A Suite of Activity-Based Probes To Dissect the KLK Activome in Drug-Resistant Prostate Cancer

• Published in: Journal of the American Chemical Society Vol. 143; no. 23; pp. 8911 - 8924
• Main Authors: Lovell, Scott, Zhang, Leran, Kryza, Thomas, Neodo, Anna, Bock, Nathalie, De Vita, Elena, Williams, Elizabeth D, Engelsberger, Elisabeth, Xu, Congyi, Bakker, Alexander T, Maneiro, Maria, Tanaka, Reiko J, Bevan, Charlotte L, Clements, Judith A, Tate, Edward W
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 16.06.2021
• Subjects: Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Cell Line, Tumor; Cell Proliferation - drug effects; Coumarins - chemistry; Coumarins - pharmacology; Drug Resistance, Neoplasm - drug effects; Drug Screening Assays, Antitumor; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - pharmacology; Humans; Kallikreins - antagonists & inhibitors; Kallikreins - metabolism; Male; Molecular Structure; Prostate-Specific Antigen - antagonists & inhibitors; Prostate-Specific Antigen - metabolism; Prostatic Neoplasms - drug therapy; Prostatic Neoplasms - metabolism; Prostatic Neoplasms - pathology

Kallikrein-related peptidases (KLKs) are a family of secreted serine proteases, which form a network (the KLK activome) with an important role in proteolysis and signaling. In prostate cancer (PCa), increased KLK activity promotes tumor growth and metastasis through multiple biochemical pathways, an...