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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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Epidermal growth factor --- Receptors --- Testing. --- Inhibitors. --- Anthelone --- EGF (Growth factor) --- EGF-URO (Growth factor) --- EGF-Urogastrone --- Epidermal growth factor-Urogastrone --- Uroanthelone --- Uroenterone --- Growth factors
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Sex steroids, including androgens, estrogens, and progestogens, are knownto have widespread physiological actions beyond the reproductive systemvia binding to the sex hormone receptors. Meanwhile, emerging evidence hasindicated that sex hormone receptor signals are involved in the outgrowth ofsome malignancies, such as prostate and breast carcinomas, as well as othersthat have not traditionally been considered as endocrine-related neoplasms. ThisSpecial Issue “Sex Hormone Receptor Signals in Human Malignancies” coversvarious aspects of the potential role of sex hormone receptors and related signalsin prostate cancer, breast cancer, and other neoplastic conditions by depictingpromising findings derived from in vitro and in vivo experiments as well as theanalyses of surgical specimens. The current observations described may thusprovide a unique insight into novel or known functions of sex hormone receptorsand related molecules.
FOXA1 --- COBRA1 --- n/a --- estrogen --- progesterone receptor negative --- mutational profiling --- heterogeneous nuclear ribonucleoprotein K --- estrogen receptor alpha --- salivary gland tumors --- castration-resistant prostate cancer --- ELK1 --- fibroblasts --- androgen receptor --- melanocytes --- drug screening and proteomics --- PI3K pathway --- NELFB --- therapeutic targets --- immunohistochemistry --- androgen deprivation therapy --- ovarian cancer --- estrogen receptor --- epidermal growth factor receptor --- ethinylestradiol --- melanoma --- breast cancer --- keratinocytes --- G-protein coupled estrogen receptor --- prognosis --- levonorgestrel --- ultraviolet radiation --- sex hormone receptors --- upper urinary tract urothelial carcinoma --- CRPC --- nuclear factor erythroid 2-related factor 2 --- TP53
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Antioxidative polyphenols represented by tannins and flavonoids are rich in numerous food sources and traditional natural medicines and currently attracting increased attention in health care and food industries because of their multiple biological activities that are favorable to human health. Commemorating the outstanding achievements on tannins by Dr. Takuo Okuda on the occasion of his passing away in December 2016, his colleagues, friends, and worldwide experts of polyphenol research have contributed 18 papers on their recent study to the Special Issue of Molecules. This book is its reprinted form. This covers reviews of structural features, historical usages, and biological activities of unique class of ellagitannins and condensed tannins, and original articles on the most up-to-date findings on the anticancer effect of green tea catechins, the antivirus effect of tannins comparing with the clinically used drugs, the analytical method of ellagitannins using quantitative NMR, the chemical structures of Hydrangea-blue complex (pigment) and condensed tannins in Ephedra sinica and purple prairie clover, and the relationship of condensed tannins in legumes and grape-marc with methane production in the in vitro ruminant system, and others. This book will be useful to natural product chemists and also to researchers in pharmaceutical and/or food industry.
Coreopsis lanceolata L. --- UV-Vis --- methanogenesis --- Lythraceae --- flavanone --- grape marc --- TDDFT --- Ephedra sinica --- macrocyclic oligomer --- triple-negative breast cancer --- antioxidant --- purple prairie clover --- chalcone --- neuraminidase --- fatty acid synthase --- (?)-epigallocatechin gallate --- epidermal growth factor --- NMR spectroscopy --- Aluminum ion --- Onagraceae --- Hydrangea macrophylla --- synthetic analogues --- blue color development --- amyloid-? peptide --- FTIR --- oseltamivir carboxylate --- quantitative NMR --- phloroglucinolysis --- thin layer chromatography --- European historic leathers --- FASN inhibition --- ECD --- colorimetric tests --- taxanes --- cynandione A --- conservation method --- 5-O-caffeoylquinic acid --- ellagitannin --- PC12 --- condensed tannin --- Trapa taiwanensis Nakai --- 1H-NMR --- Acacia --- (?)-epigallocatechin 3-gallate --- Geranium thunbergii --- condensed tannins --- immunomodulatory effect --- Acacia mearnsii bark --- Escherichia coli --- oligomer --- Horner–Wadsworth–Emmons reaction --- lung tumor --- Aspergillus fumigates --- in vitro batch fermentation --- metal complex --- Myrtaceae --- Cynanchum auriculatum --- molecular interactions --- phenolic glycoside --- bamboo leaf extract --- stability --- Microsporum canis --- Cynanchum wilfordii --- thiolysis --- anti-inflammation --- hydrolysable tannin --- geraniin --- NGF --- polyphenol --- revision --- ESI-mass --- bioactivity --- antifungal activities --- interferon-? --- antitumor effect --- tannin composition --- oenothein B --- zanamivir --- 2-O-?-laminaribiosyl-4-hydroxyacetophenone --- anticancer activity --- proanthocyanidin --- vegetable tanning --- Dittrichia viscosa --- differentiation --- aurone --- antioxidants --- protein precipitation --- apoptosis --- polyphenolic FASN inhibitors --- forage legume --- biological activities --- ultrahigh-resolution negative mode MALDI-TOF mass spectrometry --- overlay method --- spectroscopy --- wattle tannin --- immune checkpoint --- hormesis --- 3-O-glucosyldelphinidin --- gallotannin --- proanthocyanidins --- fatty acids --- flavonol --- inhibition --- structure --- Candida spp. --- Malassezia spp. --- ORAC assay --- neuroprotection --- crystal structure --- tannins
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