Is BIM a BH3 protein?
Is BIM a BH3 protein?
The pro-apoptotic Bcl-2-family protein Bim belongs to the BH3-only proteins known as initiators of apoptosis. Recent data show that Bim is constitutively inserted in the outer mitochondrial membrane via a C-terminal transmembrane anchor from where it can activate the effector of cytochrome c-release, Bax.
What do BH3-only proteins do?
The BH3-only proteins activate apoptosis by binding and neutralizing the pro-survival proteins, allowing Bax/Bak to homo-oligomerize and permeabilize the mitochondria.
How are BH3-only proteins activated?
In response to an apoptotic signal, the activator BH3-only proteins are either activated through multiple mechanisms (transcriptional, post-transcriptional and post-translational), or are released from the anti-apoptotic proteins by being displaced by sensitizer BH3 proteins that bind to anti-apoptotic proteins with …
What is BH3 in apoptosis?
BH3-only BCL-2 family proteins are effectors of canonical mitochondrial apoptosis. They discharge their pro-apoptotic functions through BH1-3 pro-apoptotic proteins such as BAX and BAK, while their activity is suppressed by BH1-4 anti-apoptotic BCL-2 family members.
What BH3 means?
BH3
| Acronym | Definition |
|---|---|
| BH3 | Bcl-2 Homology 3 |
What is a BH3 mimetic?
BH3 mimetics are a class of compounds that compete for this hydrophobic groove to antagonize the function of anti-apoptotic proteins. BH3 mimetics have entered the clinic and even gained regulatory approval for use in cancer.
What is Bim expression?
Bim expression and activity are regulated at the transcriptional, translational and post-translational levels; coordinated expression and activity of Bim shape immune responses, and ensure tissue integrity. Cancer cells develop mechanisms that suppress Bim expression, which allows for tumor progression and metastasis.
Does BH3 exist?
Due to absence of lone pair of electrons on H the back bonding does not occur in BH3. In other words electron deficiency of boron remains and BH3 does not exist. To reduce electron deficiency BH3 dimerises to form B2H6. Hence boron hydride exists in dimeric form and known as diborane.
What are proapoptotic BH3 mimetics?
BH3 mimetics are small compounds that antagonize anti-apoptotic BCL-2 family proteins, resulting in apoptosis induction in cancer cells [9,10]. Recently, several BH3 mimetics were identified, and accumulating evidence has shown their efficacy in cancer therapy.
