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

Table 3 Binding affinity (K_d), structure, and inhibitors of the critical PPIs involving MLL1 fusion proteins

PPIs	K_d (μM)	Structures (PDB)	Inhibitors
AFF4-ELL2	0.086 [190]	5JW9 [190]	None
AFF4-Cyclin T1	0.1 [191]	4IMY [191]	[192]
AFF4-P-TEFb	0.01 [191]	4IMY [191]	[192]
AFF4-Tat-P-TEFb	0.0009 [191]	4OR5 [193]	None
AF9(AHD)-AF4	0.0002 [194]	2LM0 [194]	[195]
AF9(AHD)-DOT1L	0.0016 [194]	2MV7 [196]	[197]
ENL(AHD)-DOT1L	0.2 or 1.34 [198]	None	None
AF9 or ENL AHD-CBX8	> 0.5 or 0.11 [199]	2N4Q [199]	None
AF9 or ENL AHD-BCoR	0.018 or 0.002 nM [199]	6B7G [199]	None
AF9(YEATS)-H3K9ac	3.7 [172]	4TMP [172]	[200,201,202,203,204]
ENL(YEATS)-H3K9ac	32.2 [205]	None	[200,201,202,203,204]
ENL(YEATS)-H3K27ac	30.5 [205]	5J9S [205]	[200,201,202,203,204]

ISSN: 1756-8722