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] |