ALT-PG2
sEH-targeting PROTAC (Proteolysis-targeting chimera) ALT-PG2 degrades this protein at low nanomolar concentration in the human hepatoma-derived Huh-7 cell line and in primary mouse hepatocytes
General
Type : Urea derivative, Trifluo, PROTAC, Multitarget
Chemical_Nomenclature :
Canonical SMILES : C1(=CC=C(C=C1)C(=O)N(CCOCCOCCOCCN(C(=O)COC2=C3C(=CC=C2)C(N(C3=O)C4C(N(C(CC4)=O)[H])=O)=O)[H])[H])O[C@@H]5CC[C@H](CC5)N(C(=O)N(C6=CC=C(C=C6)OC(F)(F)F)[H])[H].CC
InChI : InChI=1S\/C44H49F3N6O13.C2H6\/c45-44(46,47)66-32-14-8-29(9-15-32)51-43(60)50-28-6-12-31(13-7-28)65-30-10-4-27(5-11-30)39(56)49-19-21-62-23-25-63-24-22-61-20-18-48-37(55)26-64-35-3-1-2-33-38(35)42(59)53(41(33)58)34-16-17-36(54)52-40(34)57\;1-2\/h1-5,8-11,14-15,28,31,34H,6-7,12-13,16-26H2,(H,48,55)(H,49,56)(H2,50,51,60)(H,52,54,57)\;1-2H3\/t28-,31-,34?\;
InChIKey : CTXVVVILCJCWDW-FBWMZPCKSA-N
Other name(s) :
Target
Families : ALT-PG2 ligand of proteins in family
Epoxide_hydrolase
Protein :
human-EPHX2
References (2)
| Title : Soluble epoxide hydrolase-targeting PROTAC activates AMPK and inhibits endoplasmic reticulum stress - Peyman_2023_Biomed.Pharmacother_168_115667 |
| Author(s) : Peyman M , Barroso E , Turcu AL , Estrany F, Jr. , Smith D , Jurado-Aguilar J , Rada P , Morisseau C , Hammock BD , Valverde A M , Palomer X , Galdeano C , Vazquez S , Vazquez-Carrera M |
| Ref : Biomed Pharmacother , 168 :115667 , 2023 |
| PubMedID: 37826940 |
| Gene_locus related to this paper: human-EPHX2 |
| Title : PROTAC-Mediated Selective Degradation of Cytosolic Soluble Epoxide Hydrolase Enhances ER Stress Reduction - Wang_2023_ACS.Chem.Biol__ |
| Author(s) : Wang Y , Morisseau C , Takamura A , Wan D , Li D , Sidoli S , Yang J , Wolan DW , Hammock BD , Kitamura S |
| Ref : ACS Chemical Biology , : , 2023 |
| PubMedID: 36947831 |
| Gene_locus related to this paper: human-EPHX2 |