Targeting T-type channels in cancer: What is on and what is off?

Drug Discov Today. 2022 Mar;27(3):743-758. doi: 10.1016/j.drudis.2021.11.021. Epub 2021 Nov 24.

Abstract

Over the past 20 years, various studies have demonstrated a pivotal role of T-type calcium channels (TTCCs) in tumor progression. Cytotoxic effects of TTCC pharmacological blockers have been reported in vitro and in preclinical models. However, their roles in cancer physiology are only beginning to be understood. In this review, we discuss evidence for the signaling pathways and cellular processes stemming from TTCC activity, mainly inferred by inverse reasoning from pharmacological blocks and, only in a few studies, by gene silencing or channel activation. A thorough analysis indicates that drug-induced cytotoxicity is partially an off-target effect. Dissection of on/off-target activity is paramount to elucidate the physiological roles of TTCCs, and to deliver efficacious therapies suited to different cancer types and stages.

Keywords: Apoptosis; Autophagy; Ca(2+) signaling; Cancer cells; Chemotherapy; On/off-target effects; Pharmacological blockers; Repurposing; T-type Ca(2+) channels.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Calcium Channel Blockers / pharmacology
  • Calcium Channels, T-Type* / genetics
  • Calcium Channels, T-Type* / metabolism
  • Humans
  • Neoplasms* / drug therapy
  • Neoplasms* / metabolism
  • Signal Transduction

Substances

  • Antineoplastic Agents
  • Calcium Channel Blockers
  • Calcium Channels, T-Type