Identification of Breast Cancer - Specific Proteolytic Activities for Targeted Prodrug Activation

Denmeade, Samuel R.

doi:10.21236/ada443732

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The Klk Family1

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2009

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Cited by 1 publication

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“…5). In addition, PSA-activated prodrugs have been designed for treatment of prostate cancer based on the fact that serum PSA is mostly enzymatically inactive, whereas in the prostate gland, it is found in its active form (6). Notably, administration of recombinant KLK6 to mice with EAE resulted in the production of anti-KLK6 antibodies that inhibited its enzymatic activity, attenuated the severity of symptoms, and delayed the course of disease progression (7).…”

Section: The Klk Familymentioning

confidence: 99%

Functional Roles of Human Kallikrein-related Peptidases

Sotiropoulou

Pampalakis

Diamandis

2009

Journal of Biological Chemistry

195

194

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Kallikrein-related peptidases constitute a single family of 15 (chymo)trypsin-like proteases (KLK1-15) with pleiotropic physiological roles. Aberrant regulation of KLKs has been associated with diverse diseases such as hypertension, renal dysfunction, skin disorders, inflammation, neurodegeneration, and cancer. Recent studies suggested that coordinated activation and regulation of KLK activity are achieved via a complex network of interactions referred to as the "KLK activome." However, it remains to be validated whether these hypothetical KLK activation cascade pathways are operative in vivo. In addition, KLKs have emerged as versatile signaling molecules. In summary, KLKs represent attractive biomarkers for clinical applications and potential therapeutic targets for common human pathologies.

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Section: The Klk Familymentioning

confidence: 99%