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""Frontiers in Anti-Cancer Drug Discovery"" is an Ebook series devoted to publishing the latest and the most important advances in Anti-Cancer drug design and discovery. Eminent scientists write contributions on all areas of rational drug design and drug discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, recent important patents, and structure-activity relationships. The Ebook series should prove to be of interest to all pharmaceutical scientists involved in research in Anti-Cancer drug design and discovery. Each vo

Antineoplastic agents. --- Anticancer agents --- Antineoplastic drugs --- Antineoplastics --- Antitumor agents --- Antitumor drugs --- Cytotoxic drugs --- Inhibitors, Neoplasm --- Neoplasm inhibitors --- Drugs --- Cancer --- Chemotherapy

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Diacylglycerol kinases (DGKs) phosphorylate diacylglycerol (DG), catalyzing its conversion into phosphatidic acid (PA). This reaction attenuates membrane DG levels, limiting the localization/activation of signaling proteins that bind this lipid. Initially recognized as modulators of classical and novel PKC family members, the function of the DGK has further expanded with the identification of novel DG effectors including Ras Guanyl nucleotide-releasing proteins (RasGRP) and chimaerin Rac GTPases. The product of the DGK reaction, PA, is also a signaling lipid that mediates activation of multiple proteins including the mammalian target of rapamycin (mTOR). The DGK pathway thus modulates two lipids with important signaling properties that are also key intermediates in lipid metabolism and membrane trafficking. The DGK family in eukaryotes comprises 10 different members grouped into five different subfamilies characterized by the presence of particular regulatory motifs. These regions allow the different DGK isoforms to establish specific complexes and/or to be recruited to specific subcellular compartments. The subtle regulation of DG and PA catalyzed byspecific DGKs is sensed by a restricted set of molecules, providing the means for spatio-temporal regulation of signals in highly specialized cell systems. In the recent years, multiple studies have unveiled the functions of specific isoforms, their mechanisms of regulation and their participation in different pathways leading to and from DG and PA. Animal models have greatly helped to understand the specialized contribution of DGK mediated signals, particularly in the immune and central nervous systems. Mice deficient for individual DGK isoforms show defects in T and B cell functions, dendritic spine maintenance, osteoclast and mechanical-induced skeletal muscle formation. Studies in flies and worms link DGK mediated DAG metabolism with mTOR- mediated regulation of lifespan and stress responses. In plants DGK mediated PA formation contributes to plant responses to environmental signals. Aberrant DGK function has been recently associated with pathological states, an expected consequence of the essential role of these enzymes in the regulation of multiple tissue and systemic functions. DGK mutations/deletions have been related to human diseases including diabetes, atypical hemolytic-uremic syndrome, Parkinson disease and bipolar disorders. On the contrary DGK upregulation emerges as a non-oncogenic addition of certain tumors and represents one of the main mechanism by which cancer evades the immune attack. As a result, the DGK field emerges an exciting new area of research with important therapeutic potential.

T cell receptor --- immunotherapy of cancer --- immune system --- synaptic transmission --- synaptic plasticity (LTP/LTD) --- cytotoxic T cells --- lipid signaling --- tolerance

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The ultimate source of information on the design of new anticancer agents, emphasizing small molecules, this newest work covers recent notable successes resulting from the human genome and cancer genomics projects. These advances have provided information on targets involved in specific cancers that are leading to effective medicines for at least some of the common solid tumors. Unique sections explain the basic underlying principles of cancer drug development and provide a practical introduction to modern methods of drug design.

Antineoplastic agents --- Development. --- Design. --- Anticancer agents --- Antineoplastic drugs --- Antineoplastics --- Antitumor agents --- Antitumor drugs --- Cytotoxic drugs --- Inhibitors, Neoplasm --- Neoplasm inhibitors --- Drugs --- Cancer --- Chemotherapy

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Frontiers in Clinical Drug Research - Anti-Cancer Agents - Volume 1 should prove to be a valuable resource for pharmaceutical scientists and postgraduate students seeking updated and critical information for developing clinical trials and devising research plans in the field. The chapters in this volume have been written by leading experts from the field.The contents of this book include new approaches to cancer therapy, treatment of metastatic non-small cell lung cancer with epidermal growth factor receptor-tyrosine kinase inhibitors, targeting key signaling pathways in pediatric brain tumors

Cancer --- Antineoplastic agent. --- Alternative treatment. --- Alternative therapy --- Treatment --- Antineoplastic agents. --- Anticancer agents --- Antineoplastic drugs --- Antineoplastics --- Antitumor agents --- Antitumor drugs --- Cytotoxic drugs --- Inhibitors, Neoplasm --- Neoplasm inhibitors --- Drugs --- Chemotherapy

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Peritoneal dissemination is a common route of cancer metastasis. The benefit of administering chemotherapy directly into the peritoneal cavity is supported by preclinical and pharmacokinetic data. In comparison to intravenous (IV) treatment, intraperitoneal (IP) administration results in a several-fold increase in drug concentration within the abdominal cavity. There is now growing evidence from clinical studies showing a survival advantage for IP chemotherapy in various tumor typies, including ovarian, gastric and colorectal cancer. However, while the use of IP chemotherapy is slowly gaining acceptance, it is not universal, largely due to the greater toxicity associated with this approach. Moreover, efficacy of IP chemotherapy is limited by poor distribution within the abdominal cavity and by poor tissue penetration. A new way of IP chemotherapy is the application of cytotoxics in form of a pressurized aerosol into the abdominal of thoracic cavity. Pressurized intraperitoneal aerosol chemotherapy (PIPAC) is applied through laparoscopic access using two balloon trocars in an operating room equipped with laminar air-flow. In a first step,a normothermic capnoperitoneum is established with a pressure of 12 mmHg. A cytotoxic solution (about 10% of a normal systemic dose) is nebulized with a micropump into the abdominal cavity, and maintained for 30 min. The aerosol is then removed through a closed suction system. Applying an aerosol in the peritoneal cavity allows a homogeneous distribution of the chemotherapeutic agent within the abdomen. Furthermore, an artificial pressure gradient is generated that overcomes tumoral interstitial fluid pressure, an obstacle in cancer therapy. This results in a higher local drug concentration compared to conventional IP or IV chemotherapy. At the same time the plasma concentration of the chemotherapeutic agent remains low. In first clinical studies with limited number of patients in ovarian, gastric and colorectal cancer, as well as peritoneal mesothelioma, PIPAC has obtained encouraging tumor response rates and survival, with a low-side effects profile. Larger clinical trials are currently ongoing to examine if these data can be reproduced and extrapolated to other situations.

Antineoplastic agents. --- Aerosols. --- Colloids --- Gases --- Anticancer agents --- Antineoplastic drugs --- Antineoplastics --- Antitumor agents --- Antitumor drugs --- Cytotoxic drugs --- Inhibitors, Neoplasm --- Neoplasm inhibitors --- Drugs --- Cancer --- Chemotherapy --- Aerosol.