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61.
Singh Archana Singh Sujata Singh Ragini Kumar Sumit Singh Sanjay Kumar Singh Indrakant Kumar 《Functional & integrative genomics》2021,21(5-6):571-592
Functional & Integrative Genomics - Zea mays defense response is well-crafted according to the physical and chemical weapons utilized by their invaders during the coevolutionary period. Maize... 相似文献
62.
Vito W. Rebecca Renato R. Massaro Inna V. Fedorenko Vernon K. Sondak Alexander R. A. Anderson Eunjung Kim Ravi K. Amaravadi Silvya S. Maria‐Engler Jane L. Messina Geoffrey T. Gibney Ragini R. Kudchadkar Keiran S. M. Smalley 《Pigment cell & melanoma research》2014,27(3):465-478
This study investigates the mechanism of action behind the long‐term responses (12–16 months) of two BRAF WT melanoma patients to the AKT inhibitor MK‐2206 in combination with paclitaxel and carboplatin. Although single agent MK‐2206 inhibited phospho‐AKT signaling, it did not impact in vitro melanoma growth or survival. The combination of MK‐2206 with paclitaxel and carboplatin was cytotoxic in long‐term colony formation and 3D spheroid assays, and induced autophagy. Autophagy was initially protective with autophagy inhibitors and deletion of ATG5 found to enhance cytotoxicity. Although prolonged autophagy induction (>6 days) led to caspase‐dependent apoptosis, drug resistant clones still emerged. Autophagy inhibition enhanced the cell death response through reactive oxygen species and could be reversed by anti‐oxidants. We demonstrate for the first time that AKT inhibition in combination with chemotherapy may have clinical activity in BRAF WT melanoma and show that an autophagy inhibitor may prevent resistance to these drugs. 相似文献
63.
Babasaheb P. Bandgar Shrikant S. Gawande Ragini G. Bodade Jalinder V. Totre Chandrahas N. Khobragade 《Bioorganic & medicinal chemistry》2010,18(3):1364-1370
Chalcones have been identified as interesting compounds with cytotoxicity, anti-inflammatory and antioxidant properties. In the present study, simple methoxychalcones were synthesized by Claisen–Schmidt condensation reaction and evaluated for above biological activities. The structures of the compounds were established by IR, 1H NMR and mass spectral analysis. The data revealed that compound 3s (99–100% at 10 μM concentration) completely inhibit the selected five human cancer cell lines as compared to standard flavopiridol and gemcitabine (70–90% at 700 nM and 500 nM concentrations, respectively), followed by 3a, 3n, 3o, 3p, 3q, 3r. Among the tested compounds 3l, 3m, 3r, and 3s exhibited promising anti-inflammatory activity against TNF-α and IL-6 with 90–100% inhibition at 10 μM concentration. DPPH free radical scavenging activity was given by the compounds 3o, 3n, 3l, 3r, 3m, 3a, 3p, 3c and 3s at 1 mM concentration. Overall, 3s was obtained as lead compound with promising anticancer, anti-inflammatory and antioxidant activities. Bioavailability of compounds were checked by in vitro cytotoxicity study and confirmed to be nontoxic. The structure activity relationship (SAR) and in silico drug relevant properties (HBDs, HBAs, PSA, c Log P, ionization potential, molecular weight, EHOMO and ELUMO) further confirmed that the compounds were potential candidates for future drug discovery study. 相似文献