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Table 2 Promising mimetics and inhibitor therapeutic agents for cancer

From: BH3-mimetics: recent developments in cancer therapy

Agent Type Origins Target Off-Target Developer Ref
ABT-737 BH3-M Structure-based design,
BAK peptide
Bcl-2, Bcl-xL Abbott Labs. (IL, USA) [58]
Navitoclax BH3-M ABT-737 Bcl-2, Bcl-xL, Mcl1 Mcl1 (weak) Abbott Labs. (IL, USA) [59]
Gossypol
(AT-101)
BH3-M Structure-based design,
BIM peptide
Bcl-2, Bcl-xL, Mcl1 University of Michigan (MI, US) [60]
Obatoclax BH3-M In silico docking studies Bcl-2, Mcl1 Bcl-xL University of Montreal (CAN) [61]
Venetoclax BH3-M Navitoclax Bcl-2 Bcl-xL (weak) AbbieVie (IL, USA) [62]
Compound 3 Smac-M Smac (AVPI/AVPF
peptide sequence)
xIAP, cIAP1/2 NF-κB activation University of Texas (TX, USA) [63]
[64]
APG1387 Smac-M Smac (AVPI peptide sequence) xIAP, cIAP1/2 University of Michigan (MI, USA) [65]
AT-406 Smac-M Structure-based design xIAP, cIAP1/2 University of Michigan (MI, USA) [66]
Compound A Smac-M Small molecule screen xIAP, cIAP1/2 University of Texas (TX, USA) [63]
LC161 Smac-M Structure-based design xIAP, cIAP1/2 Dana-Farber CI (MA, US) [67]
SM-164 Smac-M Structure-based design xIAP University of Michigan (MI, USA) [68]
Birinapant Smac-M Smac (AVPI peptide sequence) cIAP1 xIAP (weak) Duke University (NC, USA) [69]
A1210477 Mcl1-I High throughput screen Mcl1 AbbieVie (IL, USA)
Genetech (CA, US)
[70]
[71]
AMG-176 Mcl1-I Structure-based design,
High throughput screen
Mcl1 Bcl-2, Bcl-xL (minimal) Amgen (CA, USA) [72]
AZD-5991 Mcl1-I Structure-based design Mcl1 AstraZeneca (MA, US) [73]
S63845 Mcl1-I In-silico modelling Mcl1 Institut de Recherches Servier Oncology (FRA) [74]
MIM1 Mcl1-I Small molecule screen Mcl1 Dana-Farber CI (MA, USA) [75]
VU661013 Mcl1-I Structure-based design Mcl1 BIM-Mcl1 destabilization Vanderbilt University (TN, USA) [76]
[77]
GDC-0941 Mcl1-I In-silico modelling PI3Kα/δ, Mcl1 Piramed Pharma (UK) [78]
  1. BH3-mimetics (-M), Smac-mimetics (-M) and Mcl1 inhibitors (-I) are highlighted along with the techniques utilized for their discovery or origins. For each drug, we show its cognate target and off-target proteins or effects, its developer and the publication describing its development (Ref)