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Finasteride has been shown to be a
2024-12-02
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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Young disease transitioning B Sle mice show partial
2024-12-02
Young disease-transitioning B6·Sle1 mice show partial loss of leukocyte Axl versus B6 controls (data not shown). Further, BMDM from diseased B6·Sle1.Yaa mice do not express detectable levels of ADAM10 and TACE (ADAM17) but do express basal levels of Axl similar to wild type B6-derived BMDM (Suppleme
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The authors thank Dr J Aoki University of Tokyo
2024-12-02
The authors thank Dr. J. Aoki, University of Tokyo, for kindly providing 5E5-ATX antibody. This work was supported by a grant from the Deutsche Forschungsgemeinschaft to A.E.K. (KR4391/1-1), research grants “Primary sclerosing cholangitis” from the Deutsche Crohn-Colitis-Vereinigung and the Norwegia
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Endoplasmic reticulum ER stress resulting from accumulation
2024-12-02
Endoplasmic reticulum (ER) stress resulting from accumulation of misfolded proteins in ER lumen stimulates a chain of adaptive responses termed as the unfolded protein response (UPR). Glucose related protein (GRP78/BiP), key ER chaperone essential for the activation of the ER-transmembrane signaling
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Jesus et al discovered a
2024-12-02
Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified dhfr inhibitors 48 and 49 showe
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Song et al reported series of triazolylsalicylamide derivati
2024-12-02
Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se
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The Rv c EQ protein was purified from ml
2024-12-02
The Rv2477c-EQ2 protein was purified from 600 ml induced cultures following the same protocol described above. Elution of the mutant protein from the affinity resin was done using 200 mM imidazole. After concentration and buffer-exchange of protein as described above, the purity of the protein was c
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br Breast cancer The interactions between LOX and
2024-12-02
Breast cancer The interactions between 15-LOX and COX enzymes also affect the outcome of breast cancer. Indomethacin, a COX-1 and COX-2 inhibitor, decreased the growth of human breast cancer (BC) cells in nude mice, as well as slowed the rate of lung metastasis formation [41]. The levels of 12-HE
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The importance of the ATM
2024-12-02
The importance of the ATM/Tel1 to ATR/Mec1 switch in the response to DSBs remains to be determined. Noteworthy, resection-defective S. cerevisiae cells, such as sae2Δ, exo1Δ, fun30Δ or sgs1Δ mutants, fail to turn off the checkpoint in response to an unrepaired DSB [56], [127], [128]. Moreover, the s
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br Conclusion We present here
2024-12-02
Conclusion We present here the first comprehensive analysis of B-Raf-induced transcriptional activation in insulinoma cells. The B-Raf-induced signaling cascade targets the c-Fos and the c-Jun genes. Both gene products are constituents of the AP-1 transcription factor. The phosphatases MKP-1 and
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br Acknowledgments br Protein microarrays were developed to
2024-12-02
Acknowledgments Protein microarrays were developed to provide miniaturized high-throughput tools to study protein function, RGFP966 and post-translational modifications. Just a few years ago, the seminal work performed in Stuart Schreiber's laboratory at Harvard University () and at Michael Sny
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In addition unconventional mechanisms of
2024-12-02
In addition, unconventional mechanisms of internalization cannot be ignored. It is generally believed that the conventional homologous internalization of a GPCR depends on the activation of G proteins, since GRK activation requires the pre-activation of G proteins (Fig. 2). Feng et al. demonstrated
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br Materials and methods br Results br Discussion Knowledge
2024-11-29
Materials and methods Results Discussion Knowledge of the molecular basis of an inherited genetic disease is crucial for understanding the disease pathology and, ultimately, for therapeutic design. Several recent reports have stressed the need for physical characterization of disease-associ
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Furthermore stress hormones can indirectly induce DNA damage
2024-11-29
Furthermore, stress hormones can indirectly induce DNA damage, for example by altering DNA repair and transcriptional regulation of the cell cycle. It has been found that stress hormones induce the up-regulation of checkpoint kinase 1 (Chk1) and checkpoint kinase 2 (Chk2) and proto-oncogene cell div
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APPL was the first adaptor protein
2024-11-29
APPL1 was the first adaptor protein identified that interacts directly with adiponectin receptors [18]. A two-hybrid study by Dong and colleagues revealed that the C-terminal extracellular domain of AdipoR1 interacts with adiponectin, whereas the N-terminal cytoplasmic domain of AdipoR1 interacts wi
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