Structure, function and inhibition of critical protein–protein interactions involving mixed lineage leukemia 1 and its fusion oncoproteins

Table 1 Binding affinity (K_d), structure, and inhibitors of the critical PPIs involving MLL1

PPIs	K_d (μM)	Structures (PDB code)	Inhibitors
Menin–MLL1	0.01 or 0.082 [44, 45]	3U85 [45], 4GQ6 [46]	[16, 46,47,48,49,50,51,52,53,54,55,56,57,58,59,60,61,62,63,64,65,66,67,68]
LEDGF–Menin–MLL1	0.47 or 1.4 [45, 69]	3U88 [45]	[69, 70]
LEDGF–MLL1	14.7 [69]	2MTN [69], 2MSR [70] and 6EMQ [71]	[70]
MLL1(PHD3)-H3K4me3	19 or 30 [31, 72]	3LQJ [30]	None
MLL1(PHD3)-H3K4me2	158 [31]	3LQI [30]	None
MLL1(PHD3-BRD)-H3K4me3	4.3 [30]	3LQJ [30]	None
MLL1(PHD3-BRD)-H3K4me2	6.9 [30]	3LQI [30]	None
MLL1(PHD3)-Cyp33	14.7 [72]	2KU7 [30]	None
MLL1-CBP(KIX)	2.8 or 3.8 [73, 74]	2AGH [75]	[76,77,78]
MLL1-RbBP5-ASH2L	126 [19]	5F6L [19]	None
MLL3-RbBP5-ASH2L	0.13 [19]	5F6K [19]	None
MLL1-WDR5-RbBP5	None	3P4F [79]	None
MLL1-WDR5	0.12 or 1.7 [80, 81]	3EG6 [81], 3EMH [82], and 4ESG [83]	[36, 81, 84,85,86,87,88,89,90,91,92,93,94,95,96,97,98,99,100,101,102,103]

ISSN: 1756-8722