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In vitro inhibition of AKR1Cs by sulphonylureas and the structural basis.

Zhao Y, Zheng X, Zhang H, Zhai J, Zhang L, Li C, Zeng K, Chen Y, Li Q, Hu X
Chem Biol Interact 240 310-5 (2015)
Related entries: 4yvp, 4yvx, 4zfc

Cited: 12 times
EuropePMC logo PMID: 26362498

Abstract

Recent epidemiological studies show conflicting data for the first-line anti-diabetic sulphonylureas drugs in treating cancer progression in type II diabetes patients. How sulphonylureas promote or diminish tumor growth is not fully understood. Here, we report that seven sulphonylureas exhibit different in vitro inhibition towards AKR1Cs (AKR1C1, AKR1C2, AKR1C3), which are critical steroid hormone metabolism enzymes that are related to prostate cancer, breast cancer and endometrial diseases. Interactions of the sulphonylureas and AKR1Cs were analyzed by X-ray crystallography.

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Reviews citing this publication (1)

  1. Aldo-Keto Reductase AKR1C1-AKR1C4: Functions, Regulation, and Intervention for Anti-cancer Therapy. Zeng CM, Chang LL, Ying MD, Cao J, He QJ, Zhu H, Yang B. Front Pharmacol 8 119 (2017)

Articles citing this publication (9)

  1. Ligand binding and conformational changes of SUR1 subunit in pancreatic ATP-sensitive potassium channels. Wu JX, Ding D, Wang M, Kang Y, Zeng X, Chen L. Protein Cell 9 553-567 (2018)
  2. Liquiritin, as a Natural Inhibitor of AKR1C1, Could Interfere With the Progesterone Metabolism. Zeng C, Zhu D, You J, Dong X, Yang B, Zhu H, He Q. Front Physiol 10 833 (2019)
  3. Prognostic significance of diabetes mellitus and dyslipidemia in men receiving androgen-deprivation therapy for metastatic prostate cancer. Hirata Y, Shiota M, Kobayashi T, Kashiwagi E, Takeuchi A, Inokuchi J, Tatsugami K, Eto M. Prostate Int 7 166-170 (2019)
  4. Transcript Levels of Aldo-Keto Reductase Family 1 Subfamily C (AKR1C) Are Increased in Prostate Tissue of Patients with Type 2 Diabetes. Franko A, Berti L, Hennenlotter J, Rausch S, Scharpf MO, de Angelis MH, Stenzl A, Birkenfeld AL, Peter A, Lutz SZ, Häring HU, Heni M. J Pers Med 10 E124 (2020)
  5. Aldo-ketoreductase 1c19 ablation does not affect insulin secretion in murine islets. Miyachi Y, Kuo T, Son J, Accili D. PLoS One 16 e0260526 (2021)
  6. Computational modeling studies reveal the origin of the binding preference of 3-(3,4-di hydroisoquinolin-2(1H)-ylsulfonyl)benzoic acids for AKR1C3 over its isoforms. Kong X, Xing E, Wu S, Zhuang T, Li PK, Li C, Cheng X. Protein Sci 31 e4499 (2022)
  7. Design and development of novel inhibitors of aldo-ketoreductase 1C1 as potential lead molecules in treatment of breast cancer. Verma P, Hassan MI, Singh A, Singh IK. Mol Cell Biochem 476 2975-2987 (2021)
  8. Phytochemical profile, comparative evaluation of Satureja montana alcoholic extract for antioxidants, anti-inflammatory and molecular docking studies. Abdelshafeek KA, Osman AF, Mouneir SM, Elhenawy AA, Abdallah WE. BMC Complement Med Ther 23 108 (2023)
  9. Synthesis, molecular structure and urease inhibitory activity of novel bis-Schiff bases of benzyl phenyl ketone: A combined theoretical and experimental approach. Ahmad R, Khan M, Alam A, Elhenawy AA, Qadeer A, AlAsmari AF, Alharbi M, Alasmari F, Ahmad M. Saudi Pharm J 31 101688 (2023)


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