AP21998 is a non-immunosuppressive derivative of Rapamycin and an inducer of exocytosis. By binding to mutant FKBP (F36M), AP21998 dissociates fusion protein aggregates in the endoplasmic reticulum into monomers, which then enter the Golgi apparatus to be cleaved by furin protease, ultimately releasing the polypeptide. AP21998 can be used in cancer research [1].
In Vitro, AP21998 (1.5 μM; 2 h) exhibits activity to induce the expression and secretion of GFP and GDNF in D407 cells that are co-transduced with TEV and GFP secretion vectors, as well as those co-transduced with TEV and GDNF secretion vectors[1].
References:
[1]. Vogel R, et al. Lentiviral vectors mediate nonimmunosuppressive rapamycin analog-induced production of secreted therapeutic factors in the brain: regulation at the level of transcription and exocytosis. Human gene therapy. 2008 Feb;19(2):167-78.
In Vitro, AP21998 (1.5 μM; 2 h) exhibits activity to induce the expression and secretion of GFP and GDNF in D407 cells that are co-transduced with TEV and GFP secretion vectors, as well as those co-transduced with TEV and GDNF secretion vectors[1].
References:
[1]. Vogel R, et al. Lentiviral vectors mediate nonimmunosuppressive rapamycin analog-induced production of secreted therapeutic factors in the brain: regulation at the level of transcription and exocytosis. Human gene therapy. 2008 Feb;19(2):167-78.