Skip to main content
. 2021 Apr 20;13(8):1981. doi: 10.3390/cancers13081981

Table 2.

YAP/TAZ-inhibiting drugs.

Groups Targets Substances Effects Ref.
Group I Upstream proteins, SFKs, AMPY, Phosphatases, EGFR, CPCR, Integrins, Adenylyl cyclase families, gamma-secretase, ErbB signaling, ILK Kinase inhibitors, MEK/MAK inhibitors (trametinib, CAY10561, FR180204), Gamma secretase inhibitors, Epigenetic modulators (Panobinostat, Dacinostat, vorinostat), Actine modulators (Blebbistatin, ML-7, Cytochalasin D, Latrunculin A), Phosphatases inhibitors (okadaic acid, Calyculin A), SK2 inhibitors (Dasatinib, PP2, SV6656, AZ D0530), PI3 K inhibitors (BX795, Wortmannin/LY294002, Temserolimus, MLN0128), Mevalonate pathway inhibitors (statins, zoledronic acid), Cellular stress modulators (metformin, phenformin), AICAR.
Erlotinib, AG-1478, Losartan, Dihydrexidine, Gallein, Clengitide, Agrin, RGD peptides, VEGFR inhibitors (Apatinib, SU4312, Axitinib, Pazopanib), Forskoli, Theophylline, IBMX, Odulilast, Rolipran, Dibenzapine, QLT0267, FAK inhibitors (PF-562271, PF-573228, CT-707)
Activate YAP and TAZ, promote TAZ degradation [204,205,206,207]
Group II Disruptors preventing the formation of the YAP/TAZ-TEAD complex Verteporfin, YAP cyclic peptide (peptide 17), cystine-dense peptide (TB1 G1), Vgll1–4, substances targeting TEADs’ palmitate-binding pocket (fenamate derivatives, vinylsulfonamide derivatives, K-975) Target either TEAD family of transcription factors or YAP/TAZ [146,147,148,204,208,209]
Group III Downstream YAP/TAZ targets: metabolic enzymes (aldehyde dehydrogenase, aspartate transaminase, cyclooxygenase 2), kinases, ligands and proteins (BCL-xL, FOXM1, TG2) A37, celecoxib, WZ400, CXCL5 neutralizing antibody, SB255002, Jagged-1 neutralizing antibody, deoxybouvardin, CYR61 (093 G9) antibodies, navitoclax, thiostrepton, NC9 Inhibition of proteins that are expressed under YAP/TAZ influence [204]