Terutroban exhibits antagonist activity against the human thromboxane A2 receptor alpha with an IC50 value of 16.4 nM, as assessed through the reduction of I-BOP-induced inositol monophosphate production in QBI-HEK293A cells. This compound also shows antiviral effects, inhibiting SARS-CoV-2 induced cytotoxicity in both Caco-2 and VERO-6 cells at 10 µM concentration, though with relatively low inhibition percentages of 5.7% and -0.15%, respectively. Additionally, it inhibits SARS-CoV-2 3CL-Pro protease activity by 2.655% at 20 µM concentration.
Moreover, Terutroban demonstrates inhibitory activity on the human HDAC6 enzyme, with an inhibition of 3.38% using a commercial peptide substrate and just 0.11% with a custom peptide substrate. It also affects cell viability differently across cell lines, enhancing growth in HEK293T cells but inhibiting it in U2OS and human fibroblast cells, indicating a variable bioactivity profile.
In terms of protein thermal stability, Terutroban has mixed effects, increasing the melting temperature in some protein regions by 0.1 to 0.54 degrees Celsius while decreasing it in others by -0.38 to -2.74 degrees Celsius, which suggests complex, domain-specific protein interactions.
Furthermore, the compound impacts GPCR beta-arrestin recruitment, exhibiting both agonistic and inhibitory effects on targets such as GLP1R, GPR35, AGTR1, C5AR1, FPR2, S1PR1, ADRB2, GPR119, CX3CR1, APLNR, FFAR4, and ADRA2A. This indicates Terutroban's potential modulatory role in various GPCR signaling pathways relevant to diverse physiological processes..
Note: Summary generated by AI. Data source: ChEMBL 