Targeted Suppression of CEACAM6 via pHLIP-Delivered RNAs in Pancreatic Ductal Adenocarcinoma

<i>Background and Objectives</i>: Carcinoembryonic antigen-related cell adhesion molecule 6 (CEACAM6) is involved in pancreatic cancer progression and is an attractive therapeutic target for pancreatic cancer. In this study, we evaluated the therapeutic efficacy of small-interfering RNA...

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Main Authors: Hongsik Kim, Chang-Gok Woo, Seung-Myoung Son, Yong-Pyo Lee, Hee-Kyung Kim, Yaewon Yang, Jihyun Kwon, Ki-Hyeong Lee, Ho-Chang Lee, Ok-Jun Lee, Hye-Sook Han
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Language:English
Published: MDPI AG 2025-03-01
Series:Medicina
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Online Access:https://www.mdpi.com/1648-9144/61/4/598
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author Hongsik Kim
Chang-Gok Woo
Seung-Myoung Son
Yong-Pyo Lee
Hee-Kyung Kim
Yaewon Yang
Jihyun Kwon
Ki-Hyeong Lee
Ho-Chang Lee
Ok-Jun Lee
Hye-Sook Han
author_facet Hongsik Kim
Chang-Gok Woo
Seung-Myoung Son
Yong-Pyo Lee
Hee-Kyung Kim
Yaewon Yang
Jihyun Kwon
Ki-Hyeong Lee
Ho-Chang Lee
Ok-Jun Lee
Hye-Sook Han
author_sort Hongsik Kim
collection DOAJ
description <i>Background and Objectives</i>: Carcinoembryonic antigen-related cell adhesion molecule 6 (CEACAM6) is involved in pancreatic cancer progression and is an attractive therapeutic target for pancreatic cancer. In this study, we evaluated the therapeutic efficacy of small-interfering RNA (siRNA) targeting CEACAM6 (siCEACAM6) and the CEACAM6-suppressive microRNA-29a (miR-29a) in a pancreatic ductal adenocarcinoma xenograft mouse model using pH-low insertion peptide (pHLIP) technology, which targets the acidic tumor microenvironment. <i>Materials and Methods</i>: The delivery vectors for siRNA and miRNA were constructed by conjugating the peptide nucleic acid forms of siCEACAM6 and miR-29a to a peptide with a pHLIP, enabling the transport of siRNA and miRNA across the plasma membrane. The tumor-suppressive effects of pHLIP-siCEACAM6 and pHLIP-miR-29a were assessed in vivo using a BALB/c xenograft mouse model with the injection of the CFPAC-1 human pancreatic ductal adenocarcinoma cell line. <i>Results</i>: The treatment of CFPAC-1 cells with pHLIP-siCEACAM6 and pHLIP-miR-29a under acidic pH conditions suppressed CEACAM6 expression and decreased cell viability. In a xenograft mouse model, the intravenous injection of pHLIP-siCEACAM6 and pHLIP-miR-29a suppressed tumor growth by up to 25.1% (<i>p</i> < 0.01) and 21.2% (<i>p</i> < 0.01), respectively, compared to the control mice treated with pHLIP-scr. <i>Conclusions</i>: Our results demonstrated the efficacy of the pHLIP-mediated delivery of siCEACAM6 and miR-29a as a promising therapeutic strategy in a pancreatic ductal adenocarcinoma xenograft mouse model. The pHLIP technology, which targets the acidic tumor microenvironment, represents an innovative approach to the delivery of small RNAs to pancreatic ductal adenocarcinoma cells, providing new potential strategies for pancreatic cancer treatment.
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spelling doaj-art-e1bf7877b32d48e985fa6d09dc74092f2025-08-20T03:13:55ZengMDPI AGMedicina1010-660X1648-91442025-03-0161459810.3390/medicina61040598Targeted Suppression of CEACAM6 via pHLIP-Delivered RNAs in Pancreatic Ductal AdenocarcinomaHongsik Kim0Chang-Gok Woo1Seung-Myoung Son2Yong-Pyo Lee3Hee-Kyung Kim4Yaewon Yang5Jihyun Kwon6Ki-Hyeong Lee7Ho-Chang Lee8Ok-Jun Lee9Hye-Sook Han10Department of Internal Medicine, Chungbuk National University Hospital, College of Medicine, Chungbuk National University, Cheongju 28644, Republic of KoreaDepartment of Pathology, Chungbuk National University Hospital, College of Medicine, Chungbuk National University, Cheongju 28644, Republic of KoreaDepartment of Pathology, Chungbuk National University Hospital, College of Medicine, Chungbuk National University, Cheongju 28644, Republic of KoreaDepartment of Internal Medicine, Chungbuk National University Hospital, College of Medicine, Chungbuk National University, Cheongju 28644, Republic of KoreaDepartment of Internal Medicine, Chungbuk National University Hospital, College of Medicine, Chungbuk National University, Cheongju 28644, Republic of KoreaDepartment of Internal Medicine, Chungbuk National University Hospital, College of Medicine, Chungbuk National University, Cheongju 28644, Republic of KoreaDepartment of Internal Medicine, Chungbuk National University Hospital, College of Medicine, Chungbuk National University, Cheongju 28644, Republic of KoreaDepartment of Internal Medicine, Chungbuk National University Hospital, College of Medicine, Chungbuk National University, Cheongju 28644, Republic of KoreaDepartment of Pathology, Chungbuk National University Hospital, College of Medicine, Chungbuk National University, Cheongju 28644, Republic of KoreaDepartment of Pathology, Chungbuk National University Hospital, College of Medicine, Chungbuk National University, Cheongju 28644, Republic of KoreaDepartment of Internal Medicine, Chungbuk National University Hospital, College of Medicine, Chungbuk National University, Cheongju 28644, Republic of Korea<i>Background and Objectives</i>: Carcinoembryonic antigen-related cell adhesion molecule 6 (CEACAM6) is involved in pancreatic cancer progression and is an attractive therapeutic target for pancreatic cancer. In this study, we evaluated the therapeutic efficacy of small-interfering RNA (siRNA) targeting CEACAM6 (siCEACAM6) and the CEACAM6-suppressive microRNA-29a (miR-29a) in a pancreatic ductal adenocarcinoma xenograft mouse model using pH-low insertion peptide (pHLIP) technology, which targets the acidic tumor microenvironment. <i>Materials and Methods</i>: The delivery vectors for siRNA and miRNA were constructed by conjugating the peptide nucleic acid forms of siCEACAM6 and miR-29a to a peptide with a pHLIP, enabling the transport of siRNA and miRNA across the plasma membrane. The tumor-suppressive effects of pHLIP-siCEACAM6 and pHLIP-miR-29a were assessed in vivo using a BALB/c xenograft mouse model with the injection of the CFPAC-1 human pancreatic ductal adenocarcinoma cell line. <i>Results</i>: The treatment of CFPAC-1 cells with pHLIP-siCEACAM6 and pHLIP-miR-29a under acidic pH conditions suppressed CEACAM6 expression and decreased cell viability. In a xenograft mouse model, the intravenous injection of pHLIP-siCEACAM6 and pHLIP-miR-29a suppressed tumor growth by up to 25.1% (<i>p</i> < 0.01) and 21.2% (<i>p</i> < 0.01), respectively, compared to the control mice treated with pHLIP-scr. <i>Conclusions</i>: Our results demonstrated the efficacy of the pHLIP-mediated delivery of siCEACAM6 and miR-29a as a promising therapeutic strategy in a pancreatic ductal adenocarcinoma xenograft mouse model. The pHLIP technology, which targets the acidic tumor microenvironment, represents an innovative approach to the delivery of small RNAs to pancreatic ductal adenocarcinoma cells, providing new potential strategies for pancreatic cancer treatment.https://www.mdpi.com/1648-9144/61/4/598pancreatic ductal adenocarcinomapHLIPCEACAM6drug deliverytumor acidity
spellingShingle Hongsik Kim
Chang-Gok Woo
Seung-Myoung Son
Yong-Pyo Lee
Hee-Kyung Kim
Yaewon Yang
Jihyun Kwon
Ki-Hyeong Lee
Ho-Chang Lee
Ok-Jun Lee
Hye-Sook Han
Targeted Suppression of CEACAM6 via pHLIP-Delivered RNAs in Pancreatic Ductal Adenocarcinoma
Medicina
pancreatic ductal adenocarcinoma
pHLIP
CEACAM6
drug delivery
tumor acidity
title Targeted Suppression of CEACAM6 via pHLIP-Delivered RNAs in Pancreatic Ductal Adenocarcinoma
title_full Targeted Suppression of CEACAM6 via pHLIP-Delivered RNAs in Pancreatic Ductal Adenocarcinoma
title_fullStr Targeted Suppression of CEACAM6 via pHLIP-Delivered RNAs in Pancreatic Ductal Adenocarcinoma
title_full_unstemmed Targeted Suppression of CEACAM6 via pHLIP-Delivered RNAs in Pancreatic Ductal Adenocarcinoma
title_short Targeted Suppression of CEACAM6 via pHLIP-Delivered RNAs in Pancreatic Ductal Adenocarcinoma
title_sort targeted suppression of ceacam6 via phlip delivered rnas in pancreatic ductal adenocarcinoma
topic pancreatic ductal adenocarcinoma
pHLIP
CEACAM6
drug delivery
tumor acidity
url https://www.mdpi.com/1648-9144/61/4/598
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