Enzyme Source | fu,inc | Km,u | Vmax | Clint,u | Clint,organ |
---|---|---|---|---|---|
µM | pmol/min/mg protein | µl/min/mg mics | l/h per organ | ||
Cabotegravir | |||||
HLMs | 0.52 | 350 (41) | 705 (35) | 2.0 | 8.1 |
HIMs | 0.69 | NDa | 1031 (323) | NDa | NDa |
HKMs | 0.50 | 560 (57) | 1088 (56) | 1.9 | 0.45 |
Dolutegravir | |||||
HLMs | 0.23 | 32 (2) | 601 (13) | 18 | 76 |
HIMs | 0.37 | 96 (7) | 1170 (33) | 12 | 2.1 |
HKMs | 0.29 | 47 (8) | 291 (16) | 6.2 | 1.1 |
Raltegravir | |||||
HLMs | 1 | 183 (23) | 1737 (63) | 9.5 | 38.7 |
HIMs | 1 | 167 (23) | 326 (13) | 2.0 | 0.3 |
HKMs | 0.97 | 493 (59) | 2332 (111) | 4.7 | 0.5 |
↵a The substrate concentration versus velocity did not saturate, and the estimated Km (>6 mM) and Vmax values were unreliable. Thus, the values are not presented, and Clint,u and Clint,organ were not determined (ND).
Micr, microsomal protein.