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Article Abstract

We report on the design and synthesis of triptycene-peptide hybrids (TPHs), , -, and -, which are conjugates of a triptycene core unit with two or three cationic KKKGG peptides (K: lysine and G: glycine) through a C alkyl chain. It was discovered that - and - induce paraptosis, a type of programmed cell death (PCD), in Jurkat cells (leukemia T-lymphocytes). Mechanistic studies indicate that these TPHs induce the transfer of Ca from the endoplasmic reticulum (ER) to mitochondria, a loss of mitochondrial membrane potential (ΔΨ), tethering of the ER and mitochondria, and cytoplasmic vacuolization in the paraptosis processes.

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http://dx.doi.org/10.1021/acs.bioconjchem.2c00076DOI Listing

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