From Plant to Patient: Thapsigargin, a Tool for Understanding …
93
Fig. 15 In the prostate, PSA is active and cleaves the prodrug. In blood vessels, PSA in inactivated
by binding to proteins
Fig. 16 Prodrug cleaved at
the surface of
PSMA-producing cells to
give promoiety
(extracellular) and toxin
intracellular after penetration
of the cell membrane
prostate, brain, and lung cancer, but is not found in significant amounts outside the
prostate gland in healthy humans [94, 178–181]. The unusual substrate specificity
of this enzyme for cleaving a very polar substrate and the overexpression of PMSA
in many tumors makes it an interesting target for prodrugs.
93
Fig. 15 In the prostate, PSA is active and cleaves the prodrug. In blood vessels, PSA in inactivated
by binding to proteins
Fig. 16 Prodrug cleaved at
the surface of
PSMA-producing cells to
give promoiety
(extracellular) and toxin
intracellular after penetration
of the cell membrane
prostate, brain, and lung cancer, but is not found in significant amounts outside the
prostate gland in healthy humans [94, 178–181]. The unusual substrate specificity
of this enzyme for cleaving a very polar substrate and the overexpression of PMSA
in many tumors makes it an interesting target for prodrugs.