Synthesis of an Hsp70 inhibitor and its assessment of lysosomal membrane permeabilization.

Abstract

Hsp70 inhibitors have great potential as chemical probes and anticancer agents. Thus, it is important to elucidate their modes of action on cancer cell death. This protocol describes a step-by-step process for the synthesis of apoptozole as an inhibitor of Hsp70, analysis of internalization of apoptozole into lysosomes, and assessment of lysosomal membrane permeabilization induced by apoptozole. The current protocol can be used for detailed mechanistic studies of Hsp70 inhibitors and further substances targeting lysosomal proteins on cancer cell death. For complete information on the use and execution of this protocol, please refer to Park et al. (2018).

• Authors: Sang-Hyun Park, Sookil Park, Injae Shin
• Journal: STAR protocols (STAR Protoc) Vol. 2 Issue 1 Pg. 100349 (03 19 2021) ISSN: 2666-1667 [Electronic] United States
• PMID: 33665629 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2021 The Author(s).

Chemical References

• Antineoplastic Agents
• HSP70 Heat-Shock Proteins

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacokinetics, pharmacology)
• Cell Line, Tumor
• HSP70 Heat-Shock Proteins (antagonists & inhibitors, metabolism)
• Humans
• Intracellular Membranes (metabolism)
• Lysosomes (metabolism)
• Permeability