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Design and structure of stapled peptides binding to estrogen receptors.

Phillips C, Roberts LR, Schade M, Bazin R, Bent A, Davies NL, Moore R, Pannifer AD, Pickford AR, Prior SH, Read CM, Scott A, Brown DG, Xu B, Irving SL
J Am Chem Soc 133 9696-9 (2011)
Related entries: 2lda, 2ldc, 2ldd, 2yja

Cited: 113 times
EuropePMC logo PMID: 21612236

Abstract

Synthetic peptides that specifically bind nuclear hormone receptors offer an alternative approach to small molecules for the modulation of receptor signaling and subsequent gene expression. Here we describe the design of a series of novel stapled peptides that bind the coactivator peptide site of estrogen receptors. Using a number of biophysical techniques, including crystal structure analysis of receptor-stapled peptide complexes, we describe in detail the molecular interactions and demonstrate that all-hydrocarbon staples modulate molecular recognition events. The findings have implications for the design of stapled peptides in general.

Reviews - 2yjd mentioned but not cited (2)

  1. Peptide-based inhibitors of protein-protein interactions: biophysical, structural and cellular consequences of introducing a constraint. Wang H, Dawber RS, Zhang P, Walko M, Wilson AJ, Wang X. Chem Sci 12 5977-5993 (2021)
  2. Stapled Peptides Inhibitors: A New Window for Target Drug Discovery. Ali AM, Atmaj J, Van Oosterwijk N, Groves MR, Dömling A. Comput Struct Biotechnol J 17 263-281 (2019)

Articles - 2yjd mentioned but not cited (1)

  1. In Silico and In Vitro Anticancer Activity of Isolated Novel Marker Compound from Chemically Modified Bioactive Fraction from Curcuma longa (NCCL). Naqvi A, Malasoni R, Gupta S, Srivastava A, Pandey RR, Dwivedi AK. Pharmacogn Mag 13 S640-S644 (2017)


Reviews citing this publication (27)

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Articles citing this publication (83)

  1. Stapled α-helical peptide drug development: a potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy. Chang YS, Graves B, Guerlavais V, Tovar C, Packman K, To KH, Olson KA, Kesavan K, Gangurde P, Mukherjee A, Baker T, Darlak K, Elkin C, Filipovic Z, Qureshi FZ, Cai H, Berry P, Feyfant E, Shi XE, Horstick J, Annis DA, Manning AM, Fotouhi N, Nash H, Vassilev LT, Sawyer TK. Proc. Natl. Acad. Sci. U.S.A. 110 E3445-54 (2013)
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  10. Rational optimization of conformational effects induced by hydrocarbon staples in peptides and their binding interfaces. Lama D, Quah ST, Verma CS, Lakshminarayanan R, Beuerman RW, Lane DP, Brown CJ. Sci Rep 3 3451 (2013)
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  12. Stapled Peptides with γ-Methylated Hydrocarbon Chains for the Estrogen Receptor/Coactivator Interaction. Speltz TE, Fanning SW, Mayne CG, Fowler C, Tajkhorshid E, Greene GL, Moore TW. Angew. Chem. Int. Ed. Engl. 55 4252-4255 (2016)
  13. Double Strain-Promoted Macrocyclization for the Rapid Selection of Cell-Active Stapled Peptides. Lau YH, Wu Y, Rossmann M, Tan BX, de Andrade P, Tan YS, Verma C, McKenzie GJ, Venkitaraman AR, Hyvönen M, Spring DR. Angew. Chem. Int. Ed. Engl. 54 15410-15413 (2015)
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  17. At a supra-physiological concentration, human sexual hormones act as quorum-sensing inhibitors. Beury-Cirou A, Tannières M, Minard C, Soulère L, Rasamiravaka T, Dodd RH, Queneau Y, Dessaux Y, Guillou C, Vandeputte OM, Faure D. PLoS ONE 8 e83564 (2013)
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  20. Stapled BH3 peptides against MCL-1: mechanism and design using atomistic simulations. Joseph TL, Lane DP, Verma CS. PLoS ONE 7 e43985 (2012)
  21. Monosubstituted alkenyl amino acids for peptide "stapling". Yeo DJ, Warriner SL, Wilson AJ. Chem. Commun. (Camb.) 49 9131-9133 (2013)
  22. Letter Benzene Probes in Molecular Dynamics Simulations Reveal Novel Binding Sites for Ligand Design. Tan YS, Reeks J, Brown CJ, Thean D, Ferrer Gago FJ, Yuen TY, Goh ET, Lee XE, Jennings CE, Joseph TL, Lakshminarayanan R, Lane DP, Noble ME, Verma CS. J Phys Chem Lett 7 3452-3457 (2016)
  23. Design of a Short Thermally Stable α-Helix Embedded in a Macrocycle. Wu H, Acharyya A, Wu Y, Liu L, Jo H, Gai F, DeGrado WF. Chembiochem 19 902-906 (2018)
  24. Oxime side-chain cross-links in an α-helical coiled-coil protein: structure, thermodynamics, and folding-templated synthesis of bicyclic species. Haney CM, Horne WS. Chemistry 19 11342-11351 (2013)
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  26. A new i, i + 3 peptide stapling system for α-helix stabilization. Shim SY, Kim YW, Verdine GL. Chem Biol Drug Des 82 635-642 (2013)
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  29. Truncated and constrained helical analogs of antimicrobial esculentin-2EM. Pham TK, Kim DH, Lee BJ, Kim YW. Bioorg. Med. Chem. Lett. 23 6717-6720 (2013)
  30. Aerobic iron-based cross-dehydrogenative coupling enables efficient diversity-oriented synthesis of coumestrol-based selective estrogen receptor modulators. Kshirsagar UA, Parnes R, Goldshtein H, Ofir R, Zarivach R, Pappo D. Chemistry 19 13575-13583 (2013)
  31. Crosslinked Aspartic Acids as Helix-Nucleating Templates. Zhao H, Liu QS, Geng H, Tian Y, Cheng M, Jiang YH, Xie MS, Niu XG, Jiang F, Zhang YO, Lao YZ, Wu YD, Xu NH, Li ZG. Angew. Chem. Int. Ed. Engl. 55 12088-12093 (2016)
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  33. Iterative optimization yields Mcl-1-targeting stapled peptides with selective cytotoxicity to Mcl-1-dependent cancer cells. Rezaei Araghi R, Bird GH, Ryan JA, Jenson JM, Godes M, Pritz JR, Grant RA, Letai A, Walensky LD, Keating AE. Proc. Natl. Acad. Sci. U.S.A. 115 E886-E895 (2018)
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  35. Stapling of unprotected helical peptides via photo-induced intramolecular thiol-yne hydrothiolation. Tian Y, Li J, Zhao H, Zeng X, Wang D, Liu Q, Niu X, Huang X, Xu N, Li Z. Chem Sci 7 3325-3330 (2016)
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  39. Unexpected involvement of staple leads to redesign of selective bicyclic peptide inhibitor of Grb7. Gunzburg MJ, Kulkarni K, Watson GM, Ambaye ND, Del Borgo MP, Brandt R, Pero SC, Perlmutter P, Wilce MC, Wilce JA. Sci Rep 6 27060 (2016)
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  45. A New Methodology for Incorporating Chiral Linkers into Stapled Peptides. Serrano JC, Sipthorp J, Xu W, Itzhaki LS, Ley SV. Chembiochem 18 1066-1071 (2017)
  46. Antimicrobial activity of doubly-stapled alanine/lysine-based peptides. Dinh TT, Kim DH, Luong HX, Lee BJ, Kim YW. Bioorg. Med. Chem. Lett. 25 4016-4019 (2015)
  47. Design of ultrahigh-affinity and dual-specificity peptide antagonists of MDM2 and MDMX for P53 activation and tumor suppression. Li X, Gohain N, Chen S, Li Y, Zhao X, Li B, Tolbert WD, He W, Pazgier M, Hu H, Lu W. Acta Pharm Sin B 11 2655-2669 (2021)
  48. How does a hydrocarbon staple affect peptide hydrophobicity? Sim AY, Verma C. J Comput Chem 36 773-784 (2015)
  49. Small molecule probes to target the human Mediator complex. Phillips AJ, Taatjes DJ. Isr. J. Chem. 53 588-595 (2013)
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  51. Chiral Sulfoxide-Induced Single Turn Peptide α-Helicity. Zhang Q, Jiang F, Zhao B, Lin H, Tian Y, Xie M, Bai G, Gilbert AM, Goetz GH, Liras S, Mathiowetz AA, Price DA, Song K, Tu M, Wu Y, Wang T, Flanagan ME, Wu YD, Li Z. Sci Rep 6 38573 (2016)
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  53. Molecular insights on xenoestrogenic potential of zearalenone-14-glucoside through a mixed in vitro/in silico approach. Dellafiora L, Ruotolo R, Perotti A, Cirlini M, Galaverna G, Cozzini P, Buschini A, Dall'Asta C. Food Chem. Toxicol. 108 257-266 (2017)
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  78. PROTAC Degrader of Estrogen Receptor α Targeting DNA-Binding Domain in Breast Cancer. Zhang X, Zhang Z, Xue X, Fan T, Tan C, Liu F, Tan Y, Jiang Y. ACS Pharmacol Transl Sci 5 1109-1118 (2022)
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