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Drug Discovery Case History

Discovery and development of exenatide: the first antidiabetic agent to leverage the multiple benefits of the incretin hormone, GLP-1

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Pages 219-244 | Published online: 12 Dec 2012

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David J. Craik & Meng-Wei Kan. (2021) How can we improve peptide drug discovery? Learning from the past. Expert Opinion on Drug Discovery 16:12, pages 1399-1402.
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Hongchao Pan, Yunnan Su, Yini Xie, Weiyong Wang, Wanli Qiu, Wei Chen, Wenying Lu, Zhao Lu, Weiwei Wang & Anquan Shang. (2020) Everestmab, a novel long-acting GLP-1/anti GLP-1R nanobody fusion protein, exerts potent anti-diabetic effects. Artificial Cells, Nanomedicine, and Biotechnology 48:1, pages 854-866.
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Khyati Girdhar, Budheswar Dehury, Mahender Kumar Singh, Vineeth P. Daniel, Abhinav Choubey, Surbhi Dogra, Sunil Kumar & Prosenjit Mondal. (2019) Novel insights into the dynamics behavior of glucagon-like peptide-1 receptor with its small molecule agonists. Journal of Biomolecular Structure and Dynamics 37:15, pages 3976-3986.
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Meng-Wong Taing, Felicity J Rose & Jonathan P Whitehead. (2014) GLP-1(28-36)amide, the Glucagon-like peptide-1 metabolite: friend, foe, or pharmacological folly?. Drug Design, Development and Therapy 8, pages 677-688.
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Doaa A. Zaky, Dalaal M. Abdallah & Hanan S. El-Abhar. (2023) Intranasal Exendin-4 modifies necroptosis-mediated innate immune response to combat septic encephalopathy in rats: Role of mTORC1 in immunogenic and tolerogenic cell demise. European Journal of Pharmacology 961, pages 176191.
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Niraj Kumar Singh, Ashini Singh, Mini Varshney & Ritik Agrawal. (2023) A Research Update on Exendin-4 as a Novel Molecule Against Parkinson’s Disease. Current Molecular Medicine 23:9, pages 889-900.
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J. Michael Conlon, Finbarr P.M. O’Harte & Peter R. Flatt. (2022) Dual-agonist incretin peptides from fish with potential for obesity-related Type 2 diabetes therapy – A review. Peptides 147, pages 170706.
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Anna Roberts, Phyllis Phuah, Sijing Cheng & Kevin G. Murphy. 2022. Comprehensive Pharmacology. Comprehensive Pharmacology 344 372 .
Guilherme Rabelo Coelho, Daiane Laise da Silva, Emidio Beraldo-Neto, Hugo Vigerelli, Laudiceia Alves de Oliveira, Juliana Mozer Sciani & Daniel Carvalho Pimenta. (2021) Neglected Venomous Animals and Toxins: Underrated Biotechnological Tools in Drug Development. Toxins 13:12, pages 851.
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Luba Yammine, Charles E Green, Thomas R Kosten, Constanza de Dios, Robert Suchting, Scott D Lane, Christopher D Verrico & Joy M Schmitz. (2021) Exenatide Adjunct to Nicotine Patch Facilitates Smoking Cessation and May Reduce Post-Cessation Weight Gain: A Pilot Randomized Controlled Trial. Nicotine & Tobacco Research 23:10, pages 1682-1690.
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Helen C. Mendel, Quentin Kaas & Markus Muttenthaler. (2020) Neuropeptide signalling systems – An underexplored target for venom drug discovery. Biochemical Pharmacology 181, pages 114129.
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Albert Y. Hung & Michael A. Schwarzschild. (2020) Approaches to Disease Modification for Parkinson’s Disease: Clinical Trials and Lessons Learned. Neurotherapeutics 17:4, pages 1393-1405.
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E.L. Schneider, R. Reid, D.G. Parkes, T.A. Lutz, G.W. Ashley & D.V. Santi. (2020) A once-monthly GLP-1 receptor agonist for treatment of diabetic cats. Domestic Animal Endocrinology 70, pages 106373.
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Mohamed E.I. Badawy. 2020. Bioactive Natural Products. Bioactive Natural Products 321 364 .
Xinwang Yang, Ying Wang, Chunyun Wu & Eng-Ang Ling. (2019) Animal Venom Peptides as a Treasure Trove for New Therapeutics Against Neurodegenerative Disorders. Current Medicinal Chemistry 26:25, pages 4749-4774.
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Thomas GuttusoJr.Jr., Kelly L. Andrzejewski, David G. Lichter & Julie K. Andersen. (2019) Targeting kinases in Parkinson's disease: A mechanism shared by LRRK2, neurotrophins, exenatide, urate, nilotinib and lithium. Journal of the Neurological Sciences 402, pages 121-130.
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A.R. Pinho, A. Fortuna, A. Falcão, A.C. Santos, R. Seiça, C. Estevens, F. Veiga & A.J. Ribeiro. (2019) Comparison of ELISA and HPLC-MS methods for the determination of exenatide in biological and biotechnology-based formulation matrices. Journal of Pharmaceutical Analysis 9:3, pages 143-155.
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Yilin Tang, Ke Yang, Jue Zhao, Xiaoniu Liang & Jian Wang. (2019) Evidence of Repurposing Drugs and Identifying Contraindications from Real World Study in Parkinson’s Disease. ACS Chemical Neuroscience 10:2, pages 954-963.
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Enrico Bagnoli & Una FitzGerald. (2019) Mitral cells and the glucagon‐like peptide 1 receptor: The sweet smell of success?. European Journal of Neuroscience 49:4, pages 422-439.
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Daoqi Tang, Hong Tian, Jicheng Wu, Jiaxiao Cheng, Cheng Luo, Wenbo Sai, Xiaoda Song, Xiangdong Gao & Wenbing Yao. (2018) C-terminal site-specific PEGylated Exendin-4 analog: A long-acting glucagon like Peptide-1 receptor agonist, on glycemic control and beta cell function in diabetic db/db mice. Journal of Pharmacological Sciences 138:1, pages 23-30.
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Dilan Athauda & Thomas Foltynie. (2018) Drug Repurposing in Parkinson’s Disease. CNS Drugs 32:8, pages 747-761.
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Dilan Athauda & Thomas Foltynie. (2018) Protective effects of the GLP-1 mimetic exendin-4 in Parkinson's disease. Neuropharmacology 136, pages 260-270.
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Dilan Athauda, Kate MaclaganNatalia Budnik, Luca Zampedri, Steve HibbertSimon S. Skene, Kashfia ChowdhuryIciar Aviles-Olmos, Patricia Limousin & Thomas Foltynie. (2018) What Effects Might Exenatide have on Non-Motor Symptoms in Parkinson’s Disease: A Post Hoc Analysis. Journal of Parkinson's Disease 8:2, pages 247-258.
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Patrick J. Knerr, Brian Finan, Vasily Gelfanov, Diego Perez-Tilve, Matthias H. Tschöp & Richard D. DiMarchi. (2018) Optimization of peptide-based polyagonists for treatment of diabetes and obesity. Bioorganic & Medicinal Chemistry 26:10, pages 2873-2881.
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J. Michael Conlon, Milena Mechkarska, Yasser H. Abdel-Wahab & Peter R. Flatt. (2018) Peptides from frog skin with potential for development into agents for Type 2 diabetes therapy. Peptides 100, pages 275-281.
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Luba Yammine, Thomas R. Kosten, Paul M. Cinciripini, Charles E. Green, Janet C. Meininger, Jennifer A. Minnix & Thomas F. Newton. (2018) Exenatide once weekly for smoking cessation. Medicine 97:2, pages e9567.
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Ariadna Lobo-Ruiz & Judit Tulla-Puche. 2018. Peptide Applications in Biomedicine, Biotechnology and Bioengineering. Peptide Applications in Biomedicine, Biotechnology and Bioengineering 23 49 .
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