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. Author manuscript; available in PMC: 2018 Dec 4.

Published in final edited form as: Pharmacogenet Genomics. 2012 Aug;22(8):561–576. doi: 10.1097/FPC.0b013e328354026b

Table 1.

Kinetic analysis of UGTs active against CLZ in vitro.

	CLZ-5-N-glucuronide			CLZ-N⁺-glucuronide			dmCLZ-5-N-glucuronide
UGT variant	V_max (pmol·min⁻¹·μg⁻¹)^*	K_M (μM)	V_max/K_M (nl·min⁻¹·μg⁻¹)^*	V_max (pmol·min⁻¹·μg⁻¹)^*	K_M (μM)	V_max/K_M (nl·min⁻¹·μg⁻¹)^*	V_max (pmol·min⁻¹·μg⁻¹)^*	K_M (μM)	V_max/K_M (nl·min⁻¹·μg⁻¹)^*
UGT1A1	nd	nd	nd	0.86 ± 0.02^a,b	53 ± 2^a,b	17 ± 0.6^a	no activity detected
UGT1A4^24Pro/48Leu	42 ± 3	173 ± 19	246 ± 31	6.3 ± 0.6	768 ± 62	8.2 ± 0.8	10 ± 0.7	379 ± 46	28 ± 2.8
UGT1A4^24Thr/48Leu	33 ± 2^b,c	167 ± 19^d	196 ± 14^b,c	3.6 ± 0.1^a,b	459 ± 23^e	7.8 ± 0.3^b	6.4 ± 0.9^b,e	440 ± 45^b	15 ± 1.5^b,e
UGT1A4^24Pro/48Val	93 ± 9^a	73 ± 8^e	1284 ± 77^a	7.6 ± 0.1^c	481 ± 9^e	16 ± 0.2^a	17 ± 1.3^d	173 ± 22^e	96 ± 8.0^a

^*

Michaelis-Menten kinetic values represent per μg UGT protein. nd = not detected, below the limits of UPLC detection.

^a

p<0.0001,

^b

p<0.0001,

^c

p<0.05,

^d

p<0.002 versus corresponding value for UGT1A4^24Pro/48Val-over-expressing cell homogenate, calculated using the Students t-test (two-sided).

^e

p<0.001 versus corresponding value for UGT1A4^24Pro/48Leu-over-expressing cell homogenate, calculated using the Students t-test (two-sided).