PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia Cells

Histone deacetylase inhibitors (HDACi) have become a promising new avenue for cancer therapy, and many are currently in Phase I/II clinical trials for various tumor types. In the present study, we show that apoptosis induction and histone alterations by PCI-24781, a novel hydroxamic acid-based HDAC...

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Main Authors: Nilsa Rivera-Del Valle, Shan Gao, Claudia P. Miller, Joy Fulbright, Carolina Gonzales, Mint Sirisawad, Susanne Steggerda, Jennifer Wheler, Sriram Balasubramanian, Joya Chandra
Format: Article
Language:English
Published: Wiley 2010-01-01
Series:International Journal of Cell Biology
Online Access:http://dx.doi.org/10.1155/2010/207420
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author Nilsa Rivera-Del Valle
Shan Gao
Claudia P. Miller
Joy Fulbright
Carolina Gonzales
Mint Sirisawad
Susanne Steggerda
Jennifer Wheler
Sriram Balasubramanian
Joya Chandra
author_facet Nilsa Rivera-Del Valle
Shan Gao
Claudia P. Miller
Joy Fulbright
Carolina Gonzales
Mint Sirisawad
Susanne Steggerda
Jennifer Wheler
Sriram Balasubramanian
Joya Chandra
author_sort Nilsa Rivera-Del Valle
collection DOAJ
description Histone deacetylase inhibitors (HDACi) have become a promising new avenue for cancer therapy, and many are currently in Phase I/II clinical trials for various tumor types. In the present study, we show that apoptosis induction and histone alterations by PCI-24781, a novel hydroxamic acid-based HDAC inhibitor, require caspase-8 and the adaptor molecule, Fas-associated death domain (FADD), in acute leukemia cells. PCI-24781 treatment also causes an increase in superoxide levels, which has been reported for other HDACi. However, an antioxidant does not reverse histone alterations caused by PCI-24781, indicating that ROS generation is likely downstream of the effects that PCI-24781 exerts on histone H3. Taken together, these results provide insight into the mechanism of apoptosis induction by PCI-24781 in leukemia by highlighting the roles of caspase-8, FADD and increased superoxide levels.
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language English
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publisher Wiley
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series International Journal of Cell Biology
spelling doaj-art-684e885e38f248eaadb4ac4276f1250e2025-08-20T02:06:40ZengWileyInternational Journal of Cell Biology1687-88761687-88842010-01-01201010.1155/2010/207420207420PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia CellsNilsa Rivera-Del Valle0Shan Gao1Claudia P. Miller2Joy Fulbright3Carolina Gonzales4Mint Sirisawad5Susanne Steggerda6Jennifer Wheler7Sriram Balasubramanian8Joya Chandra9Department of Pediatrics Research, Children's Cancer Hospital, The University of Texas M. D. Anderson Cancer Center, Houston, TX 77030, USADepartment of Pediatrics Research, Children's Cancer Hospital, The University of Texas M. D. Anderson Cancer Center, Houston, TX 77030, USADepartment of Pediatrics Research, Children's Cancer Hospital, The University of Texas M. D. Anderson Cancer Center, Houston, TX 77030, USADepartment of Pediatrics Research, Children's Cancer Hospital, The University of Texas M. D. Anderson Cancer Center, Houston, TX 77030, USADepartment of Pediatrics Research, Children's Cancer Hospital, The University of Texas M. D. Anderson Cancer Center, Houston, TX 77030, USAPharmacyclics Inc., Sunnyvale, CA 94085, USAPharmacyclics Inc., Sunnyvale, CA 94085, USADepartment of Investigational Therapeutics, The University of Texas M. D. Anderson Children's Cancer Hospital, Houston, TX 77030, USAPharmacyclics Inc., Sunnyvale, CA 94085, USADepartment of Pediatrics Research, Children's Cancer Hospital, The University of Texas M. D. Anderson Cancer Center, Houston, TX 77030, USAHistone deacetylase inhibitors (HDACi) have become a promising new avenue for cancer therapy, and many are currently in Phase I/II clinical trials for various tumor types. In the present study, we show that apoptosis induction and histone alterations by PCI-24781, a novel hydroxamic acid-based HDAC inhibitor, require caspase-8 and the adaptor molecule, Fas-associated death domain (FADD), in acute leukemia cells. PCI-24781 treatment also causes an increase in superoxide levels, which has been reported for other HDACi. However, an antioxidant does not reverse histone alterations caused by PCI-24781, indicating that ROS generation is likely downstream of the effects that PCI-24781 exerts on histone H3. Taken together, these results provide insight into the mechanism of apoptosis induction by PCI-24781 in leukemia by highlighting the roles of caspase-8, FADD and increased superoxide levels.http://dx.doi.org/10.1155/2010/207420
spellingShingle Nilsa Rivera-Del Valle
Shan Gao
Claudia P. Miller
Joy Fulbright
Carolina Gonzales
Mint Sirisawad
Susanne Steggerda
Jennifer Wheler
Sriram Balasubramanian
Joya Chandra
PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia Cells
International Journal of Cell Biology
title PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia Cells
title_full PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia Cells
title_fullStr PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia Cells
title_full_unstemmed PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia Cells
title_short PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia Cells
title_sort pci 24781 a novel hydroxamic acid hdac inhibitor exerts cytotoxicity and histone alterations via caspase 8 and fadd in leukemia cells
url http://dx.doi.org/10.1155/2010/207420
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