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Steroid hormones have important roles in human physiology, but they are also implicated in the development of hormone-dependent cancers and various non-maligant diseases. Furthermore, changes in the concentrations of steroid hormones have important effects on the homeostasis of pre- and post-menopausal women, as well as of men in andropause. The associations of steroid hormones with pathophysiological processes and the altered mechanisms of their actions in disease are still not completely understood. It has been known for more than thirty years that in addition to their endocrine activity, steroid hormones act in an intracrine manner. In target organs, active androgens and estrogens can be ...
More than 40 years ago, the observation that doxorubicin-resistant tumor cells were cross-resistant to several structurally different anticancer agents was the first step in the discovery of P-glycoprotein (P-gp). P-gp belongs to the superfamily of ATP-binding cassette (ABC) transporters;its overexpression has become a therapeutic target for overcoming multidrug resistance in tumors. However, P-gp is also expressed in cells of normal tissues where it plays a physiological role, by protecting them from the toxic effects of xenobiotics. Also, ABCB1 gene polymorphisms may influence the response to anticancer drugs substrate of P-gp. Several strategies to overcome P-gp tumor drug resistance have...
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ABC Transporters and Cancer provides invaluable information on the exciting and fast-moving field of cancer research. Here, outstanding and original reviews are presented on a variety of topics. This volume covers ABC transporters and cancer, and is suitable for researchers and students alike. - Provides information on cancer research - Outstanding and original reviews - Suitable for researchers and students
Knowledge of the basic mechanisms of human disease is essential for any student or professional engaged in drug research and development. Functional gene analysis (genomics), protein analysis (proteomics), and other molecular biological techniques have made it possible to understand these cellular processes, opening up exciting opportunities for no
Transport of pharmaceutical agents in the body is paramount to therapeutic efficacy. Advances in the past decades have rendered a remarkable improvement of drug delivery strategies, which has helped to increase the bioavailability of therapeutic agents by protecting them from degradation, targeting them to diseased sites, and controlling their circ
It is increasingly recognized that various transporter proteins are expressed throughout the body and determine absorption, tissue distribution, biliary and renal elimination of endogenous compounds and drugs and drug effects. This book will give an overview on the transporter families which are most important for drug therapy. Most chapters will focus on one transporter family highlighting tissue expression, substrates, inhibitors, knock-out mouse models and clinical studies.
Transporters in Drug Development examines how membrane transporters can be dealt with in academic–industrial drug discovery and pharmaceutical development as well as from a regulatory perspective. The book describes methods and examples of in vitro characterization of single transporters in the intestines, liver and kidneys as well as characterization of substrate overlap between various transporters. Furthermore, probes and biomarkers are suggested for studies of the transporters’ impact on the pharmacokinetics of drug substrates/candidates interacting on transporters. The challenges of translating in vitro observed interaction of transporters into in vivo relevance are explored, and the book highlights perspectives of applying targeted proteomics and mechanistic modeling in this process.