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br Acknowledgement Work in the McEwan Laboratory is funded
2024-10-14
Acknowledgement Work in the McEwan Laboratory is funded by the Chief Scientist Office of Scottish Government: Grants ETM-258 and ETM-382. BE is supported by an Erasmus scholarship (D -JENA01). Introduction The equine placenta is a noninvasive transient organ, classified as diffuse and epithel
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br Conclusion We have identified three non competitive inhib
2024-10-14
Conclusion We have identified three non-competitive inhibitors of the human and porcine APN with Ki values in the μM range, by combining virtual screening and kinetic assays. Molecular docking simulations suggest these novel inhibitors block APN activity by an alternative mechanism to Zn coordina
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br Acknowledgments This work was supported by a grant of
2024-10-14
Acknowledgments This work was supported by a grant of the Romanian National Authority for Scientific Research, CNCS – UEFISCDI, project no. PN-II-ID-PCE-2011-3-0571, awarded to F.A.M. D.V.N. was co-financed from the European Social Fund through Sectorial Operational Program Human Resources Develo
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Considering our previous results with cfDNA in EGFR TKI
2024-10-14
Considering our previous results with cfDNA in EGFR TKI-resistant NSCLC patients and growing evidence about different mutations in the ALK kinase domain as responsible for acquired resistance to ALK TKIs, we planned this study. Even if a next-generation sequencing approach after PD during crizotini
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Ac-YVAD-CHO receptor To examine whether the interaction betw
2024-10-14
To examine whether the interaction between mGlu7 and α1-adrenergic receptors could be confirmed at a behavioural level, we performed the FST in mice. This test has value in predicting the antidepressant-like effect of drugs or environmental manipulations (Krishnan and Nestler, 2008, Krishnan and Nes
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Among all the compounds the novel L
2024-10-14
Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The no sodium salt receptor 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 = 1
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br Introduction ACK or Activated Cdc Associated Kinase
2024-10-12
Introduction ACK1, or Activated Cdc42-Associated Kinase, located on chromosome 3q, is a ubiquitously expressed non-receptor tyrosine kinase cloned from a human energy metabolism cDNA library (Manser et al., 1993). It was first identified to bind to activated Cdc42, a small Ras GTPase via its CRI
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br AD and COX LOX pharmacology
2024-10-12
AD and COX/5-LOX pharmacology Early studies on the role of cyclooxygenases in AD were inspired by epidemiological data suggesting that COX inhibitors such as nonsteroidal anti-inflammatory drugs (NSAIDs) could be beneficial in AD patients (Lucca et al., 1994, McGeer et al., 1990). This line of re
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Despite functional studies demonstrating the role of HT
2024-10-12
Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,
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Several tertiary prevention studies are currently
2024-10-12
Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Du
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br Identification of the kinase that phosphorylates P c
2024-10-12
Identification of the kinase that phosphorylates P450c17 The first Ser/Thr kinase that phosphorylates P450c17 was identified only recently. Of the 518 kinases in the human ‘kinome’ 278 are Ser/Thr kinases (Manning et al., 2002), but microarrays identified only 145 Ser/Thr kinases in human NCI-H29
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Optimization of the B ring specifically targeted
2024-10-12
Optimization of the B-ring specifically targeted preventing the oxidation of the ring system (). As described above, the 4-position of the phenyl ring provides the appropriate vector towards bulk solvent. - and -linked substitutions at the 4-position of the B-ring from the 4-fluoro-nitrophenyl inter
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What can we learn about the anticancer therapeutic efficacy
2024-10-12
What can we learn about the anticancer therapeutic efficacy of Aurora kinase inhibitors from our experience with the Bcr-Abl inhibitors and the long term clinical consequence of their use in treating leukemias? As discussed, all Aurora kinase inhibitors developed to date are ATP-competitive inhibito
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br Results and discussion br Conclusion A series
2024-10-12
Results and discussion Conclusion A series of aminobenzothiazole derivatives were investigated as possible Aurora B kinase inhibitors. Bioisosteric replacement of the heterocyclic core of the lead compound was performed regarding the docking analysis. Replacement of the oxygen ck1 inhibitor o
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Among the most important Ca regulatory mechanisms are the Pl
2024-10-12
Among the most important Ca regulatory mechanisms are the Plasma Membrane Calcium ATPase (PMCA) and Sarcoplasmic Reticulum Calcium ATPase (SERCA). These pumps belong to the family of P-ATPases, which share the formation of an acid-stable phosphorylated intermediate as part of their reaction cycle. P
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