Bcl-2 is a family of evolutionarily related proteins. These proteins govern mitochondrial outer membrane permeabilization (MOMP) and can be either pro-apoptotic (Bax, Bad, Bak and Bok among others) or anti-apoptotic (including Bcl-2 proper, Bcl-xL, and Bcl-w, among an assortment of others). There are a total of 25 genes in the Bcl-2 family known to date. Human genes encoding proteins that belong to this family include: Bak1, Bax, Bal-2, Bok, Mcl-1.
a) Schematic representation of BCL-2 family proteins identifying BCL-2 homology (BH) and transmembrane-targeting (TM) regions with respect to the BCL-2 core. At the left, the cartoons illustrate the structured, globular (rounded) or unstructured, intrinsically disordered (noodle-like) nature of the particular class of BCL-2 family proteins. The approximate position of α-helices in the BCL-2 core is marked at the bottom. Helices that delineate the BC groove are highlighted in red. b) The functional interaction network between pro- and anti-apoptotic BCL-2 family members is color coded as in panel a. c) The structure of the BCL-2 core of BCL-xL identifies the BH regions and α-helices colored as in panel a. d) A representative structure highlighting the BH3-into-BC groove interaction for the complex between BCL-xL and the BH3 region of BAD (shown in red). The conserved Leu and Asp side chains of BAD BH3 are engaged in hydrophobic and electrostatic interactions, respectively, with complementary sites in the BCL-2 core. PDB identifiers are shown at the bottom.
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BCL6 inhibitor 79-6 (Compound 79-6) is the first-generation, specific BCL6 BTB domain inhibitor with IC50 of 200 uM, Kd of 129 uM; binds to a pocket in the lateral groove of the BCL6 BTB domain, specifically inhibits BCL6 but not other BTB-ZF proteins; disrupts BCL6/corepressor complexes and reactivates BCL6 target genes in vitro and in vivo, selectively kills BCL6-dependent DLBCL cells; suppresses human DLBCL xenografts in mice with favorable pharmacokinetics.
A potent, specific BCL6 BTB domain inhibitor with Kd of 7 uM, binds with a greater affinity than the natural BCL6 ligand SMRT (Kd=30 uM); exhibits 10-fold greater inhibitory activity against the BCL6 BTB domain in reporter assays with IC50 of 35 uM, displays good selectivity against a panel of 50 different kinases; disrupts formation of the BCL6 repression complex, reactivates BCL6 target genes, suppresses ABC-DLBCL cells in vitro and in vivo, as well as primary human ABC-DLBCL specimens ex vivo.
S-63845 (S63845) is a highly potent, selective Mcl-1 inhibitor with Kd of 0.19 nM, with no appreciable binding affinity to BCL-2 or BCL-XL (Ki>10 uM); binds to the BH3-binding groove of Mcl-1, potently kills MCL1-dependent cancer cells, including multiple myeloma (IC50<0.1 uM), leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway; is well tolerated and shopws high effectivity against mouse cancer models.
Pyridoclax (MR29072) is a highly potent Mcl-1 inhibitor with Kd of 25 nM, disrupts Mcl-1/Bim interaction; strongly sensitizes ovarian cancer chemoresistant IGROV1-R10 cells to Bcl-xL targeting siRNA and ABT-737, leading to massive apoptosis, can not induce cell death as single agents; induces ER stress and modifies Bcl-2 family expression, but its cytotoxic effect does not require these events.
BDA-366 is a potent, selective Bcl2 BH4 domain antagonist with Ki of 3.3 nM; shows no affinity for other Bcl2 family members, including Bcl-XL, Mcl-1, or Bfl-1/A1; induces apoptotic cell death in a Bax-dependent manner, and induces calcium (Ca2+) release via inhibition of Bcl2/IP3R interaction; potently represses lung cancer in vivo, and induces Bcl2 conformational change in tumor tissues.
Mcl-1 inhibitor 26
Mcl-1 inhibitor 26 is a novel potent, selective Mcl-1 inhibitor with IC50 of <3 nM in FRET assays; displays >1,000-fold selectivity over Bcl-2 and Bcl-xL; induces cleaved caspase-3 in MV4-11 cells with IC50 of 3.78 uM.
MIK665 (S-64315, MIK-665) is a novel potent, selective Mcl-1 inhibitor with potential pro-apoptotic and antineoplastic activities; binds to and inhibits the activity of Mcl-1, which promotes apoptosis of cells overexpressing Mcl-1. Mcl-1, an anti-apoptotic protein belonging to the Bcl-2 family of proteins, is upregulated in cancer cells and promotes tumor cell survival.
BCL6 inhibitor 14
BCL6 inhibitor 14 is a potent BCL-6 inhibitor with FRET IC50 of 63 nM.
BRD1991 is a small molecule that selectively disrupt Beclin 1/Bcl-2 binding as compared to Bax/Bcl-2 and Bim/Bcl-2 binding and induces autophagic flux at concentrations with minimal cytotoxicity.
SW076956 is a small molecule that selectively disrupt Beclin 1/Bcl-2 binding as compared to Bax/Bcl-2 and Bim/Bcl-2 binding and induces autophagic flux at concentrations with minimal cytotoxicity.
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