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Target intelligence / Profile preview
Bestrophin-3 (BEST3)
- Target
- BEST3
- Molecular classification
- Ion channel, Ligand-gated anion channel, Calcium-activated chloride channel
01
Overview
Bestrophin-3 (BEST3) is a calcium-activated anion channel that belongs to the bestrophin family, which includes BEST1, BEST2, and BEST4[2][5]. BEST3 forms homo-pentameric channels in the plasma membrane, permitting the flow of monovalent anions, especially chloride, in response to rises in intracellular calcium[1][3]. It is widely expressed in various tissues, including vascular smooth muscle, where it is essential for cGMP-dependent, calcium-activated chloride conductance[1][4]. BEST3 is implicated in diseases such as vitelliform macular dystrophy and esophagus squamous cell carcinoma[2]. The channel can be pharmacologically inhibited by several non-specific chloride channel blockers, but no selective inhibitors are currently available[1].
- Other names
- Bestrophin-3BEST3VMD2L3MGC40411MGC13168Vitelliform macular dystrophy 2-like protein 3vitelliform macular dystrophy 2-like 3
02
Mechanism of action
Blockade of Ca2+-activated chloride channels; Inhibition of anion flow (by above agents)
03
Biological functions
Regulation of chloride ion transportCalcium-activated anion conductanceIntracellular signaling related to membrane potential and ion homeostasis
04
Disease associations
Vitelliform macular dystrophyEsophagus squamous cell carcinomaCardiovascular disease (through its role in vascular smooth muscle function)
05
Safety considerations
Non-specificity of channel blockers (most available inhibitors also act on other chloride channels)Incomplete understanding of its systemic role and possible off-target effects with channel modulation
06
Interacting drugs
Niflumic acid
4 more in the full profile.
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