EP39 

EP39 is a potent HIV-1 maturation inhibitor. EP39 interacts with the SP1 domain of Gag. EP39 decreases the dynamics of CA-SP1 junction, by binding to the QVT motif of the SP1 domain, and perturbs the natural coil-helix equilibrium on both sides of the SP1 domain by stabilizing the transient alpha helical structure. EP39 acts by arresting maturation of HIV-1 thereby blocking its infectivity^[1].

EP39 has binding affinity to different residues of SP1. SP1-T²³⁹ has the highest binding affinity (52.4 μM); SP1-S²³⁶, SP1-Q²³⁷ and SP1-V²³⁸ have relatively high binding affinities (179.6 μM, 154,5 μM and 204.4 μM, respectively); SP1-E²³³, SP1-M²³⁵ and NC-T²⁵⁷ have medium binding affinities (237.0 μM, 235,4 μM, 308.4 μM, respectively); CA-V²²¹, CA-L²³¹ and SP1-A²³² have weak binding affinities (669.6 μM, 678.4 μM and 691.9 μM, respectively) ^[1].
EP39 perturbs the natural coil-helix equilibrium on both sides of the SP1 domain by stabilizing the transient alpha helical structure^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

626.91

C₃₈H₆₂N₂O₅

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• [1]. Chen X, et, al. The HIV-1 maturation inhibitor, EP39, interferes with the dynamic helix-coil equilibrium of the CA-SP1 junction of Gag. Eur J Med Chem. 2020 Oct 15;204:112634.  [Content Brief]