Drug intelligence / Profile preview

MLN-273

Development stage
Preclinical
Lead developer
Millennium Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous, Intraperitoneal
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Overview

MLN-273 is a small molecule dipeptidyl boronic acid inhibitor of the 20S proteasome, originally developed by Millennium Pharmaceuticals. It selectively inhibits proteasomal protease activity in both mammalian and pathogenic cells. Studies have demonstrated its ability to block the development of Plasmodium parasites (malaria) in both blood and liver stages and to inhibit growth and protein degradation essential for parasite replication. MLN-273 has also shown activity against the proteasome of Mycobacterium tuberculosis and has been investigated for in vivo efficacy in models of viral hepatitis and other diseases. Unlike some other proteasome inhibitors like bortezomib, MLN-273 exhibits a longer half-life, which may provide advantages in certain therapeutic settings[1][3][5][9][7].

02

Targets

PSMB5 (Proteasome subunit beta Type-5)PSMB6 (Proteasome 20S subunit beta 6)PSMB7 (Proteasome subunit beta type-7)PrcB (Mycobacterium tuberculosis 20S proteasome beta subunit)

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