Hypermonones A-I, New Polyprenylated Acylphloroglucinols from
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Structural feature-driven pattern analysis for multitarget modulator landscapes. Vigneshwaran Namasivayam, Katja Stefan, Katja Silbermann, Jens Pahnke, Michael Wiese, Sven Marcel Stefan.Zinc oxide/graphene oxide nanocomposites efficiently inhibited cadmium-induced hepatotoxicity via releasing Zn ions and up-regulating MRP1 expression. Yun Liu, Xue Wang, Bo Si, Tong Wang, Yun Wu, Ying Liu, Yemian Zhou, Haiyang Tong, Xinwei Zheng, An Xu.International Journal of Biological Macromolecules 2022, 217, 775-791. Physicochemistry shapes bioactivity landscape of pan-ABC transporter modulators: Anchor point for innovative Alzheimer's disease therapeutics. Vigneshwaran Namasivayam, Katja Stefan, Lukas Gorecki, Jan Korabecny, Ondrej Soukup, Patric Jan Jansson, Jens Pahnke, Sven Marcel Stefan.Design and evaluation of pyrimidine derivatives as potent inhibitors of ABCG2, a breast cancer resistance protein. Imtaiyaz Hassan, Dinesh Gupta, Neeraj Dwivedi, Asimul Islam. A curated binary pattern multitarget dataset of focused ATP-binding cassette transporter inhibitors. Sven Marcel Stefan, Patric Jan Jansson, Jens Pahnke, Vigneshwaran Namasivayam.Astroblastomas exhibit radial glia stem cell lineages and differential expression of imprinted and X-inactivation escape genes. Lehman, Stefan Costinean, Anil Parwani, Brian J. Maclean, Paolo Fadda, Tom Liu, Vineela Gangalapudi, Jamie Carver, Zied Abdullaev, Cynthia Timmers, John R. Lehman, Nathalie Spassky, Müge Sak, Amy Webb, Cory T. Superior Pyrimidine Derivatives as Selective ABCG2 Inhibitors and Broad-Spectrum ABCB1, ABCC1, and ABCG2 Antagonists. Katja Silbermann, Jiyang Li, Vigneshwaran Namasivayam, Fabian Baltes, Gerd Bendas, Sven Marcel Stefan, Michael Wiese.: Computer-Aided Pattern Analysis to Predict Multitarget ABC Transporter Inhibitors.
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Vigneshwaran Namasivayam, Katja Silbermann, Michael Wiese, Jens Pahnke, Sven Marcel Stefan.Discovery of the TriazoloPyrimidine-Based Derivative WS-898 as a Highly Efficacious and Orally Bioavailable ABCB1 Inhibitor Capable of Overcoming Multidrug Resistance. Shuai Wang, Sai-Qi Wang, Qiu-Xu Teng, Zi-Ning Lei, Zhe-Sheng Chen, Xiao-Bing Chen, Hong-Min Liu, Bin Yu.This article is cited by 17 publications. Besides, three more new multitarget inhibitors were identified by this virtual screening approach. In addition, the thienopyrimidine could also sensitize ABCB1- as well as ABCG2-overexpressing cells toward daunorubicin and SN-38, respectively, in concentration ranges that qualified it as one of the ten best triple ABCC1/ABCB1/ABCG2 inhibitors in the literature. Further evaluation showed that it was a moderately potent, competitive inhibitor of the ABCB1-mediated transport of calcein AM, and noncompetitive inhibitor of the ABCG2-mediated pheophorbide A transport. The best hit molecule-a thienopyrimidine-was a moderately potent, competitive inhibitor of the ABCC1-mediated transport of calcein AM which also sensitized ABCC1-overexpressing cells toward daunorubicin. Biological investigation of promising candidates revealed four compounds as ABCC1 inhibitors, three of them with scaffolds not associated with ABCC1 inhibition until now. A virtual screening protocol with combination of similarity search and pharmacophore modeling was applied to virtually screen a large compound library to gain new scaffolds regarding ABCC1 inhibition.