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Current Pharmaceutical Biotechnology, Vol. 2, No. 1, 2001

Contents

Nonviral Gene Therapy and its Delivery Systems Pp.1-17

Haiching Ma and Scott L. Diamond

[Abstract]

 

Antibody Engineering for Targeted Therapy of Cancer: Recombinant Fv-Immunotoxins Pp.19-46

Revital Niv, Cyril J. Cohen, Galit Denkberg, Dina Segal and Yoram Reiter

[Abstract]

Genetically Modified Viruses: Vaccines by Design Pp. 47-76

John R. Stephenson

[Abstract]

Small Heat Shock Proteins (sHSPs) As Potential Drug Targets Pp. 77-111

M. James C. Crabbe and Henry W. Hepburne-Scott

[Abstract]

 


Abstracts

[Back to top]  Nonviral Gene Therapy and its Delivery Systems

Haiching Ma and Scott L. Diamond

 

Nonviral gene therapy has significant clinical potential, yet its therapeutic utility has been hindered by low transfection efficiency due to a combination of extracellular and intracellular barriers. Recent developments in formulation and delivery methodology have allowed a number of advances toward high efficiency gene delivery to various cell types and organs. In particular, the extracellular and intracellular pharmacokinetics of plasmid DNA trafficking are better understood in a number of cell systems. Using cationic lipid or polymers (often with receptor targeting), more than 105 plasmids can be delivered to a single cell. Endosomolytic agents promote endosome disruption, and include: weak bases, proton-sponge polymers, fusogenic peptides, viral particles, and photosensitizing compounds. Both classical and nonclassical nuclear localization signal (NLS) peptides have also been tested for enhancement of the probability of nuclear import events, a major rate-limiting step in DNA delivery to nondividing cells. For example, the M9 sequence from heterogeneous nuclear ribonucleoprotein A1 (hnRNP A1) protein, a non-classical NLS, has been found to increase gene expression level by more than 10 to 150-fold in a variety of cell types. This review will concentrate on the current understandings of the basic mechanisms of nonviral gene delivery and new approaches in the field.

 

[Back to top] Antibody Engineering for Targeted Therapy of Cancer: Recombinant Fv-Immunotoxins

Revital Niv, Cyril J. Cohen, Galit Denkberg, Dina Segal and Yoram Reiter

 

Recombinant Fv-immunotoxins are a new class of biologic anticancer agents composed of a recombinant antibody fragment linked to a very potent bacterial toxin. These potent molecules are designed to specifically bind and kill cancer cells that express a specific target antigen on their cell surface. Recombinant Fv-immunotoxins are an excellent example for the concept of rational drug design. They combine the progress in understanding cancer biology, -the recent knowledge on the mechanisms of malignant transformation and the special properties of cancer cells, -with the enormous developments in recombinant DNA technology and antibody engineering.

 

Recombinant Fv immunotoxins were developed for solid tumors and hematological malignancies and have been characterized intensively for their biological activity in vitro and in vivo in animal models. The excellent in vitro and in vivo activities of recombinant Fv-immunotoxins have lead to their pre-clinical development and to the initiation of clinical trial protocols.

 

Recent trials have demonstrated potent clinical efficacy in patients with malignant diseases that are refractory to traditional modalities of cancer treatment.

 

It is thus suggested that this strategy can be developed into a separate modality of cancer treatment with the basic rationale of specifically targeting cancer cells on the basis of their unique surface markers combined with potent effective biological toxic agents that directly kill the cancer cell. Efforts are now being made to improve the current molecules and to develop new agents with better clinical efficacy. In this review, we will describe the rationale in designing Fv-immunotoxins and will review current progress made in using thes agents for cancer treatment.

 

[Back to top] Genetically Modified Viruses: Vaccines by Design

John R. Stephenson

.

Vaccination has been one of the most successful and cost-effective health interventions ever employed. One disease (smallpox) has been eradicated, another (poliomyelitis) should disappear early in the new millennium and a third (measles) should follow shortly after. Conventional vaccines usually depend on one of three development processes, attenuation of virulent organisms (by passage in cell culture and/or experimental animals), killing of virulent organisms (by chemical inactivation) or the purification of immunogenic molecules (either proteins or carbohydrates) from whole organisms.

 

These traditional processes, although serendipitous and poorly understood, have produced effective pharmaceutical products which give excellent protection against diseases such as smallpox, rabies, measles, yellow fever, tetanus and diphtheria. In spite of these successes however, the application of these protocols have failed to produce safe and efficacious vaccines against other infectious diseases which kill or maim tens of millions of people every year. The most important of these are malaria, AIDS, herpes, dengue fever and some forms of viral hepatitis.

 

Consequently, fundamentally new technologies are required to tackle these important infections. One of the most promising has been the development of genetically modified viruses. This process normally involves taking a proven safe and efficacious vaccine virus, such as vaccinia or adenovirus, and modifying its genome to include genes coding for immunogenic proteins from other viruses such as HIV or measles. This review will describe the generation of such novel vaccine vectors and compare their advantages and shortcomings. In addition the literature describing their use as experimental vaccines will also be reviewed.

 

[Back to top]  Small Heat Shock Proteins (sHSPs) As Potential Drug Targets

M. James C. Crabbe and Henry W. Hepburne-Scott

 

Small heat shock proteins (sHSPs) belong to a family of 12- to 43-kDa proteins that are ubiquitous and are largely conserved in amino acid sequence among all organisms.

 

The principal heat-shock proteins that have chaperone activity (that is, they protect newly made proteins from misfolding) belong to five conserved classes: HSP100, HSP90, HSP70, HSP60 and the small heat-shock proteins (sHSPs). The sHSPs (which include alpha crystallin) can form large multimeric structures and have a wide range of cellular functions, including endowing cells with thermotolerance in vivo and being able to act as molecular chaperones in vitro; sHSPs do this by forming stable complexes with folding –or unfolding- intermediates of their protein substrates, probably the molten globule.

 

This paper includes: a brief survey of the chaperone family, the small heat shock protein superfamily, transcription of sHSPs, sequence comparisons and structural models of small heat shock proteins – structural elements as potential drug targets, sHSPs as chaperone-like proteins, alpha crystallin chaperone-like activity, conformational diseases – the role of alpha crystallin small heat shock protein superfamily proteins, post-translational modification and useful pharmacological agents.

 

Functionality of small heat shock proteins – targets and diseases where pharmacologically active agents are of importance, alpha crystallin- small heat shock proteins and prion diseases: specific targets for diagnostic tests and drug development, details of some specific small heat shock proteins as drug targets, structural and functional implications for treatment.