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A Novel Inhibitor of HSP70 Induces Mitochondrial Toxicity and Immune Cell Recruitment in Tumors
Journal article   Open access   Peer reviewed

A Novel Inhibitor of HSP70 Induces Mitochondrial Toxicity and Immune Cell Recruitment in Tumors

Thibaut Barnoud, Jessica C Leung, Julia I-Ju Leu, Subhasree Basu, Adi Narayana Reddy Poli, Joshua L D Parris, Alexandra Indeglia, Tetyana Martynyuk, Madeline Good, Keerthana Gnanapradeepan, …
Cancer research (Chicago, Ill.), v 80(23), pp 5270-5281
01 Dec 2020
PMID: 33023943
url
https://doi.org/10.1158/0008-5472.CAN-20-0397View
Published, Version of Record (VoR)Maybe Open Access (Publisher Bronze) Open

Abstract

Adenosine Triphosphate - metabolism Alarmins - metabolism Animals Antineoplastic Agents - pharmacology Cell-Free System Colorectal Neoplasms - drug therapy Colorectal Neoplasms - immunology Colorectal Neoplasms - metabolism Colorectal Neoplasms - pathology High-Throughput Screening Assays HMGB1 Protein - metabolism HSP70 Heat-Shock Proteins - antagonists & inhibitors HT29 Cells Humans Male Mice, Inbred C57BL Mice, Inbred NOD Mitochondria - drug effects Mitochondria - metabolism Xenograft Model Antitumor Assays
The protein chaperone HSP70 is overexpressed in many cancers including colorectal cancer, where overexpression is associated with poor survival. We report here the creation of a uniquely acting HSP70 inhibitor (HSP70i) that targets multiple compartments in the cancer cell, including mitochondria. This inhibitor was mitochondria toxic and cytotoxic to colorectal cancer cells, but not to normal colon epithelial cells. Inhibition of HSP70 was efficacious as a single agent in primary and metastatic models of colorectal cancer and enabled identification of novel mitochondrial client proteins for HSP70. In a syngeneic colorectal cancer model, the inhibitor increased immune cell recruitment into tumors. Cells treated with the inhibitor secreted danger-associated molecular patterns (DAMP), including ATP and HMGB1, and functioned effectively as a tumor vaccine. Interestingly, the unique properties of this HSP70i in the disruption of mitochondrial function and the inhibition of proteostasis both contributed to DAMP release. This HSP70i constitutes a promising therapeutic opportunity in colorectal cancer and may exhibit antitumor activity against other tumor types. SIGNIFICANCE: These findings describe a novel HSP70i that disrupts mitochondrial proteostasis, demonstrating single-agent efficacy that induces immunogenic cell death in treated tumors.

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Collaboration types
Domestic collaboration
Web of Science research areas
Oncology
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