Topics in Anti-Cancer Research

Volume 2


Atta-ur-Rahman / Khurshid Zaman

DOI: 10.2174/97816080513661130201
eISBN: 978-1-60805-136-6, 2013
ISBN: 978-1-60805-139-7
ISSN: 2468-5860 (Print)
ISSN: 2213-3585 (Online)

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Indexed in: Book Citation Index, Science (BKCI-S), Chemical Abstracts, BIOSIS Previews, EBSCO, Ulrich's Periodicals Directory.

This is the second volume of the Patent eBook Series titled Topics in Anti-Cancer Research. The eBook includes updated chapters on top...[view complete introduction]
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Table of Contents


- Pp. i-iii (3)
Atta-ur-Rahman and Khurshid Zaman
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List of Contributors

- Pp. iv-v (2)
Atta-ur-Rahman and Khurshid Zaman
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- Pp. vi
Atta-ur-Rahman and Khurshid Zaman
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Emerging Research and Therapeutic Strategies for Castration-Resistant Prostate Cancer

- Pp. 3-34 (32)
Tomoaki Tanaka and Tatsuya Nakatani
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Sphingomyelin Biosynthesis Modulates Cancer Cell Death and Growth

- Pp. 35-62 (28)
Elodie Lafont, Kazuyuki Kitatani, Toshiro Okazaki and Bruno Ségui
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The Therapeutic Promise of Anti-Cancer Drugs Against the Ras/Raf/MEK/ERK Pathway

- Pp. 63-94 (32)
Erin K. Crane and Kwong-Kwok Wong
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Recent Developments in Anticancer Agents Targeting PI3K, AKT and mTORC1/2

- Pp. 95-196 (102)
Irene Brana, Sara De Dosso, Rodrigo Dienstmann, Jordi Rodon, Josep Tabernero and Ben Markman
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Cell Cycle and Energy Metabolism in Tumor Cells: Strategies for Drug Therapy

- Pp. 197-230 (34)
Nivea D. Amoêdo, Tatiana El-Bacha Porto, Mariana F. Rodrigues and Franklin D. Rumjanek
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V-ATPase Inhibitors in Cancer Therapy: Targeting Intraorganellar Acidification

- Pp. 231-256 (26)
Agustín Hernández, Gloria Serrano-Bueno, Rosana Herrera-Palau, José R. Pérez-Castiñeira and Aurelio Serrano
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Insights into the Role of Fc Gamma Receptors (FcγRs) Genetic Variations in Monoclonal Antibody-Based Anti-cancer Therapy

- Pp. 257-278 (22)
Fabio Concetti and Valerio Napolioni
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Angiogenesis: Therapeutic Target in Renal Cell Carcinoma

- Pp. 279-298 (20)
Manisha Singh, Sudip Nanda, Santo Longo and Shree G. Sharma
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Anti-Angiogenic Therapy for Cancer: Past, Present and Future

- Pp. 299-319 (21)
Boel De Paepe
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Paradigm Shift in the Therapeutic Potential of Endogenous Angiogenesis Inhibitors for Cancer Therapy: Historical Perspective and Future Direction

- Pp. 320-362 (43)
Mohanraj Dhanabal and Natarajan Sethuraman
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Ribonucleotide Reductase as a Target to Control Cancer Proliferation

- Pp. 363-406 (44)
Nuno M.F.S.A. Cerqueira, Narayana S.H.N. Moorthy, Pedro A. Fernandes and Maria J. Ramos
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Enhancing the Anticancer Activity of Erlotinib in Glioblastoma

- Pp. 407-436 (30)
Georg Karpel-Massler, Christian R. Wirtz and Marc-Eric Halatsch
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Nanodrugs: Magic Bullets in Cancer Chemotherapy

- Pp. 437-494 (58)
Kishwar Saleem, Waseem A. Wani, Ashanul Haque, Archana Milhotra and Imran Ali
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Chemotherapy of Nano-Sized Camptothecin-Derived Drugs

- Pp. 495-521 (27)
Nguyen-Van Cuong, Chi-Hui Guo and Ming-Fa Hsieh
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Onconutrition: Redox Chemoprevention by Functional Biomolecules and Biomarker Assessment

- Pp. 522-552 (31)
María D. Defagó and Elio A. Soria
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Author Index

- Pp. 553
Atta-ur Rahman and Khurshid Zaman
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- Pp. 554-576 (23)
Atta-ur Rahman and Khurshid Zaman
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This is the second volume of our Patent eBook Series entitled "Topics in Anti-Cancer Research". The eBook includes updated chapters on important topics of cancer published in the Recent Patents on Anti-Cancer Drug Discovery.

The volume covers scientific and patented novel chemotherapeutic agents and drugs for metastatic castration-resistant prostate cancer and Ras/ Raf /MEK/ERK pathway, P1K, AKT and mTORC1/2 inhibitors, ATPase inhibitors for cancer therapy, and sphingomyelin biosynthesis which regulates cancer cell death and growth.

Tanaka et al., present the latest literature research and strategies on therapeutic agents and patented compounds and improvement of survival for metastatic castration - resistant prostate cancer (CRPC). The role of novel patented compounds e.g. N-cadherin, AR splicing variants, PCGEM-1, ELR-CXC chemokine antagonist, dual inhibitor of MET and VEGF as an alternative options for prostate cancer has been discussed in Chapter 1.

Chapter 2 by Ségui et al., focuses on the regulation of cancer cell death, sensitivity and growth by sphingomyelin biosynthesis through a series of metabolic pathways and sphingolipid signaling. Hematological malignancies are also discussed in this chapter.

Chapter 3 provides a complete overview of novel patented compounds and patent applications inhibiting the activities of B-Raf/Ras/ERK and MEK signaling pathways. Wong et al. present the results of current clinical trials of these inhibitors.

Tabernero et al., in Chapter 4 review new emerging preclinical researches, clinical trials for targeting of P13K, AKT, dual P13K and mTOR inhibitors for treating different types of cancers.

Approaches for studying main stages of cell cycle via biochemical regulatory processes and energy metabolism in cancer cells are presented by Rumjanek et al., in Chapter 5. These pathways are inhibited by synthetic and natural compounds and the involvement of cyclin dependent kinases and phosphatases, oncogenes, mitochondria and histone deacetylases is also discussed.

Hernández et al., in Chapter 6 have given an overview of the origin, structure, function and mechanism of action of patented V-ATPase inhibitors by intraorganellar acidification of membranes for the treatment of cancer.

Chapter 7 describes the use of monoclonal antibodies (MoAbs) used in cancer therapy. Napolioni et al. discuss the mechanisms, genetic profiles and interaction of the Fc gamma receptors (FcγRs) with immunotherapeutic drugs.

Sharma et al., present the key role of molecular vascular endothelial growth factor (VEGF) in the treatment of metastatic renal cell carcinoma (RCC) with reference to patents for anti-VEGF drugs for RCC and molecular pathways involved in the development of angiogenesis drugs for renal cancer in Chapter 8.

In the next chapter, Boel De Paepe covers different approaches on tumor neovascularization as a target for cancer therapy. Novel anti-angiogenic agents are also discussed along with relevant biological pathways of neo angiogenesis and its inhibition by natural metabolites, pharmaceutical compounds, and combination therapy.

Cerqueira et al. in Chapter 11 review the papers and patents on RNA inhibition, ribonucleotidase reductase inhibitors structure, action mechanism and biochemistry. Rribonucleotidase reductase is clinically used for the control of different specific types of cancers.

Karpel-Massler et al. focus on relevant patents for enhancing the anti-cancer activity of erlotinib by combining HER/EGFR- targeted TK inhibitors for the cure of malignant glioblastoma in Chapter 12.

Imran et al. present the role of nanodrugs in cancer chemotherapy. Nanodrugs act specifically on cancer cells. Nanodrugs diversity and mechanism, future perspectives, and conventional chemotherapeutic drugs are discussed in Chapter 13.

Chapter 14 by Hsieh et al. describe the present status including the literature and patents on nano-sized camptothecin and its analogs for cancer chemotherapy.

In the subsequent chapter, Soria et al. discuss the patents on recent developments of redox - chemoprevention by dietary onconutrition and the role and assessment of anticancer functional biomarkers and biomolecules.

Topics in Anti-Cancer Research, is an essential e-book series for oncologists, pharmaceutical scientists, clinicians, scientists, R&D experts and researchers in other cancer related disciplines.

It is hoped that the second volume will be of immense interest to a large number of medicinal chemists, pharmacologists, researchers, clinicians, scientists, R&D experts and medical doctors seeking new targets for the prevention of cancer and new developments for cancer chemotherapy. The editors wish to express their sincere gratitude to Mr. Mahmood Alam, Ms. Raheela Anjum, Ms. Iffat Shaheen and Mrs. Rafia Rehan, the reviewers, the authors, friends and all colleagues for their assistance in the finalization of eBook.

Atta-ur-Rahman, FRS
Kings College
University of Cambridge

Dr. Khurshid Zaman
Bentham Science Publishers

List of Contributors

Atta-ur-Rahman / Khurshid Zaman
University of Cambridge

Imran Ali
Department of Chemistry
Jamia Millia Islamia (Central University)
New Delhi, 110025

Nuno M.F.S.A. Cerqueira
REQUIMTE / Faculdade de Ciências do Porto
Rua Campo Alegre, 687
Porto, 4169-007

Boel De Paepe
Neurology and Pathology
Ghent University Hospital
UZ 1K12A, De Pintelaan 185
Ghent, 9000

Mohanraj Dhanabal
EMD Serono Research Institute Inc
45A Middlesex Turnpike
MA , 01821

Agustín Hernández
Instituto de Bioquímica Vegetal y Fotosíntesis
CSIC-Universidad de Sevilla
Avda. Américo Vespucio 49
Seville, 41092

Ming-Fa Hsieh
Department of Biomedical Engineering
Chung Yuan Christian University
200, Chung Pei Rd Chung Li
Taiwan, 32023

Georg Karpel-Massler
Department of Neurosurgery
University of Ulm School of Medicine
Albert-Einstein-Allee 23
Ulm , D-89081

Valerio Napolioni
School of Biosciences and Biotechnologies
University of Camerino
Via Gentile III da Varano
Camerino, 62032

Franklin D. Rumjanek
Instituto de Bioquímica Médica CCS-Universidade Federal do Rio de Janeiro
Ilha do Fundão
Rio de Janeiro, CEP 21941-590

Bruno Ségui
INSERM UMR1037-Cancer Research Center of Toulouse
Toulouse Cedex 4, 31432

Shree G. Sharma,
Department of Pathology
University of Arkansas for Medical Sciences
Little Rock

Elio A. Soria
Instituto de Biología Celular
Enrique Barros S/N
Ciudad Universitaria Córdoba
Córdoba, 5014

Josep Tabernero
Medical Oncology Service
Vall d'Hebron University Hospital and Vall d'Hebron Institute of Oncology, Universitat Autonoma de Barcelona

Tomoaki Tanaka
Department of Urology
Osaka City University Graduate School of Medicine

Kwong-Kwok Wong
Department of Gynecologic Oncology and Reproductive Medicine
The University of Texas M.D. Anderson Cancer Center
1515 Holcombe Blvd
TX, 77030


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