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- Volume 10, Issue 1, 2010
Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 10, Issue 1, 2010
Volume 10, Issue 1, 2010
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Editorial [Hot topic: Hepatocyte Growth Factor and cMET, New Development in Cancer Therapies (Guest Editors: T.A. Martin and W.G. Jiang)]
Authors: T. A. Martin and W. G. JiangCancer metastasis is the most life threatening event in patients with solid tumours. As a result, understanding the underlying mechanisms and searching for factors that control the metastatic spread of cancer cells are critical in the area of cancer research. Furthermore, agents that interfere with the metastasis of cancer cells are of great value in cancer treatment. Of the complex nature of cancer metastasis, a few Read More
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Hepatocyte Growth Factor and Its Receptor Signalling Complex as Targets in Cancer Therapy
Authors: Tracey A. Martin and Wen G. JiangHepatocyte growth factor (HGF) and it's receptor, cMET, have become the focus on intense scrutiny since its discovery in the late 1980s [1, 2] as regards it role in cancer. HGF is now known to be a potent morphogen that can regulate tissue and organ regeneration and modulate cell morphology, it is a motogen that can stimulate cell motility and migration, and is a mitogen able to regulate cell growth and death and a Read More
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Discovery of Small Molecule c-Met Inhibitors: Evolution and Profiles of Clinical Candidates
Authors: Ted L. Underiner, Torsten Herbertz and Sheila J. MiknyoczkiThe scatter factor/hepatocyte growth factor (HGF)-c-Met axis is involved in the malignant phenotype of various tumor types via activation of a wide range of autocrine and paracrine processes. Autocrine activation of tumor cell c-Met receptors enhances tumor cell proliferation, angiogenesis, invasion/metastasis and resistance to apoptosis and cytotoxic therapies. In addition, tumor and stroma cell-derived HGF functions as a p Read More
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An Orally Bioavailable c-Met Kinase Inhibitor Potently Inhibits Brain Tumor Malignancy and Growth
The receptor tyrosine kinase, c-Met and its ligand hepatocyte growth factor (HGF) are important regulators of malignancy in human cancer including brain tumors. c-Met is frequently activated in brain tumors and has emerged as a promising target for molecular therapies. Recently, an orally bioavailable small molecule kinase inhibitor of c-Met (SGX523) was developed by SGX Pharmaceuticals. We tested the effects of th Read More
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Anti-Cancer Approach with NK4: Bivalent Action and Mechanisms
Authors: Takahiro Nakamura, Katsuya Sakai, Toshikazu Nakamura and Kunio MatsumotoWe identified NK4, the N-terminal and four kringle domains of hepatocyte growth factor (HGF), as a specific inhibitor of HGF. NK4 binds to the Met/HGF receptor, but does not activate the Met receptor, thereby competitively inhibiting the HGF-Met pathway. Independent of its inhibition of HGF-Met, NK4 acts as an angiogenesis inhibitor. The angioinhibitory action of NK4 is mediated by perlecan, a multidomain proteoglycan i Read More
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Hepatocyte Growth Factor Activation Inhibitors – Therapeutic Potential in Cancer
Authors: Christian Parr, Andrew J. Sanders and Wen G. JiangHepatocyte growth factor (HGF) plays a plethora of roles in the progression of many invasive and metastatic cancers. The interaction between tumour cells and their surrounding stromal environment remains a crucial factor governing tumour invasion and metastasis. HGF is primarily synthesised by stromal fibroblasts as an inactive precursor known as pro-HGF. A number of proteases have demonstrated the ability to c Read More
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Application of Biological Study for Met Expression to Cancer Therapy
Authors: Shinji Osada and Kazuhiro YoshidaMetastasization is an undesirable process in cancer development and may represent the most critical factor in deciding patient prognosis. Organ specificity of the metastasis process suggests the importance of the paracrine factors: one of the most potent paracrine regulators of tumor cell migration is hepatocyte growth factor/scatter factor (HGF/SF). Because the liver-specific growth factor is HGF, its receptor c-Met express Read More
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The Type II Transmembrane Serine Protease, Matriptase-2: Possible Links to Cancer?
Authors: Andrew J. Sanders, Siobhan L. Webb, Christian Parr, Malcolm D. Mason and Wen G. JiangMatriptase-2 is a newly identified member of the Type II Transmembrane Serine Protease (TTSP) family. The expression profile of many members of this family of proteases is frequently altered in cancerous cells and tissues and a number of TTSPs have been linked to cancer progression and development. Matriptase-2 is structurally similar to matriptase-1, a TTSP which has gained recent interest due to its potential to enhanc Read More
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Barminomycin, a Model for the Development of New Anthracyclines
Authors: K. Kimura, D. M.S. Spencer, R. Bilardi, L. P. Swift, A. J. Box, R. T.C. Brownlee, S. M. Cutts and D. R. PhillipsBarminomycin is a member of the anthracycline class of anticancer agents and was originally discovered as a pink/red complex with DNA and RNA and named SN-07. The chromophore was subsequently separated from the nucleic acids by nuclease digestion and contained the four-membered anthraquinone ring system characteristic of anthracyclines, but with an unusual eight membered ring that contained a carbinolamine w Read More
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Anticancer Activities and Mechanisms of Bisdioxopiperazine Compounds Probimane and MST-16
Authors: Da-Yong Lu and Ting-Ren LuBisdioxopiperazine compounds, including ICRF-154 and razoxane (ICRF-159, Raz), are anticancer agents developed in the UK specifically targeting tumor metastases. Further two bisdioxopiperazine derivatives, probimane (Pro) and MST-16, have been synthesized at the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, PR China after 1980. Anticancer activities and mechanisms of Pro and MST-16 compared Read More
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Male Fertility-Implications of Anticancer Treatment and Strategies to Mitigate Gonadotoxicity
Authors: Ahmed M. Ragheb and Edmund S. Sabanegh Jr.With the advent of the modern cancer treatment, survival rates have improved substantially raising new concerns towards quality of life issues such as future fertility and offspring welfare. Cancer researchers are expanding their focus beyond survival and recurrence rates to include maximization of fertility potential for young cancer patients. Despite promising cure rates with chemotherapy, studies have shown it to a Read More
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Volumes & issues
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Volume 25 (2025)
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Volume 24 (2024)
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Volume 23 (2023)
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Volume 22 (2022)
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Volume 21 (2021)
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Volume 20 (2020)
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Volume 19 (2019)
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Volume 18 (2018)
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Volume 17 (2017)
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Volume 16 (2016)
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Volume 15 (2015)
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Volume 14 (2014)
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Volume 13 (2013)
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Volume 12 (2012)
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Volume 11 (2011)
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Volume 10 (2010)
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Volume 9 (2009)
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Volume 8 (2008)
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Volume 7 (2007)
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Volume 6 (2006)
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