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Targeting TGFβ signaling to inhibit fibroblast activation as a therapy for fibrosis and cancer: effect of halofuginone

, PhD
Pages 11-20 | Published online: 19 Dec 2007

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Qiang Luo, Ziquan Hu, Hongcheng Zhao, Yanmei Fan, Xiancong Tu, Yueqing Wang & Xiaowen Liu. (2023) The role of TGF-β in the tumor microenvironment of pancreatic cancer. Genes & Diseases 10:4, pages 1513-1524.
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Ting Lv, Jianhua Huang, Minfeng Wu, Hongwei Wang, Qingyu Zeng & Xiuli Wang. (2022) Halofuginone enhances the anti-tumor effect of ALA-PDT by suppressing NRF2 signaling in cSCC. Photodiagnosis and Photodynamic Therapy 37, pages 102572.
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Jacqui Allen. (2021) Current approaches to management of vocal fold scar. Current Opinion in Otolaryngology & Head & Neck Surgery 29:6, pages 465-472.
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Pritesh P. Jain, Tengteng Zhao, Mingmei Xiong, Shanshan Song, Ning Lai, Qiuyu Zheng, Jiyuan Chen, Shane G. Carr, Aleksandra Babicheva, Amin Izadi, Marisela Rodriguez, Shamin Rahimi, Francesca Balistrieri, Shayan Rahimi, Tatum Simonson, Daniela Valdez‐Jasso, Patricia A. Thistlethwaite, John Y.‐J. Shyy, Jian Wang, Ayako Makino & Jason X.‐J. Yuan. (2021) Halofuginone, a promising drug for treatment of pulmonary hypertension. British Journal of Pharmacology 178:17, pages 3373-3394.
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Jacqueline Allen. (2021) Effects of corticosteroids vs halofuginone on vocal fold wound healing in an ovine model. Laryngoscope Investigative Otolaryngology 6:4, pages 786-793.
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Nuo Wang, Shi-ying Hou, Xin Qi, Mi Deng, Jia-min Cao, Bo-Ding Tong & Wei Xiong. (2021) LncRNA LPAL2/miR-1287-5p/EGFR Axis Modulates TED-Derived Orbital Fibroblast Activation Through Cell Adhesion Factors. The Journal of Clinical Endocrinology & Metabolism 106:8, pages e2866-e2886.
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Sharon Mordechay, Shaun Smullen, Paul Evans, Olga Genin, Mark Pines & Orna Halevy. (2021) Differential Effects of Halofuginone Enantiomers on Muscle Fibrosis and Histopathology in Duchenne Muscular Dystrophy. International Journal of Molecular Sciences 22:13, pages 7063.
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Wen-Jie Wu, Yu-Fang Tang, Shuang Dong & Jie Zhang. (2021) Ginsenoside Rb3 Alleviates the Toxic Effect of Cisplatin on the Kidney during Its Treatment to Oral Cancer via TGF-β-Mediated Mitochondrial Apoptosis. Evidence-Based Complementary and Alternative Medicine 2021, pages 1-11.
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Hila Barzilai-Tutsch, Olga Genin, Mark Pines & Orna Halevy. (2020) Early pathological signs in young dysf mice are improved by halofuginone. Neuromuscular Disorders 30:6, pages 472-482.
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Hila Barzilai-Tutsch, Melissa Dewulf, Christophe Lamaze, Gillian Butler Browne, Mark Pines & Orna Halevy. (2018) A promotive effect for halofuginone on membrane repair and synaptotagmin-7 levels in muscle cells of dysferlin-null mice. Human Molecular Genetics 27:16, pages 2817-2829.
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Shaun Smullen, Noel P. McLaughlin & Paul Evans. (2018) Chemical synthesis of febrifugine and analogues. Bioorganic & Medicinal Chemistry 26:9, pages 2199-2220.
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Linghui Luo, Yong Gao, Cao Yang, Zengwu Shao, Xinghuo Wu, Shuai Li, Liming Xiong & Chao Chen. (2018) Halofuginone attenuates intervertebral discs degeneration by suppressing collagen I production and inactivating TGFβ and NF-кB pathway. Biomedicine & Pharmacotherapy 101, pages 745-753.
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Wenbo Mu, Boyong Xu, Hairong Ma, Jiao Li, Baochao Ji, Zhendong Zhang, Abdusami Amat & Li Cao. (2018) Halofuginone Attenuates Osteoarthritis by Rescuing Bone Remodeling in Subchondral Bone Through Oral Gavage. Frontiers in Pharmacology 9.
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Patricia Juárez, Pierrick G.J. Fournier, Khalid S. Mohammad, Ryan C. McKenna, Holly W. Davis, Xiang H. Peng, Maria Niewolna, Alain Mauviel, John M. Chirgwin & Theresa A. Guise. (2017) Halofuginone inhibits TGF-β/BMP signaling and in combination with zoledronic acid enhances inhibition of breast cancer bone metastasis. Oncotarget 8:49, pages 86447-86462.
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Yin Luo, Xiaoyan Xie, Di Luo, Yuan Wang & Yijun Gao. (2017) The role of halofuginone in fibrosis: more to be explored?. Journal of Leukocyte Biology 102:6, pages 1333-1345.
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Berna Karakoyun. 2017. Liver Cirrhosis - Update and Current Challenges. Liver Cirrhosis - Update and Current Challenges.
Wenbo Mu, Boyong Xu, Hairong Ma, Baochao Ji, Zhendong Zhang, Jiao Li, Abdusami Amat & Li Cao. (2017) Halofuginone attenuates articular cartilage degeneration by inhibition of elevated TGF-β1 signaling in articular cartilage in a rodent osteoarthritis model. Molecular Medicine Reports 16:5, pages 7679-7684.
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Jacqueline Allen. (2016) Response of an ovine laryngeal injury model to a novel fibrosis inhibitor. ANZ Journal of Surgery 87:4, pages 266-270.
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Mark Pines, Oshrat Levi, Olga Genin, Adi Lavy, Corrado Angelini, Valérie Allamand & Orna Halevy. (2017) Elevated Expression of Moesin in Muscular Dystrophies. The American Journal of Pathology 187:3, pages 654-664.
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Yang Chen, Weishuai Liu, Peng Wang, Hailing Hou, Ningbo Liu, Linlin Gong, Youyou Wang, Kai Ji, Lujun Zhao & Ping Wang. (2016) Halofuginone inhibits radiotherapy-induced epithelial-mesenchymal transition in lung cancer. Oncotarget 7:44, pages 71341-71352.
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Hisashi Oishi, Tereza Martinu, Masaaki Sato, Yasushi Matsuda, Shin Hirayama, Stephen C. Juvet, Zehong Guan, Tomohito Saito, Marcelo Cypel, David M. Hwang, Tracy L. Keller, Malcolm R. Whitman, Mingyao Liu & Shaf Keshavjee. (2016) Halofuginone treatment reduces interleukin-17A and ameliorates features of chronic lung allograft dysfunction in a mouse orthotopic lung transplant model. The Journal of Heart and Lung Transplantation 35:4, pages 518-527.
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Hila Barzilai-Tutsch, Anna Bodanovsky, Hadar Maimon, Mark Pines & Orna Halevy. (2016) Halofuginone promotes satellite cell activation and survival in muscular dystrophies. Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease 1862:1, pages 1-11.
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Oshrat Levi, Olga Genin, Corrado Angelini, Orna Halevy & Mark Pines. (2015) Inhibition of muscle fibrosis results in increases in both utrophin levels and the number of revertant myofibers in Duchenne muscular dystrophy. Oncotarget 6:27, pages 23249-23260.
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Mark Pines & Itai Spector. (2015) Halofuginone — The Multifaceted Molecule. Molecules 20:1, pages 573-594.
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Anna Bodanovsky, Noga Guttman, Hila Barzilai-Tutsch, Ola Genin, Oshrat Levy, Mark Pines & Orna Halevy. (2014) Halofuginone improves muscle-cell survival in muscular dystrophies. Biochimica et Biophysica Acta (BBA) - Molecular Cell Research 1843:7, pages 1339-1347.
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Noel P. McLaughlin, Paul Evans & Mark Pines. (2014) The chemistry and biology of febrifugine and halofuginone. Bioorganic & Medicinal Chemistry 22:7, pages 1993-2004.
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Mark Pines. (2014) Halofuginone for fibrosis, regeneration and cancer in the gastrointestinal tract. World Journal of Gastroenterology 20:40, pages 14778.
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Itai Spector, Yael Zilberstein, Adi Lavy, Olga Genin, Hila Barzilai-Tutsch, Ana Bodanovsky, Orna Halevy & Mark Pines. (2013) The Involvement of Collagen Triple Helix Repeat Containing 1 in Muscular Dystrophies. The American Journal of Pathology 182:3, pages 905-916.
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Kelly E. Murphy, Scott W. McCue & D.L. Sean McElwain. (2012) Clinical strategies for the alleviation of contractures from a predictive mathematical model of dermal repair. Wound Repair and Regeneration 20:2, pages 194-202.
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Donatella Pietrella, Anna Rachini, Mark Pines, Neelam Pandey, Paolo Mosci, Francesco Bistoni, Cristophe d'Enfert & Anna Vecchiarelli. (2011) Th17 Cells and IL-17 in Protective Immunity to Vaginal Candidiasis. PLoS ONE 6:7, pages e22770.
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Itai Spector, Hen Honig, Norifumi Kawada, Arnon Nagler, Olga Genin & Mark Pines. (2010) Inhibition of Pancreatic Stellate Cell Activation by Halofuginone Prevents Pancreatic Xenograft Tumor Development. Pancreas 39:7, pages 1008-1015.
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Yoram Nevo, Orna Halevy, Olga Genin, Itai Moshe, Tidhar Turgeman, Michal Harel, Edva Biton, Shimon Reif & Mark Pines. (2010) Fibrosis inhibition and muscle histopathology improvement in laminin‐α2‐deficient mice. Muscle & Nerve 42:2, pages 218-229.
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John A. Cook, Rajani Choudhuri, William DeGraff, Janet Gamson & James B. Mitchell. (2010) Halofuginone enhances the radiation sensitivity of human tumor cell lines. Cancer Letters 289:1, pages 119-126.
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Olga Genin, Gideon Rechavi, Arnon Nagler, Ofer Ben-Itzhak, Kellie J. Nazemi & Mark Pines. (2008) Myofibroblasts in Pulmonary and Brain Metastases of Alveolar Soft-Part Sarcoma: A Novel Target for Treatment?. Neoplasia 10:9, pages 940-948.
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