Kumar et al., Med chem 2015, 5:3
DOI: 10.4172/2161-0444.1000252
Review Article Open Access
Med chem
ISSN: 2161-0444 Med chem, an open access journal
Volume 5(3): 115-123 (2015) - 115
Drug Targets for Cancer Treatment: An Overview
Shashank Kumar
1
, Mohammad Kaleem Ahmad
1
, Mohammad Waseem
1
and Abhay K Pandey
2
*
1
Molecular and Cell Biology Laboratory, Department of Biochemistry, King Georges Medical university, Lucknow-226003, India
2
Department of Biochemistry, University of Allahabad, Allahabad-211002, India
*Corresponding author: Abhay K. Pandey, Department of Biochemistry, University
of Allahabad, Allahabad-211002, India, E-mail: akpandey23@rediffmail.com
Received February 24, 2015; Accepted March 17, 2015; Published March 19
2015
Citation: Kumar S, Ahmad MK, Waseem M, Pandey AK (2015) Drug Targets
for Cancer Treatment: An Overview. Med chem 5: 115-123. doi:10.4172/2161-
0444.1000252
Copyright: © 2015 Kumar S, et al. This is an open-access article distributed under
the terms of the Creative Commons Attribution License, which permits unrestricted
use, distribution, and reproduction in any medium, provided the original author and
source are credited.
Abstract
Cancer is one of the major cause of death worldwide. Malignant cells display metabolic changes, when compared
to normal cells, because of both genetic and epigenetic alterations. Number of drugs being used for the cancer
treatment follows different mechanisms of action. Therapeutic strategies include targeting of drugs at specifc genes
or proteins/enzymes found in cancer cells or the internal tissue environment which contributes to growth and survival
of these cells. Targeted therapy is often used along with chemotherapy and other treatments to restrict the growth
and spread of cancer cells. During the past few decades, targeted therapy has emerged as a promising approach
for the development of selective anticancer agents. There is a class of targeted therapy drugs called angiogenesis
inhibitors which focus on blocking the development of new blood vessels in tumor tissues. In addition, anticancer drugs
also include DNA intercalators, DNA synthesis inhibitors, transcription regulators, enzyme inhibitors etc. This review
focuses on major classes of anticancer drug targets and their therapeutic importance.
Keywords: Anticancer drug targets; Angiogenesis; Gene regulation;
Enzyme; Microtubules
Introduction
Cancer is the second leading cause of death in Europe and
America. Tremendous resources are being invested all around the
world for developing preventive, diagnostic, and therapeutic strategies
for cancer [1]. Several pharmaceutical companies and government/
non-government organizations are involved in the discovery and
development of anticancer agents [2]. Identifcation of novel cytotoxic
compounds has led to the development of anticancer therapeutics for
several decades. Boom of knowledge in molecular sciences, genomics
and proteomics has also helped in creating new potential drug targets.
Tis has changed the paradigms of anticancer drug discovery toward
molecularly targeted therapeutics. Tere are unique challenges and
opportunities in discovery of anticancer drug delivery which might
refect at each stage of the drug development process [3]. Cancer is
primarily a disease of uncontrolled cell division, thus identifcation
of anti-proliferative compounds and their efects on regression of
tumor size are the main aims for therapeutic discovery. For this
purpose murine models of cancer were developed and several clinically
important anticancer compounds were identifed [1]. Diferentiated
result outputs among fast growing and slow growing tumors led
investigators to modify the screening protocols to include a variety
of cell lines and tumor types. Te rationale that cancer cells are more
likely to be replicating than normal cells makes the basis for targeting
cell division process by most of the chemotherapeutics. Unfortunately
signifcant toxicity is associated with chemotherapeutics as they lack
specifc action [1-3].
Double-helical DNA consists of two complementary
strands running anti-parallel having sugar-phosphate poly-
deoxyribonucleotide backbone associated with specifc hydrogen
bonding between nucleotide bases [4]. In a given DNA sequence
diference in chemical feature of the molecular surfaces in either groove
forms the basis for molecular recognition by small molecules and
proteins. B-form of the DNA i.e. biologically relevant double helix is
characterized by a shallow wide major groove and a deep narrow minor
groove [5]. DNA replication, transcription and protein synthesis are
the major steps in cell growth and division. Being carrier of genetic
information as well as central to tumorigenesis and pathogenesis, DNA
is a major target for drug development. Tere is always a challenge for
drug to achieve maximum specifc DNA binding afnity. Te other
thing that needs consideration is that drug should not afect cellular
and nuclear transport activity of the normal cells. Some of the most
efective anticancer agents that target DNA are known to produce
signifcant survival rate in cancer patients when used in combination
with drugs having diferent mechanisms of action [6]. Besides DNA,
RNA, enzymes and other proteins also contributes as major targets for
anticancer drug development [7]. Structures of some anticancer drugs
are depicted in Figure 1. In this review we have tried to discuss some
molecular aspects of anticancer drug mechanisms.
Angiogenesis Inhibitors
Angiogenesis (AG) is the process by which tumour develops new
blood supply (neovascularisation) for the growth and metastasis.
Small tumours can obtain oxygen and nutrients by difusion but
as they become enlarged they need to develop new blood vessels
for the fulfllment of required nutrients for growth, invasion and
metastasis. Diferent anti- and pro-angiogenic factors are involved
in the development of blood vessels in a complex equilibrium [8]. In
physiological processes such as wound healing this equilibrium may
go in favor of angiogenesis by infammation or hypoxia. But on the
other hand it may be the part of the pathological process in cancer
or other chronic infammatory diseases. Vascular endothelial growth
factor (VEGF), angiogenin, transforming growth factor-β (TGF-β) and
fbroblast growth factor (FGF) are some pro-angiogenic factors that
are released in tumor associated angiogenesis which in turn induces
the proliferation, migration and invasion of endothelial cells in new
vascular structures [8]. Platelet derived growth factor receptor and cell
adhesion molecules (e.g., integrins) play important role in the process of
angiogenesis. Oxygen deprivation, oncogenic mutations, infammation
and mechanical stress are the stimulus that initiates growth of new
vessels in tumor (angiogenic switch). Tis leads to vascularisation
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ISSN: 2161-0444
Medicinal chemistry