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Third Generation EGFR Inhibitors: Overcoming EGFR Resistance and Toxicity Problems reviews current issues relating to the design of reversible and irreversible third generation EGFR inhibitors, highlighting the types of mutation responsible for resistance, and providing different chemical starting points for researchers to optimize and develop in designing the next generation of drugs. Beginning with an introduction to EGFR inhibitors and a review of inhibitors currently approved or in clinical trials, the book goes on to discuss current approaches in the development of both covalent irreversible and covalent reversible EGFR Inhibitors. In addition, mechanisms of resistance to third generation inhibitors, and discovery of fourth generation allosteric C797S inhibitors are explored before a discussion of potential future trends. This comprehensive coverage of the design and development of improved analogues to overcome the problems of resistance and toxicity associated with third generation EGFR inhibitors makes Third Generation EGFR Inhibitors a crucial resource for medicinal chemists, drug developers, and researchers investigating cancer therapeutics.

Epidermal growth factor --- Receptors --- Testing. --- Inhibitors.

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In this study, we have investigated the effects of v-Src on receptor –mediated endocytosis of transferring and EGF, using two different cell lines bearing two different v-Src mutants with thermosensive kinase activity.
Thermo-activation of v-Src had no detectable effect on receptor-mediated endocytosis of transferring in Rat-1/tsLA29 cells, but quickly stimulated this endocytosis in MDCK/tsLA31 cells.
In this cell line, the effects of v-Src on receptor-mediated endocytosis of EGF are more complex. Indeed, v-Src thermo-activation (i) first decreased the efficacy of endocytosis of occupied receptor; (ii) induced after ~30 min a desensitization attributed to triggered endocytosis or reduced recycling of an occupied receptor; and (iii) led after 12-24h to a compensation that restored the efficacy of EGF-receptor complex internalization Les effets de v-Src sur l’endocytose médiée par les récepteurs de la transferrine et de l’EGF ont été étudiés sur deux lignées cellulaires, portent chacune un mutant v-Src thermosensible.
La réactivation thermique de v-Src n’a pas d’effet décelable sur l’endocytose médiée par le récepteur de la transferrine dans les cellules fibroblastiques Rat-1/tsLA29, mais l’accélère d’environ 3 fois dans la lignée épithéliale MDCK/tsLA31.
Dans cette lignée épithéliale, les effets de v-Src sur l’endocytose du récepteur de l’EGF sont plus complexes. En effet, la réactivation thermique de v-Src (i) ralentit tout d’abord l’efficacité de l’endocytose du récepteur EGF occupé par son ligand ; (ii) provoque après ~30 min une désensibilisation en induisant l’endocytose ou en ralentissant le recyclage du récepteur inoccupé ; et (iii) conduit après 12-24h enfin à une compensation restaurant l’efficacité de l’endocytose ligand-récepteur

Avian Sarcoma Viruses --- Endocytosis --- Receptor, Epidermal Growth Factor --- Epidermal Growth Factor --- Receptors, Transferrin --- Transferrin

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Cancer invasiveness --- Cancer --- Epidermal growth factor --- Epidermal growth factor --- Tumors --- Disease Progression --- Neoplasms --- Receptor, Epidermal Growth Factor --- Receptor Protein-Tyrosine Kinases --- Signal Transduction --- Immunotherapy --- Receptors --- Growth --- drug therapy

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Cancer --- Immunotherapy. --- Immunological aspects --- Treatment --- Drug resistance in cancer cells. --- Epidermal growth factor. --- Drug Resistance, Neoplasm --- Epidermal Growth Factor

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Epidermis --- Epidermal growth factor --- Growth factors --- Epidermal Growth Factor --- Cytokines --- Molecular aspects --- physiology --- Cytokines. --- Epidermal growth factor. --- Growth factors. --- Epidermal Growth Factor-Urogastrone --- Molecular aspects. --- physiology. --- Human Urinary Gastric Inhibitor --- beta-Urogastrone --- EGF --- Urogastrone --- Growth Factor, Epidermal --- Growth Factor-Urogastrone, Epidermal --- beta Urogastrone --- Epidermis - Molecular aspects --- Epidermal Growth Factor - physiology --- Cytokines - physiology