Molecular Delivery of Cytotoxic Agents via Integrin Activation

Integrins are cell adhesion receptors overexpressed in tumor cells. A direct inhibition of integrins was investigated, but the best inhibitors performed poorly in clinical trials. A gained attention towards these receptors arouse because they could be target for a selective transport of cytotoxic agents. Several active-targeting systems have been developed to use integrins as a selective cell entrance for some antitumor agents. The aim of this review paper is to report on the most recent results on covalent conjugates between integrin ligands and antitumor drugs. Cytotoxic drugs thus conjugated through specific linker to integrin ligands, mainly RGD peptides, demonstrated that the covalent conjugates were more selective against tumor cells and hopefully with fewer side effects than the free drugs.

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Nano Technological Approach for Anti-Tumor Therapy: Opportunities and Challenges

Nanoscience &Nanotechnology-Asia ◽

10.2174/2210681210666200213121156 ◽

2020 ◽

Vol 10 ◽

Author(s):

Krishna Champaneria ◽

Prajesh Prajapati

Keyword(s):

Adverse Effects ◽

Tumor Cells ◽

Targeted Delivery ◽

Blood Circulation ◽

Review Paper ◽

Tumor Therapy ◽

Conventional Chemotherapy ◽

Targeting Delivery ◽

Tumor Accumulation ◽

Work Done

Cancer is one of the reason for mortality and its individual and collective impact is substantial. Conventional chemotherapy utilizes drugs that can destroy Tumor cells effectively. But these agents destroy healthy cells along with the tumor cells, leading to many adverse effects which include hypersensitivity reactions, nephrotoxicity, and neurotoxicity. To minimize the adverse effects, various drug delivery systems (DDSs) has been developed. Among them, nanoparticles are attractive platforms for it. So this review paper explores the recent work done on targeted delivery, enhancing tumor accumulation and longer blood circulation using more effective biomaterial that will enhance the properties of nanoparticles. Moreover, various target-specific delivery of drugs like antibody-targeted, targeting delivery through angiogenesis, mitochondria, CD44 receptor are also explained.

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Induction of Apoptosis by Hybrid Liposomes without Antitumor Drugs toward Human Breast Tumor Cells

JOURNAL OF CHEMICAL ENGINEERING OF JAPAN ◽

10.1252/jcej.36.1127 ◽

2003 ◽

Vol 36 (9) ◽

pp. 1127-1129 ◽

Cited By ~ 3

Author(s):

Hideaki Nagami ◽

Keiichi Yamamoto ◽

Hideaki Ichihara ◽

Yoko Matsumoto ◽

Ryuichi Ueoka

Keyword(s):

Tumor Cells ◽

Breast Tumor ◽

Antitumor Drugs ◽

Human Breast ◽

Human Breast Tumor ◽

Breast Tumor Cells ◽

Induction Of Apoptosis

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Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant—taxoid conjugates as novel cytotoxic agents

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2007.06.083 ◽

2007 ◽

Vol 17 (18) ◽

pp. 5204-5209 ◽

Cited By ~ 33

Author(s):

Kyoko Nakagawa-Goto ◽

Koji Yamada ◽

Seikou Nakamura ◽

Tzu-Hsuan Chen ◽

Po-Cheng Chiang ◽

...

Keyword(s):

Antitumor Agents ◽

Cytotoxic Agents ◽

Dietary Antioxidant

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Understanding the Role of Fibroblasts following a 3D Tumoroid Implantation for Breast Tumor Formation

Bioengineering ◽

10.3390/bioengineering8110163 ◽

2021 ◽

Vol 8 (11) ◽

pp. 163

Author(s):

Girdhari Rijal

Keyword(s):

Tumor Cells ◽

Breast Tumor ◽

Tumor Tissue ◽

Review Paper ◽

Cell Activity ◽

Tumor Formation ◽

Cancer Associated Fibroblasts ◽

Technical Challenge ◽

Signaling Systems

An understanding of the participation and modulation of fibroblasts during tumor formation and growth is still unclear. Among many speculates, one might be the technical challenge to reveal the versatile function of fibroblasts in tissue complexity, and another is the dynamics in tissue physiology and cell activity. The histology of most solid tumors shows a predominant presence of fibroblasts, suggesting that tumor cells recruit fibroblasts for breast tumor growth. In this review paper, therefore, the migration, activation, differentiation, secretion, and signaling systems that are associated with fibroblasts and cancer-associated fibroblasts (CAFs) after implantation of a breast tumoroid, i.e., a lab-generated tumor tissue into an animal, are discussed.

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Potential antitumor agents. 56. Minimal DNA-intercalating ligands as antitumor drugs: phenylquinoline-8-carboxamides

Journal of Medicinal Chemistry ◽

10.1021/jm00400a029 ◽

1988 ◽

Vol 31 (5) ◽

pp. 1048-1052 ◽

Cited By ~ 43

Author(s):

Graham J. Atwell ◽

Claudia D. Bos ◽

Bruce C. Baguley ◽

William A. Denny

Keyword(s):

Antitumor Agents ◽

Antitumor Drugs ◽

Potential Antitumor

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Clinical relevance of transmembrane drug efflux as a mechanism of multidrug resistance.

Journal of Clinical Oncology ◽

10.1200/jco.1998.16.11.3674 ◽

1998 ◽

Vol 16 (11) ◽

pp. 3674-3690 ◽

Cited By ~ 145

Author(s):

D M Bradshaw ◽

R J Arceci

Keyword(s):

Drug Resistance ◽

Cell Death ◽

Multidrug Resistance ◽

Programmed Cell Death ◽

Tumor Cells ◽

Efflux Pump ◽

Active Form ◽

Cytotoxic Agents ◽

Transport Systems ◽

Drug Efflux

For cytotoxic agents to have an effect on tumor cells, drugs must first be transported into the cell, potentially be metabolized to an active form, and interact appropriately with target molecules. A final common pathway of cytotoxic agents is usually the initiation of programmed cell death, or apoptosis. Tumor cells overcome the effects of cytotoxic agents at one or more of these levels. The classic multidrug-resistance (MDR) phenotype, as mediated by the drug efflux pump, P-glycoprotein, is one of the most extensively studied mechanisms of drug resistance. Additional drug transporters, such as the multidrug resistance-associated proteins (MRPs), have also been identified and can convey drug-resistance phenotypes. Important questions remain as to how and whether such transport systems can be specifically measured and effectively targeted to improve therapeutic outcomes. Furthermore, alterations in drug targets, drug metabolism, repair of DNA damage caused by drugs, and the inability to initiate programmed cell death can all contribute to drug resistance and must be ultimately considered in the explanation of tumor-cell resistance to therapy. Continued exploration of the pharmacologic methods to circumvent drug resistance, as well as strategies that involve targeted therapy and immunomodulation, should increase the specificity and efficacy of treatments for patients with cancer.

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ChemInform Abstract: Antitumor Agents. Part 209. Pheophorbide-a Derivatives as Photo-Independent Cytotoxic Agents.

ChemInform ◽

10.1002/chin.200220086 ◽

2010 ◽

Vol 33 (20) ◽

pp. no-no

Author(s):

Prapai Wongsinkongman ◽

Arnold Brossi ◽

Hui-Kang Wang ◽

Kenneth F. Bastow ◽

Kuo-Hsiung Lee

Keyword(s):

Antitumor Agents ◽

Cytotoxic Agents ◽

Pheophorbide A

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Use of a Rapid Throughput In Vivo Screen To Investigate Inhibitors of Eukaryotic Topoisomerase II Enzymes

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.42.4.889 ◽

1998 ◽

Vol 42 (4) ◽

pp. 889-894 ◽

Cited By ~ 17

Author(s):

Timothy R. Hammonds ◽

Anthony Maxwell ◽

John R. Jenkins

Keyword(s):

Topoisomerase Ii ◽

Antitumor Agents ◽

Viable Cell ◽

Cytotoxic Agents ◽

New Method ◽

Temperature Sensitive ◽

Cell Counts ◽

Similar Drug ◽

In Vivo Screen

ABSTRACT Topoisomerase II catalyzes the passage of one DNA helix through another via a transient double-stranded break. The essential nature of this enzyme in cell proliferation and its mechanism of action make it an ideal target for cytotoxic agents. Saccharomyces cerevisiae topoisomerase II has been frequently used as a model for testing potential inhibitors of eukaryotic topoisomerase II as antitumor agents. The standard in vivo method of estimating the sensitivity of S. cerevisiae to the antitopoisomerase drugs is via inhibition or kill curves which rely on viable-cell counts and is labor intensive. We present an alternative to this, a high-throughput in vivo screen. This method makes use of a drug-permeable S. cerevisiae strain lacking endogenous topoisomerase II, which is modified to express either human topoisomerase IIα or IIβ or S. cerevisiae topoisomerase II carried on plasmids. Each modified strain expresses a full-length topoisomerase II enzyme, as opposed to the more commonly used temperature-sensitive S. cerevisiae mutant expressing yeast or yeast/human hybrid enzymes. A comparison of this new method with a plating-and-counting method gave similar drug sensitivity results, with increased accuracy and reduced manual input for the new method. The information generated has highlighted the sensitivities of different topoisomerase II enzymes and isoenzymes to several different classes of topoisomerase II inhibitor.

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