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Review
. 2020 Jun;25(5-6):305-320.
doi: 10.1007/s10495-020-01601-9.

BCL-2 family deregulation in colorectal cancer: potential for BH3 mimetics in therapy

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Review

BCL-2 family deregulation in colorectal cancer: potential for BH3 mimetics in therapy

Prashanthi Ramesh et al. Apoptosis. 2020 Jun.

Abstract

Apoptosis is a form of programmed cell death that is essential for tissue homeostasis. De-regulation of the balance between proliferation and apoptosis contributes to tumor initiation. Particularly in the colon where apoptosis is a crucial process in intestinal turnover, inhibition of apoptosis facilitates transformation and tumor progression. The BCL-2 family of proteins are key regulators of apoptosis and have been implicated in colorectal cancer (CRC) initiation, progression and resistance to therapy. In this review we outline the current knowledge on the BCL-2 family-regulated intrinsic apoptosis pathway and mechanisms by which it is de-regulated in CRC. We further review BH3 mimetics as a therapeutic opportunity to target this pathway and evaluate their potential for CRC treatment.

Keywords: Apoptosis; BCL-2 family; BH3 mimetics; Colorectal cancer.

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Figures

Fig. 1
Fig. 1
BCL-2 family protein interactions regulate mitochondrial outer membrane permeabilization (MOMP)
Fig. 2
Fig. 2
BH3-only proteins have specific affinities for anti-apoptotic proteins
Fig. 3
Fig. 3
An overview of selective BH3 mimetics designed to inhibit anti-apoptotic proteins

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