Human PRMT5:MEP50 structure with Fragment 3 and MTA Bound

2-Gaussian fit: Grosse-Kunstleve RW, Sauter NK, Adams PD: Newsletter of the IUCr Commission on Crystallographic Computing 2004, 3, 22-31.

Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits.

72 kDa ICln-binding protein,Histone-arginine N-methyltransferase PRMT5,Jak-binding protein 1,Shk1 kinase-binding protein 1 homolog,SKB1Hs

MEP-50,Androgen receptor cofactor p44,WD repeat-containing protein 77,p44/Mep50

10% PEG 8000, 100 mM Sodium Citrate 5.4, 100 mM Sodium Acetate

MTAP, methyl transferase, fragment-based lead discovery, FBDD, TRANSFERASE