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Plasminogen activator inhibitor-1 inhibitors: a patent review (2006 – present)

, PhD
Pages 801-815 | Published online: 25 Mar 2013

Keep up to date with the latest research on this topic with citation updates for this article.

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Aly A Yousef, Faisal Y Mohamed, Naglaa F Boraey, Nagwa E Akeel, Attia A Soliman, Nevin M Waked, Mustafa I A Hashem, Hassan Shehata, Dalia S Fahmy, Ali Ismael, Lamya M Ibrahim, Mohamed A M Ibrahim, Hanan F Salem, Sherif M Yousry, Sherif F Osman, Rania A Fouad, Eman T Enan, Mohammed A Attia, Mona R Afify, Nancy M S Zeidan & Mohamed Nashat. (2020) Association of Plasminogen Activator Inhibitor 1 (PAI-1) 4G/5G Polymorphism and Susceptibility to SLE in Egyptian Children and Adolescents: A Multicenter Study. Journal of Inflammation Research 13, pages 1103-1111.
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B. U. Anaya-Macias, U. De la Cruz-Mosso, C. A. Palafox-Sánchez, I. Parra-Rojas, G. Martínez-Bonilla, L. González-López, J. I. Gámez-Nava, E. E. Pérez-Guerrero, S. L. Barrientos-Avalos & J. F. Muñoz-Valle. (2020) The −675 4G/5G PAI-1 polymorphism confers genetic susceptibility to systemic lupus erythematosus, its clinical manifestations, and comorbidities in Mexican-Mestizo population. Autoimmunity 53:2, pages 71-77.
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Lingqin Li, Fan Li, Zhehao Xu, Liyang Li, Haiyi Hu, Yang Li, Shicheng Yu, Mingchao Wang & Lei Gao. (2023) Identification and validation of SERPINE1 as a prognostic and immunological biomarker in pan-cancer and in ccRCC. Frontiers in Pharmacology 14.
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Yongzhuo Yu, Wenxuan Li, Lili Xu & Yangang Wang. (2023) Circadian rhythm of plasminogen activator inhibitor-1 and cardiovascular complications in type 2 diabetes. Frontiers in Endocrinology 14.
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Anheng Wang, Leigh A. Madden & Vesselin N. Paunov. (2022) Fabrication of Angiogenic Sprouting Coculture of Cell Clusteroids Using an Aqueous Two-Phase Pickering Emulsion System. ACS Applied Bio Materials 5:4, pages 1804-1816.
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Thanaa Abdulmahdi Mokif, Zena Abdul-Ameer Mahdi, Raheem Tuama Obayes Al- Mammori, Hussein Oleiwi Muttaleb Al-Dahmoshi & Noor Salman Kadhim Al-Khafaji. (2022) Correlation of Vitamin D3, PAI-1, and HCG Hormone in Pre- and Post-Menopausal in Babylon Province. Reports of Biochemistry and Molecular Biology 11:1, pages 36-43.
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Chong Xu, Xia Liu, Jie Shen, Quan Sun, Xiaohong Guo, Min Yang & Jing Leng. (2021) Integrative identification of human serpin PAI‐1 inhibitors from Dracaena dragon blood and molecular implications for inhibitor‐induced PAI‐1 allosterism . Biotechnology and Applied Biochemistry 69:1, pages 221-229.
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H.M.C. Kumara, Addison Poppy, Dasuni Gamage, Erica Pettke, Abhinit Shah, Xiaohong Yan, Vesna Cekic & Richard Whelan. (2021) Sustained postoperative plasma elevations of plasminogen activator inhibitor‑1 following minimally invasive colorectal cancer resection. Molecular and Clinical Oncology 16:2.
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Noppadol Kietsiriroje, Robert A.S. Ariëns & Ramzi A. Ajjan. (2021) Fibrinolysis in Acute and Chronic Cardiovascular Disease. Seminars in Thrombosis and Hemostasis 47:05, pages 490-505.
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Thembaninkosi G. Gaule & Ramzi A. Ajjan. (2021) Fibrin(ogen) as a Therapeutic Target: Opportunities and Challenges. International Journal of Molecular Sciences 22:13, pages 6916.
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Rawan Altalhi, Nikoletta Pechlivani & Ramzi A. Ajjan. (2021) PAI-1 in Diabetes: Pathophysiology and Role as a Therapeutic Target. International Journal of Molecular Sciences 22:6, pages 3170.
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Machteld Sillen & Paul J. Declerck. (2021) A Narrative Review on Plasminogen Activator Inhibitor-1 and Its (Patho)Physiological Role: To Target or Not to Target?. International Journal of Molecular Sciences 22:5, pages 2721.
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Machteld Sillen, Toshio Miyata, Douglas E. Vaughan, Sergei V. Strelkov & Paul J. Declerck. (2021) Structural Insight into the Two-Step Mechanism of PAI-1 Inhibition by Small Molecule TM5484. International Journal of Molecular Sciences 22:3, pages 1482.
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Elsa P. Bianchini, Claire Auditeau, Mahita Razanakolona, Marc Vasse & Delphine Borgel. (2021) Serpins in Hemostasis as Therapeutic Targets for Bleeding or Thrombotic Disorders. Frontiers in Cardiovascular Medicine 7.
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Machteld Sillen & Paul J. Declerck. (2020) Targeting PAI-1 in Cardiovascular Disease: Structural Insights Into PAI-1 Functionality and Inhibition. Frontiers in Cardiovascular Medicine 7.
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Machteld Sillen, Stephen D. Weeks, Sergei V. Strelkov & Paul J. Declerck. (2020) Structural Insights into the Mechanism of a Nanobody That Stabilizes PAI-1 and Modulates Its Activity. International Journal of Molecular Sciences 21:16, pages 5859.
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Machteld Sillen, Stephen D. Weeks, Xiaohua Zhou, Andrey A. Komissarov, Galina Florova, Steven Idell, Sergei V. Strelkov & Paul J. Declerck. (2020) Molecular mechanism of two nanobodies that inhibit PAI‐1 activity reveals a modulation at distinct stages of the PAI‐1/plasminogen activator interaction. Journal of Thrombosis and Haemostasis 18:3, pages 681-692.
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Katherine A. Vousden, Tomas Lundqvist, Bojana Popovic, Brian Naiman, Alan M. Carruthers, Philip Newton, Daniel J. D. Johnson, Anja Pomowski, Trevor Wilkinson, Patrick Dufner, Isabelle de Mendez, Philip R. Mallinder, Clare Murray, Martin Strain, Jane Connor, Lynne A. Murray, Matthew A. Sleeman, David C. Lowe, James A. Huntington & Tristan J. Vaughan. (2019) Discovery and characterisation of an antibody that selectively modulates the inhibitory activity of plasminogen activator inhibitor-1. Scientific Reports 9:1.
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Sunhye Shin, Mi Kyoung Kim, Woong Jung & Youhoon Chong. (2018) (−)-Epigallocatechin gallate derivatives reduce the expression of both urokinase plasminogen activator and plasminogen activator inhibitor-1 to inhibit migration, adhesion, and invasion of MDA-MB-231 cells. Phytotherapy Research 32:10, pages 2086-2096.
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Richard G. Jung, Trevor Simard, Alisha Labinaz, F. Daniel Ramirez, Pietro Di Santo, Pouya Motazedian, Rebecca Rochman, Chantal Gaudet, Mohammad Ali Faraz, Rob S.B. Beanlands & Benjamin Hibbert. (2018) Role of plasminogen activator inhibitor-1 in coronary pathophysiology. Thrombosis Research 164, pages 54-62.
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Flavio Dormont, Mariana Varna & Patrick Couvreur. (2018) Nanoplumbers: biomaterials to fight cardiovascular diseases. Materials Today 21:2, pages 122-143.
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Deniz Agirbasli & Mehmet Agirbasli. 2018. Encyclopedia of Signaling Molecules. Encyclopedia of Signaling Molecules 4055 4063 .
Katherine Kearney, Darren Tomlinson, Kerrie Smith & Ramzi Ajjan. (2017) Hypofibrinolysis in diabetes: a therapeutic target for the reduction of cardiovascular risk. Cardiovascular Diabetology 16:1.
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M. Luo, Y. Ji, Y. Luo, R. Li, W.P. Fay & J. Wu. (2017) Plasminogen activator inhibitor‐1 regulates the vascular expression of vitronectin. Journal of Thrombosis and Haemostasis 15:12, pages 2451-2460.
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Erika Nakatsuka, Kenjiro Sawada, Koji Nakamura, Akihito Yoshimura, Yasuto Kinose, Michiko Kodama, Kae Hashimoto, Seiji Mabuchi, Hiroshi Makino, Eiichi Morii, Yoichi Yamaguchi, Takeshi Yanase, Akiko Itai, Ken-ichirou Morishige & Tadashi Kimura. (2017) Plasminogen activator inhibitor-1 is an independent prognostic factor of ovarian cancer and IMD-4482, a novel plasminogen activator inhibitor-1 inhibitor, inhibits ovarian cancer peritoneal dissemination. Oncotarget 8:52, pages 89887-89902.
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Mehmet Agirbasli, Fatih Göktay, Irem Peker, Pembegul Gunes, Fugen Vardar Aker & Mustafa Akkiprik. (2017) Enhanced mRNA expression of plasminogen activator inhibitor-1 in livedoid vasculopathy lesions. Cardiovascular Therapeutics 35:3, pages e12255.
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Kexin Sun, Jing Song, Kuo Liu, Kai Fang, Ling Wang, Xueyin Wang, Jing Li, Xun Tang, Yiqun Wu, Xueying Qin, Tao Wu, Pei Gao, Dafang Chen & Yonghua Hu. (2016) Associations between homocysteine metabolism related SNPs and carotid intima-media thickness: a Chinese sib pair study. Journal of Thrombosis and Thrombolysis 43:3, pages 401-410.
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Deniz Agirbasli & Mehmet Agirbasli. 2017. Encyclopedia of Signaling Molecules. Encyclopedia of Signaling Molecules 1 9 .
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Yan JiZhen WengPhilip FishNeha GoyalMao LuoSamantha P. MyearsTammy L. StrawnBysani ChandrasekarJianbo WuWilliam P. Fay. (2016) Pharmacological Targeting of Plasminogen Activator Inhibitor-1 Decreases Vascular Smooth Muscle Cell Migration and Neointima Formation. Arteriosclerosis, Thrombosis, and Vascular Biology 36:11, pages 2167-2175.
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Kevin Dietrich, Geoff D. C. Ball & Lesley G. Mitchell. (2016) Increased plasminogen activator inhibitor results in a hypofibrinolytic state in adolescents with obesity: in vivo and ex vivo evidence . British Journal of Haematology 175:2, pages 300-307.
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Miguel Angel Pavón, Irene Arroyo-Solera, Maria Virtudes Céspedes, Isolda Casanova, Xavier León & Ramón Mangues. (2016) uPA/uPAR and SERPINE1 in head and neck cancer: role in tumor resistance, metastasis, prognosis and therapy. Oncotarget 7:35, pages 57351-57366.
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Tihami Qureshi, Sumit Goswami, Carlee S. McClintock, Matthew T. Ramsey & Cynthia B. Peterson. (2016) Distinct encounter complexes of PAI-1 with plasminogen activators and vitronectin revealed by changes in the conformation and dynamics of the reactive center loop. Protein Science 25:2, pages 499-510.
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Tihami Qureshi & Cynthia B. Peterson. (2016) Single fluorescence probes along the reactive center loop reveal site-specific changes during the latency transition of PAI-1. Protein Science 25:2, pages 487-498.
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Amparo Estepa & Julio Coll. (2015) Inhibition of SERPINe1 reduces rhabdoviral infections in zebrafish. Fish & Shellfish Immunology 47:1, pages 264-270.
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Veronica R. Placencio & Yves A. DeClerck. (2015) Plasminogen Activator Inhibitor-1 in Cancer: Rationale and Insight for Future Therapeutic Testing. Cancer Research 75:15, pages 2969-2974.
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Veronica R. Placencio, Atsuhiko Ichimura, Toshio Miyata & Yves A. DeClerck. (2015) Small Molecule Inhibitors of Plasminogen Activator Inhibitor-1 Elicit Anti-Tumorigenic and Anti-Angiogenic Activity. PLOS ONE 10:7, pages e0133786.
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MARZENA WYGANOWSKA-ŞWIĄTKOWSKA & JERZY JANKUN. (2015) Plasminogen activation system in oral cancer: Relevance in prognosis and therapy (Review). International Journal of Oncology 47:1, pages 16-24.
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Stephany C. Barreto, Christina A. Hopkins, Meghnad Bhowmick & Amitabha Ray. (2015) Extracellular matrix in obesity – cancer interactions. Hormone Molecular Biology and Clinical Investigation 22:2, pages 63-77.
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Anne Rouch, Corinne Vanucci-Bacqué, Florence Bedos-Belval & Michel Baltas. (2015) Small molecules inhibitors of plasminogen activator inhibitor-1 – An overview. European Journal of Medicinal Chemistry 92, pages 619-636.
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Tine Wyseure & Paul J. Declerck. (2014) Novel or expanding current targets in fibrinolysis. Drug Discovery Today 19:9, pages 1476-1482.
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Jared DamareStephanie BrandalYolanda M. Fortenberry. (2014) Inhibition of PAI-1 Antiproteolytic Activity Against tPA by RNA Aptamers. Nucleic Acid Therapeutics 24:4, pages 239-249.
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Yanqiong Zhang, Rongtian Wang, Shangzhu Li, Xiangying Kong, Zhiyao Wang, Weiheng Chen & Na Lin. (2013) Genetic polymorphisms in plasminogen activator inhibitor-1 predict susceptibility to steroid-induced osteonecrosis of the femoral head in Chinese population. Diagnostic Pathology 8:1.
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