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Ligand binding and conformational changes of SUR1 subunit in pancreatic ATP-sensitive potassium channels.

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Wu JX, Ding D, Wang M, Kang Y, Zeng X, Chen L
OpenAccess logo Protein Cell 9 553-567 (2018)
Related entries: 5yke, 5ykg, 5yw7, 5yw8, 5yw9, 5ywa, 5ywb, 5ywc, 5ywd

Cited: 49 times
EuropePMC logo PMID: 29594720

Abstract

ATP-sensitive potassium channels (KATP) are energy sensors on the plasma membrane. By sensing the intracellular ADP/ATP ratio of β-cells, pancreatic KATP channels control insulin release and regulate metabolism at the whole body level. They are implicated in many metabolic disorders and diseases and are therefore important drug targets. Here, we present three structures of pancreatic KATP channels solved by cryo-electron microscopy (cryo-EM), at resolutions ranging from 4.1 to 4.5 Å. These structures depict the binding site of the antidiabetic drug glibenclamide, indicate how Kir6.2 (inward-rectifying potassium channel 6.2) N-terminus participates in the coupling between the peripheral SUR1 (sulfonylurea receptor 1) subunit and the central Kir6.2 channel, reveal the binding mode of activating nucleotides, and suggest the mechanism of how Mg-ADP binding on nucleotide binding domains (NBDs) drives a conformational change of the SUR1 subunit.

Reviews - 5ykf mentioned but not cited (3)

  1. Structural and functional diversity calls for a new classification of ABC transporters. Thomas C, Aller SG, Beis K, Carpenter EP, Chang G, Chen L, Dassa E, Dean M, Duong Van Hoa F, Ekiert D, Ford R, Gaudet R, Gong X, Holland IB, Huang Y, Kahne DK, Kato H, Koronakis V, Koth CM, Lee Y, Lewinson O, Lill R, Martinoia E, Murakami S, Pinkett HW, Poolman B, Rosenbaum D, Sarkadi B, Schmitt L, Schneider E, Shi Y, Shyng SL, Slotboom DJ, Tajkhorshid E, Tieleman DP, Ueda K, Váradi A, Wen PC, Yan N, Zhang P, Zheng H, Zimmer J, Tampé R. FEBS Lett 594 3767-3775 (2020)
  2. The role of the degenerate nucleotide binding site in type I ABC exporters. Stockner T, Gradisch R, Schmitt L. FEBS Lett 594 3815-3838 (2020)
  3. Mechanistic insights on KATP channel regulation from cryo-EM structures. Driggers CM, Shyng SL. J Gen Physiol 155 e202113046 (2023)

Articles - 5ykf mentioned but not cited (6)



Reviews citing this publication (12)

  1. New insights into KATP channel gene mutations and neonatal diabetes mellitus. Pipatpolkai T, Usher S, Stansfeld PJ, Ashcroft FM. Nat Rev Endocrinol 16 378-393 (2020)
  2. Ion Channels of the Islets in Type 2 Diabetes. Jacobson DA, Shyng SL. J Mol Biol 432 1326-1346 (2020)
  3. Targeting receptor complexes: a new dimension in drug discovery. Rosenbaum MI, Clemmensen LS, Bredt DS, Bettler B, Strømgaard K. Nat Rev Drug Discov 19 884-901 (2020)
  4. Kir Channel Molecular Physiology, Pharmacology, and Therapeutic Implications. Cui M, Cantwell L, Zorn A, Logothetis DE. Handb Exp Pharmacol 267 277-356 (2021)
  5. Multidrug Resistance in Mammals and Fungi-From MDR to PDR: A Rocky Road from Atomic Structures to Transport Mechanisms. Khunweeraphong N, Kuchler K. Int J Mol Sci 22 4806 (2021)
  6. Pharmacological chaperones of ATP-sensitive potassium channels: Mechanistic insight from cryoEM structures. Martin GM, Sung MW, Shyng SL. Mol Cell Endocrinol 502 110667 (2020)
  7. Membrane transporters in drug development and as determinants of precision medicine. Galetin A, Brouwer KLR, Tweedie D, Yoshida K, Sjöstedt N, Aleksunes L, Chu X, Evers R, Hafey MJ, Lai Y, Matsson P, Riselli A, Shen H, Sparreboom A, Varma MVS, Yang J, Yang X, Yee SW, Zamek-Gliszczynski MJ, Zhang L, Giacomini KM. Nat Rev Drug Discov 23 255-280 (2024)
  8. Kir6.1 and SUR2B in Cantú syndrome. McClenaghan C, Nichols CG. Am J Physiol Cell Physiol 323 C920-C935 (2022)
  9. Personalized Therapeutics for KATP-Dependent Pathologies. Nichols CG. Annu Rev Pharmacol Toxicol 63 541-563 (2023)
  10. KATP channel mutations in congenital hyperinsulinism: Progress and challenges towards mechanism-based therapies. ElSheikh A, Shyng SL. Front Endocrinol (Lausanne) 14 1161117 (2023)
  11. KATP channels in focus: Progress toward a structural understanding of ligand regulation. Martin GM, Patton BL, Shyng SL. Curr Opin Struct Biol 79 102541 (2023)
  12. Dynamic duo: Kir6 and SUR in K<sub>ATP</sub> channel structure and function. Patton BL, Zhu P, ElSheikh A, Driggers CM, Shyng SL. Channels (Austin) 18 2327708 (2024)

Articles citing this publication (28)



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