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Retinoids : An A-Z guide to their biology, therapeutic opportunities and pharmaceutical development

  • ID: 16654
  • February 2003
  • Lead Discovery
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The retinoids play a key role in differentiation, proliferation and apoptosis and as a result over 30 naturally occurring and synthetic analogs of retinoic acid are now either in development or on the market. Retinoids in current use are effective in only a small number of cancers as well as acne and psoriasis. Extending this benefit to other types of cancer as well as newer indications such as diabetes and airway inflammation has represented a hurdle that will only be fully overcome by taking into account the biology of the retinoids. LeadDiscovery’s "Retinoids: An A-Z guide to their biology, therapeutic opportunities & pharmaceutical development" represents one of the most comprehensive insights into the retinoid field published in recent years. The aim of this report is to bring the reader up to date with advances in this area, pharmaceutical activity relating to retinoid development and strategies that will lead to the identification of improved retinoids.

Available retinoids are effective in treating acne and psoriasis. Likewise the retinoids are also beneficial in the treatment of acute promyelocytic leukemia, skin cancer, Kaposi's sarcoma and cutaneous T cell READ MORE >

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A (very) early history of the retinoids
- From liver to “fat soluble factor A”
- Identification and early functional characterization of vitamin A

Basic retinoid metabolism
- Vision and the retinoids
- Bioavailability of retinol
- Intestinal absorption of retinol
- Retinyl ester formation

Retinoids mobilization, storage and delivery
- Retinyl esters and chylomicrons
- Retinyl ester uptake by the liver
- Retinyl ester hydrolysis in the liver
- Bile-salt-dependent retinyl ester hydrolase (carboxylester lipase)
- Bile-salt-independent retinyl ester hydrolases
- Retinyl ester storage in the stellate cells of the liver
- Retinoids delivery to and between target cells
- Retinyl esters and chylomicrons
- Retinol and plasma retinol-binding protein
- b-Carotene and retinyl esters and plasma lipoproteins
- Retinoic acid and albumin
- The interphotoreceptor (or interstitial) retinol-binding protein (IRBP)
- The epididymus retinoic-acid binding protein (E-RABP)

Cellular retinoid-binding proteins
- The cellular retinol-binding proteins (CRBPs)
- The cellular retinoic-acid-binding proteins (CRABPs)
- The cellular retinaldehyde-binding protein (CRALBP)

Retinoic acid
- Retinoic acid biosynthesis
- The early ideas
- The alcohol dehydrogenase family
- The short-chain dehydrogenase/reductase family
- The aldehyde dehydrogenase family
- The cytochrome P450-dependent monooxygenases
- Retinoic acid and beyond
- Retinoic acid catabolism

The retinoid receptors
- The nuclear receptors
- The retinoid receptors
- The retinoic acid receptors
- The retinoid X receptors
- The RARs and RXRs as nuclear receptors
- Synthetic retinoids

The retinoids and transcriptional activation
- The retinoids response elements
- Autoregulation of retinoid signaling
- Dimerization for activation
- RXR/RAR heterodimers
- RXR homodimers
- Further RXR heterodimers
- Specificity within RXR/RAR heterodimers
- Structural determinants for dimerization

Co-regulators and transcriptional activation
- General transcription factors
- Pre-initiation complex assembly
- Further transcriptional processes
- Initiation
- Promoter clearance
- Transcript elongation
- Transcriptional termination
- Non-nuclear-receptor transcriptional co-regulators
- Nuclear receptor co-activators
- Nuclear receptor co-repressors
- General co-regulator considerations

The retinoids and cancer chemoprevention
- General introduction
- Statistical information on incidence of major cancers
- Treatment options for major cancers
- The retinoids connection
- The retinoids and cancers
- Skin cancer
- Oral cancers
- Head and neck cancers
- Breast cancer
- Lung cancer
- Pancreas cancer
- Liver cancer
- Prostate cancer
- Bladder cancer
- Colorectal cancer
- Renal cancer
- Ovarian cancer
- Thyroid cancer
- Blood cancers

Some specific mechanisms behind retinoid action
- Retinoid receptor co-regulator recruitment: further structural considerations
- The retinoic acid receptor b (RARb)
- The transcription factor AP-1
- Apoptosis, 4-HPR, and CD437
- PPARg/RXR in diet-induced obesity and type 2 diabetes

Research tools
- Reference retinoids used in research
- Methodologies

An overview of current development activity

Profiles of molecules developed as regulators of retinoid acid biology including
- adapalene (CD271)
- AGN-194310
- AGN-195183
- alitretinoin (9-cis-retinoic acid)
- bexarotene (Tagretin, LG-1069)
- etretinate (Tigason, Ro 10-9359)
- fenretinide (4-HPR)
- isotretinoin (13-cis-retinoic acid)
- LGD-1550
- MDI-101
- MDI-301
- MDI-403
- motretinide (Ro 11-1430)
- PLT-99257
- PLT-99511
- R-667
- rambazole
- RAR?2 gene therapy
- tazarotene (AGN-190168)
- tocoretinate
- tretinoin (all-trans-retinoic acid, vitamin A acid)
- UAB-30

Companies involved in retinoid biology

Note: Product cover images may vary from those shown
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Note: Product cover images may vary from those shown