The retinoids : Therapeutic & pharmaceutical opportunities

Members of the retinoid family have long been known to be physiological regulators of a range of essential biological processes, including vision, embryonic development, reproduction, and bone formation. Similarly, their modulation of cell metabolism, growth, differentiation, proliferation and apoptosis has brought the retinoids to the forefront of oncology. Over 30 naturally occurring and synthetic analogs of retinoic acid are now either in development or on the market, targeting diverse clinical conditions ranging from various tumor types to a range of skin conditions, with more recent interest being shown in the retinoids with respect to diabetes and airway inflammation.

Much of the early development of therapeutic retinoids was underway before the advent of molecular biology. Advances in the latter have precipitated dramatic steps forward in our understanding of retinoid biology, and in particular the role of their nuclear receptors in transcriptional control, resulting in a deeper appreciation of their involvement in multiple cellular events ranging from cell differentiation to apoptosis. LeadDiscovery in collaboration with Dr Chris Berrie has recently published "Histone deacetylase inhibitors: Redefining pharmaceutical approaches to the treatment of cancer", a key analysis of the therapeutic and pharmaceutical potential of HDAC inhibitors in the control of gene transcription. LeadDiscovery and Dr Berrie now tackle the retinoids, producing one of the most up-to-date and comprehensive reviews of this alternative, and sometimes overlapping, approach to transcriptional regulation.

This 220+ page report covers all the major areas of retinoid biology and their pharmaceutical development, taking the reader through the early data describing the metabolism and transport of retinol (vitamin A), the retinyl esters, and the naturally occurring retinoic acids, and then moving on to a thorough review of the more modern molecular biology aspects of retinoid function. As the complexities behind the retinoids have been elucidated, the close coupling of the metabolism, distribution and function of the retinoids to their binding proteins, CRBPI-IV, CRABPI/II and CRALB, has become clear, thus demonstrating a further level of modulation of their intracellular effects that goes beyond that of the retinoic acid and retinoid X nuclear receptors (RARs and RXRs), and the RAR/RXR response elements. To gain a full understanding of retinoid biology it is therefore essential that researchers appreciate the combined implications of the multiple isoforms, tissue expression, and molecular biology of both these cellular retinoid-binding proteins and the retinoid receptors themselves. This report covers each of these areas, and then offers a full overview of how agonist binding to the nuclear receptors and RXR homo- and heterodimerization is able to influence transcriptional activation in conjunction with the large families of the nuclear receptor co-activators, co-repressors and co-regulatory complexes.

This review of the molecular biology of retinoid signaling naturally leads in to the involvement of this transcriptional control in the progression of various cancers. By way of a background, statistical data is provided describing incidence, mortality and survival rates, as well as current treatment options relevant to the major cancers. This report also discusses the present knowledge behind the specific physiological and molecular mechanisms by which the retinoids are able to modulate tumorigenesis.

In producing "The retinoids: Therapeutic & pharmaceutical opportunities" the authors have attempted to offer a full overview of the retinoids and to demonstrate how they can be more effectively targeted for the prevention of cancer, and it is hoped that this will support increased pharmaceutical activity in this area. To help companies justify such an increase, this report gives not just a summary of the RAR/RXR ligands and methodologies used in research, but also a full profile and analysis of retinoid-related molecules already in development or on the market.

This report can thus be considered a key tool for any company involved in molecular biology, oncology or the retinoids.

It should be noted that this report does not cover the potential involvement of the retinoids in the treatment of COPD (emphysema and bronchitis).

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