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Structural basis for vitamin D receptor agonism by novel non-secosteroidal ligands.

Asano L, Ito I, Kuwabara N, Waku T, Yanagisawa J, Miyachi H, Shimizu T
FEBS Lett 587 957-63 (2013)
Related entries: 3w0h, 3w0i, 3w0j

Cited: 12 times
EuropePMC logo PMID: 23462137

Abstract

Non-secosteroidal ligands for vitamin D receptor (VDR) have been developed for the agonist with non-calcemic profiles. Here, we provide the structural mechanism of VDR agonism by novel non-secosteroidal ligands. All ligands had the similar efficacy, while two had the higher potency. Crystallographic analyses revealed that all ligands interacted with helix H10 and the loop between helices H6 and H7 in a similar manner, but also that the two ligands with higher potency had different interaction modes. This study suggests that distinct ligand potency depend upon differences in the formation and rearrangement of hydrogen-bond networks induced by each ligand.

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  1. A multidisciplinary approach disclosing unexplored Aflatoxin B1 roles in severe impairment of vitamin D mechanisms of action. Persico M, Sessa R, Cesaro E, Dini I, Costanzo P, Ritieni A, Fattorusso C, Grosso M. Cell Biol Toxicol 39 1275-1295 (2023)


Reviews citing this publication (6)

  1. Vitamin D and Its Synthetic Analogs. Maestro MA, Molnár F, Carlberg C. J Med Chem 62 6854-6875 (2019)
  2. Vitamin D receptor agonists' anti-inflammatory properties. Vojinovic J. Ann N Y Acad Sci 1317 47-56 (2014)
  3. Structural considerations of vitamin D signaling. Molnár F. Front Physiol 5 191 (2014)
  4. Structure-activity relationship of nonsecosteroidal vitamin D receptor modulators. Yamada S, Makishima M. Trends Pharmacol Sci 35 324-337 (2014)
  5. Structural Biology-Based Exploration of Subtype-Selective Agonists for Peroxisome Proliferator-Activated Receptors. Miyachi H. Int J Mol Sci 22 9223 (2021)
  6. Structural Biology Inspired Development of a Series of Human Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Ligands: From Agonist to Antagonist. Miyachi H. Int J Mol Sci 24 3940 (2023)

Articles citing this publication (5)

  1. The application of the open pharmacological concepts triple store (open PHACTS) to support drug discovery research. Ratnam J, Zdrazil B, Digles D, Cuadrado-Rodriguez E, Neefs JM, Tipney H, Siebes R, Waagmeester A, Bradley G, Chau CH, Richter L, Brea J, Evelo CT, Jacoby E, Senger S, Loza MI, Ecker GF, Chichester C. PLoS One 9 e115460 (2014)
  2. Structural development of stapled short helical peptides as vitamin D receptor (VDR)-coactivator interaction inhibitors. Misawa T, Demizu Y, Kawamura M, Yamagata N, Kurihara M. Bioorg Med Chem 23 1055-1061 (2015)
  3. Development of stapled short helical peptides capable of inhibiting vitamin D receptor (VDR)-coactivator interactions. Demizu Y, Nagoya S, Shirakawa M, Kawamura M, Yamagata N, Sato Y, Doi M, Kurihara M. Bioorg Med Chem Lett 23 4292-4296 (2013)
  4. The Binding Mode Prediction and Similar Ligand Potency in the Active Site of Vitamin D Receptor with QM/MM Interaction, MESP, and MD Simulation. Selvaraman N, Selvam SK, Muthusamy K. Chem Biol Drug Des 88 272-280 (2016)
  5. Effect of Calcitriol and Vitamin D Receptor Modulator 2 on Recovery of Injured Skeletal Muscle in Wistar Rats. Stratos I, Schleese S, Rinas I, Vollmar B, Mittlmeier T. Biomedicines 11 2477 (2023)


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