glycogen phosphorylase inhibitor

Using a focused screening approach, acyl ureas have been discovered as a new class of inhibitors of human liver glycogen phosphorylase (hlGPa). 2019 Jun 5;377(4):19. doi: 10.1007/s41061-019-0243-6. Glycogen phosphorylase inhibitors are considered as potential antidiabetic agents. Get the latest public health information from CDC: https://www.coronavirus.gov, Get the latest research information from NIH: https://www.nih.gov/coronavirus, Find NCBI SARS-CoV-2 literature, sequence, and clinical content: https://www.ncbi.nlm.nih.gov/sars-cov-2/. Inhibition of glycogen phosphorylase in the context of type 2 diabetes, with focus on recent inhibitors bound at the active site. With the rapid increase of type 2 diabetic patients recently, it is becoming an interesting field to discover GP inhibitor for potential antidiabetic drugs. Molecules. The cloning of the human liver glycogen phosphorylase (HLGP) revealed a new allosteric binding site near the subunit interface that is not present in the rabbit muscle glycogen phosphorylase (RMGP) normally used in studi… Epub 2013 Apr 30. Reduces blood glucose levels and increases hepatic glycogen content in C57/BL6J mice. Active Inhibitor 1 protein and direct phosphorylation by cAMP-dependent protein kinase keep protein phosphatase 1 in the inactive state so that is does not remove the activating phosphate group from glycogen phosphorylase. on the catalytic and structural properties of glycogen phosphorylase a has been studied. Somsák L, Nagya V, Hadady Z, Docsa T, Gergely P. Curr Pharm Des. 2020 Oct 30;10:592455. doi: 10.3389/fonc.2020.592455. 2020 Nov 22;25(22):5463. doi: 10.3390/molecules25225463. Glycogen phosphorylase (GP) catalyzes the hydrolysis of glycogen to generate glucose-1-phosphate and shortened glycogen molecule and is considered the rate limiting step in the degradation of glycogen. The knowledge of the three-dimensional structures of protein-ligand complexes allows analysis of how the ligands interact with the target and has the potential to facilitate structure-based drug design. Increasing doses (50–100 μ M) of the glycogen phosphorylase inhibitor CP-320626 inhibited [1,2-13C2]glucose stable isotope substrate re-distribution among glycolysis, pentose and … Glycogen phosphorylase inhibitor, 2,3-bis[(2E)-3-(4-hydroxyphenyl)prop-2-enamido] butanedioic acid (BF142), improves baseline insulin secretion of MIN6 insulinoma cells. Probing the catalytic site of rabbit muscle glycogen phosphorylase using a series of specifically modified maltohexaose derivatives. Introduction: Glycogen phosphorylase (GP) is the enzyme responsible for the synthesis of glucose-1-phosphate, the source of energy for muscles and the rest of the body. Design of potent GP inhibitors is a therapeutic strategy in the context of type 2 diabetes. NLM It is a part of the glucosyltransferase family and acts on the α-1,4-glycosidic linkage; the phosphorylase comes to a standstill 4 residues from an α-1,6-branchpoint, where debranching enzyme takes over . Advances in glycogen phosphorylase inhibitor design. 2020 Sep 22;15(9):e0236081. High Consistency of Structure-Based Design and X-Ray Crystallography: Design, Synthesis, Kinetic Evaluation and Crystallographic Binding Mode Determination of Biphenyl-. Glycogen phosphorylase is a dimer composed of two identical subunits, molecular weight 97,444 (842 amino acids), and an ... Glucose is an inhibitor that binds to the catalytic site and stabilizes the T state. This site needs JavaScript to work properly. Glycogen Phosphorylase Inhibitor | C17H15ClF2N4O4 | CID 10070301 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more. Glycogen metabolism has implications in beta cell function. Synonym: 1-(3-(3-(2-Chloro-4,5-difluorobenzoyl)ureido)-4-methoxyphenyl)-3-methylurea, Glycogen Phosphorylase Inhibitor - CAS 648926-15-2 - Calbiochem. This site needs JavaScript to work properly. Synthesis of New C- and N-β-d-Glucopyranosyl Derivatives of Imidazole, 1,2,3-Triazole and Tetrazole, and Their Evaluation as Inhibitors of Glycogen Phosphorylase. C-glycoside; Type 2 diabetes; carbohydrate; glycogen phosphorylase; inhibitor; steroids. Anomeric Spironucleosides of β-d-Glucopyranosyl Uracil as Potential Inhibitors of Glycogen Phosphorylase. Please enable it to take advantage of the complete set of features! The protein glycogen phosphorylase has been linked to type 2 diabetes, indicating the importance of this target to human health. Control of glycemia is crucial in the treatment of type 2 diabetes complications. The protein glycogen phosphorylase has been linked to type 2 diabetes, indicating the importance of this target to human health. Hence, the search for potent and selective inhibitors of this enzyme, which may lead to antihyperglycaemic drugs, has received particular attention. Glycogen phosphorylase inhibitor is a cell-permeable acyl urea first identified as an inhibitor of human liver glycogen phosphorylase (IC 50 = 53 nM). Curr Protein Pept Sci. 2000 Sep;7(9):677-82. doi: 10.1016/s1074-5521(00)00004-1. Glycogen phosphorylase (GP) catalyzes the breakdown of glycogen and largely contributes to hepatic glucose production making GP inhibition an attractive target to … While industry has slowed down on GP inhibitors design, academic groups are pursuing investigations and have provided potential drug candidates which will resuscitate the interest for GP, including its potential for targeting cancer. Top Curr Chem (Cham). 2016 Jan 27;108:444-454. doi: 10.1016/j.ejmech.2015.12.004. Introduction: 1.2 Diabetes Diabetes is the most common hormonal deficiency disease in the world. In this review, the synthesis, structure determination and computational studies of the most recent inhibitors of glycogen phosphorylase at the different binding sites are presented and analyzed. 2010 Oct;10(12):1156-74. doi: 10.2174/1389557511009011156. An inhibitor of human liver glycogen phosphorylase a (HLGPa) has been identified and characterized in vitro and in vivo. Goyard D, Kónya B, Chajistamatiou AS, Chrysina ED, Leroy J, Balzarin S, Tournier M, Tousch D, Petit P, Duret C, Maurel P, Somsák L, Docsa T, Gergely P, Praly JP, Azay-Milhau J, Vidal S. Eur J Med Chem. In vitro data are reported for GP inhibition but the in vivo biological data at the cellular or animal levels are often missing, even though the literature reported for these molecules is also discussed.  |  Expert opinion: 2020 Nov 22;25(22):5463. doi: 10.3390/molecules25225463. Crystallographic studies indicate, however, that selectivity between glycogen phosphorylase in skeletal muscle and liver is unlikely to be achieved. This review covers advances in the design of small molecule inhibitors of this enzyme, their biological activity, and their potential as effective antihyperglycemic agents for the treatment of Type 2 diabetes. Clipboard, Search History, and several other advanced features are temporarily unavailable. 2019 Apr 3;24(7):1322. doi: 10.3390/molecules24071322. 1. This substance, [R- (R*,S*)]-5-chloro- N - [3- (dimethylamino)-2-hydroxy-3-oxo-1- (phenylmethyl)propyl]-1H-indole-2-carboxamide (CP-91149), inhibited HLGPa with an IC 50 of 0.13 μM in the presence of 7.5 mM glucose. Synthesis, Kinetic and Conformational Studies of 2-Substituted-5-(β-d-glucopyranosyl)-pyrimidin-4-ones as Potential Inhibitors of Glycogen Phosphorylase.  |  Mini Rev Med Chem. Synthesis, Kinetic and Conformational Studies of 2-Substituted-5-(β-d-glucopyranosyl)-pyrimidin-4-ones as Potential Inhibitors of Glycogen Phosphorylase. Activation of glycogen phosphorylase and phosphorolysis of glycogen: The active form of glycogen phosphorylase kinase phosphorylates and activates glycogen phosphorylase. In the Search of Glycoside-Based Molecules as Antidiabetic Agents. NIH The X-ray structure of screening hit 1 (IC50 = 2 microM) in a complex with rabbit muscle glycogen phosphorylase b reveals that 1 binds at the AMP site, the main allosteric effector site of the dimeric enzyme. COVID-19 is an emerging, rapidly evolving situation. Computation as a tool for glycogen phosphorylase inhibitor design. Kun S, Bokor É, Sipos Á, Docsa T, Somsák L. Molecules. A glycogen phosphorylase inhibitor selectively enhances local rates of glucose utilization in brain during sensory stimulation of conscious rats: implications for glycogen turnover Gerald A. Dienel, Kelly K. Ball and Nancy F. Cruz Department of Neurology, University of Arkansas for Medical Sciences, Little Rock, Arkansas, USA Abstract HHS Another set of patents disclose cholic acid/7-aza-indole conjugates for targeted drug delivery to the liver. Revisiting Glycogen in Cancer: A Conspicuous and Targetable Enabler of Malignant Transformation. CP-91149 is a selective inhibitor of glycogen phosphorylase (GP) with an IC50 value of 0.13 μM. A structural analogy between glucose-based GP inhibitors and C-glucosides targeting sodium glucose co-transporter 2 (SGLT2) is intriguing. The present survey is focused on recent new molecules, potential inhibitors of the enzyme. 2, 3, 4 eCollection 2020. Get the latest public health information from CDC: https://www.coronavirus.gov, Get the latest research information from NIH: https://www.nih.gov/coronavirus, Find NCBI SARS-CoV-2 literature, sequence, and clinical content: https://www.ncbi.nlm.nih.gov/sars-cov-2/. Progress in our understanding of the mechanism of action of these inhibitors has been made by the determination of high-resolution enzyme inhibitor structures (both muscle and liver). Recent advances in the allosteric inhibition of glycogen phosphorylase. A glucopyranosyl urea compound that acts as an inhibitor of muscle glycogen phosphorylase (K i = 930 nM). The design of glycogen phosphorylase (GP) inhibitors targeting the catalytic site of the enzyme is a promising strategy for a better control of hyperglycaemia in the context of type 2 diabetes. Glycogen phosphorylase (GP) releases glucose from the liver into the blood stream. eCollection 2020.  |  Benzazepinones were very recently described and no associated literature is available, making it very difficult to comment at present. Pałasz A, Cież D, Trzewik B, Miszczak K, Tynor G, Bazan B. Glycogen phosphorylase …. 2010 Oct;10(12):1102-26. Inhibition of hepatic glycogen phosphorylase is a promising treatment strategy for attenuating hyperglycemia in type 2 diabetes. 2018 Mar 15;23(3):666. doi: 10.3390/molecules23030666. 2008 Apr;9(4):379-95. Cholic acid/7-aza-indole conjugates are promising in vivo drug delivery systems to the liver. CAS Number 648926-15-2. Glycogen phosphorylase as a molecular target for type 2 diabetes therapy. Since glucose production in the liver has been shown to increase in type 2 diabetes patients, inhibiting the release of glucose from the liver's glycogen's supplies appears to be a valid approach. Glycogen phosphorylase is a phosphorylase enzymes that can catalize phosphorolytic cleavage of the glycosidic linkages of glycogen by releasing glucose-1-phosphate from the terminal alpha-1, 4 … 2019 Jun 25;24(12):2327. doi: 10.3390/molecules24122327. 2003;9(15):1177-89. doi: 10.2174/1381612033454919. is an allosteric enzyme whose activity is primarily controlled by reversible phosphory-lation of Ser14 of the dephosphorylated enzyme ~GPb, less active, predominantly T-state! Glycogen phosphorylase inhibitor N-(3,5-dimethyl-Benzoyl)-N′-(β-D-glucopyranosyl)urea improves glucose tolerance under normoglycemic and diabetic conditions and rearranges hepatic metabolism. Nakamura M, Makino Y, Takagi C, Yamagaki T, Sato M. Glycoconj J. 2013 Aug;23(8):1017-32. doi: 10.1517/13543776.2013.794790. glycogen phosphorylase glycogen debranching enzyme phosphoglucomutase Glycogen phosphorylase (phosphorylase) - phosphorolysis of glucose residues at least 5 units from branch point Glycogen + Pi glycogen + glucose-1-phosphate (n residues) (n-1 residues) homodimer of 842-residues (92-kD) subunits allosteric regulation - inhibitors (ATP, glucose-6- Glycogen phosphorylase inhibitors: a patent review (2008 - 2012). Therefore, suppression of glucose output from the liver may be achieved by inhibition of glycogen phosphorylase. Front Oncol. Such inhibitors may be of use for therapy of the non-insulin dependent form of diabetes (NIDDM or Type II diabetes). Curr Opin Investig Drugs. Glycogen phosphorylase ~GP! Glycogen phosphorylase is a typical allosteric protein with five different ligand binding sites, thus offering multiple opportunities for modulation of enzyme activity. Nagy L, Béke F, Juhász L, Kovács T, Juhász-Tóth É, Docsa T, Tóth A, Gergely P, Somsák L, Bai P. PLoS One. Enhances glucose sensitivity in chow-fed, obese, diabetic mice and increasing hepatic glucose uptake. Epub 2017 Jun 8. Design of potent GP inhibitors is a therapeutic strategy in the context of type 2 diabetes. Epub 2020 Jan 10. There are two forms of glycogen phosphorylase, namely glycogen phosphorylase a and b forms. Hence, the search for potent and selective inhibitors of this enzyme, which may lead to antihyperglycaemic drugs, has received particular attention. 1 Glycogen phosphorylase inhibitor has been used to study glycogen utilization in human liver HepG2 cells, retinal explants, and human T lymphocyte Kit 225 cells. doi: 10.1371/journal.pone.0236081. potential inhibitors of glycogen phosphorylase, an enzyme implicated in type 2 diabetes. Areas covered: Glucose-based inhibitors have found potential applications since they now reach low nanomolar Ki values. Glucose-derived spiro-isoxazolines are anti-hyperglycemic agents against type 2 diabetes through glycogen phosphorylase inhibition. Rath VL, Ammirati M, Danley DE, Ekstrom JL, Gibbs EM, Hynes TR, Mathiowetz AM, McPherson RK, Olson TV, Treadway JL, Hoover DJ. The Glycogen Phosphorylase Inhibitor, also referenced under CAS 648926-15-2, controls the biological activity of Glycogen Phosphorylase. Advances in glycogen phosphorylase inhibitor design. Chem Biol. HHS Keywords: Glucose-based inhibitors have found potential applications since they now reach low nanomolar Ki values. Goyard D, Kónya B, Czifrák K, Larini P, Demontrond F, Leroy J, Balzarin S, Tournier M, Tousch D, Petit P, Duret C, Maurel P, Docsa T, Gergely P, Somsák L, Praly JP, Azay-Milhau J, Vidal S. Org Biomol Chem. Epub 2016 Feb 29. 2016;25(5):932-940. doi: 10.1007/s00044-016-1539-5. 2010 Oct;10(12):1139-55. doi: 10.2174/1389557511009011139. 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