Table 1. Kinetic parameters from... | American Society of Hematology

Table 1.

Kinetic parameters from recombinant PK-R enzymes measured with or without treatment with AG-348

Enzyme	No compound				5 μM AG-348
Enzyme	V_max, μmol/s/mg	PEP K_M, mM	k_cat, 1/s	k_cat/K_M	V_max, μmol/s/mg	PEP K_M, mM	k_cat, 1/s	k_cat/K_M	% of WT PK-R k_cat/K_M
WT	0.69	1.13	42.5	37.6	0.74	0.32	45.7	142.0	378
R532W	0.22	1.73	13.6	7.9	0.21	0.42	12.9	30.4	81
R510Q	1.60	1.45	98.8	68.1	1.64	0.32	101.5	317.3	844
R479H	0.50	1.65	30.9	18.7	0.53	0.55	32.4	58.5	156
R486W	0.34	1.45	21.2	14.6	0.39	0.25	24.2	98.4	262
G332S	0.14	2.73	8.3	3.0	0.15	1.11	9.4	8.5	23
R490W	0.37	1.52	22.8	15.0	0.39	0.51	24.2	47.6	127
G364D	0.16	2.14	10.1	4.7	0.22	0.55	13.5	24.7	65
T384M	0.11	1.42	6.9	4.8	0.12	0.37	7.2	19.3	51

Enzyme	No compound				5 μM AG-348
Enzyme	V_max, μmol/s/mg	PEP K_M, mM	k_cat, 1/s	k_cat/K_M	V_max, μmol/s/mg	PEP K_M, mM	k_cat, 1/s	k_cat/K_M	% of WT PK-R k_cat/K_M
WT	0.69	1.13	42.5	37.6	0.74	0.32	45.7	142.0	378
R532W	0.22	1.73	13.6	7.9	0.21	0.42	12.9	30.4	81
R510Q	1.60	1.45	98.8	68.1	1.64	0.32	101.5	317.3	844
R479H	0.50	1.65	30.9	18.7	0.53	0.55	32.4	58.5	156
R486W	0.34	1.45	21.2	14.6	0.39	0.25	24.2	98.4	262
G332S	0.14	2.73	8.3	3.0	0.15	1.11	9.4	8.5	23
R490W	0.37	1.52	22.8	15.0	0.39	0.51	24.2	47.6	127
G364D	0.16	2.14	10.1	4.7	0.22	0.55	13.5	24.7	65
T384M	0.11	1.42	6.9	4.8	0.12	0.37	7.2	19.3	51

k_cat, first-order rate constant; k_cat/K_M, measure of enzymatic efficiency³⁹; K_M, substrate concentration to achieve half maximal velocity; V_max, maximum velocity.

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