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Titlebook: Rational Drug Design; Methods and Protocol Yi Zheng Book 2012 Springer Science+Business Media New York 2012 ATP binding.GTPases.Structure b

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Affinity Purification of Protein Kinases that Adopt a Specific Inactive Conformation,onserved in all kinases, the inactive DFG-out conformation appears to be accessible to only certain kinases. This inactive conformation has been successfully targeted with highly selective kinase inhibitors, including the cancer drugs imatinib and sorafenib. However, the structural and sequence requ
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Mouse Models for Tumor Metastasis,ntaneous metastasis mouse model, 4T1 mouse breast tumor cells are injected into the mammary gland of host mice and the metastasis of 4T1 tumor cells into the lung are examined with a colonogenic assay. In the second experimental metastasis mouse model, luciferase-labeled MDA-MB-231 human breast tumo
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Purification and Specific Assays for Measuring APE-1 Endonuclease Activity,celerated by the use of high-throughput screening. Nevertheless, potential inhibitors must be tested in other counterscreens to validate their selectivity for APE-1. Here, we describe in-depth protocols for APE-1 purification and development of assays specific for APE-1 endonuclease activity.
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An In Vitro Screening to Identify Drug-Resistant Mutations for Target-Directed Chemotherapeutic Ageening strategy to identify the spectrum of resistance-conferring mutations, which has helped in designing the next-generation BCR/ABL inhibitors such as Nilotinib, Dasatinib, and Ponatinib. Here we provide a detailed methodology for the screen, which can be generally applied to any drug–target pair.
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