LE-135

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LE-135

LE-135 is a synthetic compound that acts as a selective antagonist of the retinoic acid receptor beta (RARβ). It is primarily used in research settings to study the role of RARβ in various biological processes, including development, differentiation, and disease.

Chemical Structure and Properties[edit | edit source]

LE-135 is a small molecule with a complex chemical structure that allows it to specifically bind to the RARβ receptor, inhibiting its activity. The molecular formula of LE-135 is C26H27NO3, and it has a molecular weight of 401.5 g/mol. The compound is characterized by its high affinity for RARβ, with minimal activity on other retinoic acid receptors such as RARα and RARγ.

Mechanism of Action[edit | edit source]

LE-135 functions by competitively binding to the ligand-binding domain of RARβ, preventing the natural ligand, retinoic acid, from activating the receptor. This inhibition blocks the transcriptional activity of RARβ, which is involved in regulating gene expression related to cell growth, differentiation, and apoptosis. By inhibiting RARβ, LE-135 can be used to dissect the specific roles of this receptor in various cellular processes.

Applications in Research[edit | edit source]

LE-135 is widely used in biomedical research to explore the functions of RARβ in:

  • Developmental Biology: Studies using LE-135 have provided insights into the role of RARβ in embryonic development, particularly in the formation of the central nervous system and limb patterning.
  • Cancer Research: LE-135 has been used to investigate the involvement of RARβ in cancer, as alterations in retinoic acid signaling are implicated in the pathogenesis of several cancers, including breast and lung cancer.
  • Neuroscience: Research has utilized LE-135 to study the effects of RARβ on neural differentiation and neuroplasticity, contributing to our understanding of neurodegenerative diseases and potential therapeutic approaches.

Safety and Handling[edit | edit source]

As with many research chemicals, LE-135 should be handled with care. Appropriate safety measures, including the use of personal protective equipment (PPE) such as gloves and goggles, should be employed when handling the compound. It should be stored in a cool, dry place, away from light and moisture to maintain its stability.

Also see[edit | edit source]

Template:Retinoic Acid Receptor Antagonists

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Contributors: Prab R. Tumpati, MD