. Several reports have highlighted the role of modulation of drug-metabolizing enzymes, especially CYP450 s, as a major mechanism involved in clinical DDIs [3,4,7]. The present study aimed to investigate the effec
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br Clinical trials of CRM
2021-01-22

Clinical trials of CRM1 inhibitors KPT-330 clinical trials have been initiated with promising very early results. One trial includes patients with advanced solid tumors whose disease has progressed after at least one prior therapy for metastatic disease (NCT01607905). Another trial includes patie
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br Methods and materials br Cyclooxygenase COX
2021-01-22

Methods and materials Cyclooxygenase (COX) is the key enzyme required for the conversion of arachidonic NFAT Inhibitor synthesis to prostaglandin, prostacyclins and thromboxanes., , , Two distinct isoforms of COX were initially discovered: COX-1 is a constitutive, housekeeping enzyme that is
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Not all of the biological activities exhibited by progestoge
2021-01-22

Not all of the biological activities exhibited by progestogens (Table 1) are mediated via binding to SRs. For example, the anti-estrogenic action of progestogens in the Fmoc-Phe-OPfp is due to the progestogen-bound PR suppressing ER gene expression, and consequently the ability of the cell to respo
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br Acknowledgments br Significance The mechanisms underlying
2021-01-22

Acknowledgments Significance The mechanisms underlying the adverse effects of Epo-stimulating agents on the reduced survival of cancer patients are not well understood. Here, we identified EphB4 as an alternative Epo receptor, which triggers Src/Stat3 signaling via EphB4. We also showed that r
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Initial investigations in the heart uncovered Epac
2021-01-22

Initial investigations in the heart uncovered Epac as a positive regulator of myocyte hypertrophy [8], [9]. Concomitantly, Epac has been shown to regulate cardiac Ca homeostasis [8], [10], [11], [12], [13]. Ca is an essential second messenger in the cardiac physiology because its rhythmic variations
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br Acknowledgements br Introduction Three structurally relat
2021-01-22

Acknowledgements Introduction Three structurally related fungal metabolites have been isolated from chloroform extracts of submerged rice cultures of Aspergillus terreus 23-1 from stored unhulled rice in Taiwan; these were named territrems A–C to indicate their biological origin (A. terreus) a
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Lymphocyte mobility and homing is modulated by
2021-01-22

Lymphocyte mobility and homing is modulated by the chemoattractant receptor subfamily of G protein-coupled receptors (GPCRs) (Campbell et al., 2003, Rot and von Andrian, 2004). B cell migration and position are controlled to a large extent by the lymphoid chemokines CXCL13, CXCL12, CCL19, and CCL21
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br E E backside interaction The E possesses
2021-01-22

E3–E2 backside interaction The E2 possesses an important regulatory interface which is termed its backside as it is opposite to the catalytic cleft that bears the active-site cysteine forming the thioester with SUMOD. This backside site interacts noncovalently with a scaffold SUMOB and was origin
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Most enzymes involved in the addition and removal of
2021-01-22

Most 4-IPP involved in the addition and removal of ubiquitin bind weakly to an overlapping surface on ubiquitin. Previously, Sidhu and colleagues diversified this surface and then used phage display to screen these libraries of ubiquitin variants (UbVs) for binding to DUBs and E3 ligases (Ernst et
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br Authors contribution br Disclosure statement br Acknowled
2021-01-22

Authors contribution Disclosure statement Acknowledgements This study has received funding from the Italian Ministry of University and Research (PRIN 2015, grant number 2015373Z39_008) and from the Innovative Medicines Initiative 2 Joint Undertaking under grant agreement No 115797 (INNODIA)
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STF 083010 mg These data from developing brain are in contra
2021-01-22

These data from developing STF 083010 mg are in contrast to noradrenergic receptor regulation in the adult brain. In adult animals, a persistent increase in the α2-AR high affinity state is elicited as a result of DSP-4 lesion or reserpinization, as measured by [3H]clonidine binding to membrane prep
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