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A patent review of glucokinase activators and disruptors of the glucokinase – glucokinase regulatory protein interaction: 2011 – 2014

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Sachin Sharma, Karan Wadhwa, Manjusha Choudhary & Vikas Budhwar. (2022) Ethnopharmacological perspectives of glucokinase activators in the treatment of diabetes mellitus. Natural Product Research 36:11, pages 2962-2976.
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Tereso J. Guzmán & Carmen M. Gurrola-Díaz. (2021) Glucokinase activation as antidiabetic therapy: effect of nutraceuticals and phytochemicals on glucokinase gene expression and enzymatic activity. Archives of Physiology and Biochemistry 127:2, pages 182-193.
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André J. Scheen. (2016) Investigational insulin secretagogues for type 2 diabetes. Expert Opinion on Investigational Drugs 25:4, pages 405-422.
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Oluremi N. Ajala, David M. Huffman & Ibrahim I. Ghobrial. (2016) Glucokinase mutation–a rare cause of recurrent hypoglycemia in adults: a case report and literature review. Journal of Community Hospital Internal Medicine Perspectives 6:5.
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Loranne Agius. (2014) Lessons from glucokinase activators: the problem of declining efficacy. Expert Opinion on Therapeutic Patents 24:11, pages 1155-1159.
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Articles from other publishers (22)

Adil Iqbal Qazi, Bashir Ahmad, Muhammad Umar Khayam Sahibzada, Fareeha Anwar, Ameer Khusro, Fahad A. Alhumaydhi, Amany Abdel-Rahman Mohamed, Gomaa Mostafa-Hedeab & Talha Bin Emran. (2023) Evaluation of Antidiabetic Activity of Oxadiazole Derivative in Rats. Evidence-Based Complementary and Alternative Medicine 2023, pages 1-15.
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Siddharth Yadav, Samuel Bharti & Puniti Mathur. (2023) GlucoKinaseDB: A comprehensive, curated resource of glucokinase modulators for clinical and molecular research. Computational Biology and Chemistry 103, pages 107818.
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Ying Du, Leili Gao, Xinhua Xiao, Xin Hou & Linong Ji. (2022) A multicentre, randomized, double‐blind, parallel, active‐ and placebo‐controlled Phase 3 clinical study of the glucokinase activator PB ‐201 in treatment‐naive patients with type 2 diabetes mellitus: A study protocol . Diabetes, Obesity and Metabolism 25:3, pages 649-655.
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Prateek Sharma, Sukhbir Singh, Neelam Sharma, Deepak Singla, Kumar Guarve & Ajmer Singh Grewal. (2022) Targeting human Glucokinase for the treatment of type 2 diabetes: an overview of allosteric Glucokinase activators. Journal of Diabetes & Metabolic Disorders 21:1, pages 1129-1137.
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Sarbani Pal & Manojit Pal. 2021. Drug Discovery and Drug Development. Drug Discovery and Drug Development 179 212 .
Brian E. Ford, Shruti S. Chachra, Ahmed Alshawi, Alfie Brennan, Suzannah Harnor, Celine Cano, David J. Baker, David M. Smith, Rebecca J. Fairclough & Loranne Agius. (2020) Chronic glucokinase activator treatment activates liver Carbohydrate response element binding protein and improves hepatocyte ATP homeostasis during substrate challenge . Diabetes, Obesity and Metabolism 22:11, pages 1985-1994.
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Ping Wu, Zhenyu Liu, Xiaohong Jiang & Hao Fang. (2020) An Overview of Prospective Drugs for Type 1 and Type 2 Diabetes. Current Drug Targets 21:5, pages 445-457.
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Konstantinos A. Toulis, Krishnarajah Nirantharakumar, Chrysa Pourzitaki, Anthony H. Barnett & Abd A. Tahrani. (2020) Glucokinase Activators for Type 2 Diabetes: Challenges and Future Developments. Drugs 80:5, pages 467-475.
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Ronald J. Hinklin, Brian R. Baer, Steven A. Boyd, Mark D. Chicarelli, Kevin R. Condroski, Walter E. DeWolfJr.Jr., John Fischer, Michele Frank, Gary P. Hingorani, Patrice A. Lee, Nickolas A. Neitzel, Scott A. Pratt, Ajay Singh, Francis X. Sullivan, Timothy Turner, Walter C. Voegtli, Eli M. Wallace, Lance Williams & Thomas D. Aicher. (2020) Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic & Medicinal Chemistry 28:1, pages 115232.
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Ling Song, Yi Zhang, Ji Jiang, Shuang Ren, Li Chen, Dongyang Liu, Xijing Chen & Pei Hu. (2018) Development of a Physiologically Based Pharmacokinetic Model for Sinogliatin, a First-in-Class Glucokinase Activator, by Integrating Allometric Scaling, In Vitro to In Vivo Exploration and Steady-State Concentration–Mean Residence Time Methods: Mechanistic Understanding of its Pharmacokinetics. Clinical Pharmacokinetics 57:10, pages 1307-1323.
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Zhengyu Wang, Xiaofan Shi, Huan Zhang, Liang Yu, Yanhua Cheng, Hefeng Zhang, Huibin Zhang, Jinpei Zhou, Jing Chen, Xu Shen & Wenhu Duan. (2017) Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. European Journal of Medicinal Chemistry 139, pages 128-152.
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Ziad H. Al-Oanzi, Sophia Fountana, Tabassum Moonira, Susan J. Tudhope, John L. Petrie, Ahmed Alshawi, Gillian Patman, Catherine Arden, Helen L. Reeves & Loranne Agius. (2017) Opposite effects of a glucokinase activator and metformin on glucose-regulated gene expression in hepatocytes. Diabetes, Obesity and Metabolism 19:8, pages 1078-1087.
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Edmond Differding. (2017) The Drug Discovery and Development Industry in India-Two Decades of Proprietary Small-Molecule R&D. ChemMedChem 12:11, pages 786-818.
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Anil M. Deshpande, Debnath Bhuniya, Siddhartha De, Bhavesh Dave, Vinod P. Vyavahare, Santosh H. Kurhade, Sachin R. Kandalkar, Keshav P. Naik, Balasaheb S. Kobal, Rahul D. Kaduskar, Sujay Basu, Vaibhav Jain, Pratima Patil, Sandhya Chaturvedi Joshi, Ganesh Bhat, Amol A. Raje, Satyanarayana Reddy, Jayasagar Gundu, Vamsi Madgula, Suhas Tambe, Prasad Shitole, Dhananjay Umrani, Anita Chugh, Venkata P. Palle & Kasim A. Mookhtiar. (2017) Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. European Journal of Medicinal Chemistry 133, pages 268-286.
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Jiayi Xu, Songnian Lin, Robert W. Myers, Maria E. Trujillo, Michele J. Pachanski, Sunita Malkani, Hsuan-shen Chen, Zhesheng Chen, Brian Campbell, George J. Eiermann, Nadine Elowe, Brian T. Farrer, Wen Feng, Qinghong Fu, Roman Kats-Kagan, Michael Kavana, Daniel R. McMasters, Kaushik Mitra, Xinchun Tong, Libo Xu, Fengqi Zhang, Rui Zhang, George H. Addona, Joel P. Berger, Bei Zhang & Emma R. Parmee. (2017) Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus. Bioorganic & Medicinal Chemistry Letters 27:9, pages 2063-2068.
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Jiayi Xu, Songnian Lin, Robert W. Myers, George Addona, Joel P. Berger, Brian Campbell, Hsuan-shen Chen, Zhesheng Chen, George J. Eiermann, Nadine H. Elowe, Brian T. Farrer, Wen Feng, Qinghong Fu, Roman Kats-Kagan, Michael Kavana, Sunita Malkani, Daniel R. McMasters, Kaushik Mitra, Michele J. Pachanski, Xinchun Tong, Maria E. Trujillo, Libo Xu, Bei Zhang, Fengqi Zhang, Rui Zhang & Emma R. Parmee. (2017) Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic & Medicinal Chemistry Letters 27:9, pages 2069-2073.
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Hao He, Wan-Guo Yu, Jun-peng Yang, Sheng Ge & Yan-Hua Lu. (2015) Multiple Comparisons of Glucokinase Activation Mechanisms of Five Mulberry Bioactive Ingredients in Hepatocyte. Journal of Agricultural and Food Chemistry 64:12, pages 2475-2484.
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Lewis D. Pennington, Michael D. Bartberger, Michael D. Croghan, Kristin L. Andrews, Kate S. Ashton, Matthew P. Bourbeau, Jie Chen, Samer Chmait, Rod Cupples, Christopher Fotsch, Joan Helmering, Fang-Tsao Hong, Randall W. Hungate, Steven R. Jordan, Ke Kong, Longbin Liu, Klaus Michelsen, Carolyn Moyer, Nobuko Nishimura, Mark H. Norman, Andreas Reichelt, Aaron C. Siegmund, Glenn Sivits, Seifu Tadesse, Christopher M. Tegley, Gwyneth Van, Kevin C. Yang, Guomin Yao, Jiandong Zhang, David J. Lloyd, Clarence Hale & David J. St. JeanJr.Jr.. (2015) Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (n N → σ* S–X ) Interaction for Conformational Constraint . Journal of Medicinal Chemistry 58:24, pages 9663-9679.
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P. M. Rubtsov, E. L. Igudin & A. N. Tiulpakov. (2015) Glucokinase and glucokinase regulatory proteins as molecular targets for novel antidiabetic drugs. Molecular Biology 49:4, pages 494-499.
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Kaapjoo Park, Byoung Moon Lee, Kwan Hoon Hyun, Taedong Han, Dong Hoon Lee & Hyun Ho Choi. (2015) Design and Synthesis of Acetylenyl Benzamide Derivatives as Novel Glucokinase Activators for the Treatment of T2DM. ACS Medicinal Chemistry Letters 6:3, pages 296-301.
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Akinobu Nakamura & Yasuo Terauchi. (2014) Present status of clinical deployment of glucokinase activators. Journal of Diabetes Investigation 6:2, pages 124-132.
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Ronald J. Hinklin, Thomas D. Aicher, Deborah A. Anderson, Brian R. Baer, Steven A. Boyd, Kevin R. Condroski, Walter E. DeWolfJr.Jr., Christopher F. Kraser, Maralee McVean, Susan P. Rhodes, Hillary L. Sturgis, Walter C. Voegtli, Lance Williams & Jonathan B. Houze. (2014) Discovery of 2-Pyridylureas as Glucokinase Activators. Journal of Medicinal Chemistry 57:19, pages 8180-8186.
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