4uyd › Citations

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.

Demont EH, Bamborough P, Chung CW, Craggs PD, Fallon D, Gordon LJ, Grandi P, Hobbs CI, Hussain J, Jones EJ, Le Gall A, Michon AM, Mitchell DJ, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ
ACS Med Chem Lett 5 1190-5 (2014)
Cited: 40 times
EuropePMC logo PMID: 25408830

Abstract

The BRPF (bromodomain and PHD finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. Here, we report the discovery, binding mode, and structure-activity relationship (SAR) of the first potent, selective series of inhibitors of the BRPF1 bromodomain.

Articles - 4uyd mentioned but not cited (2)

  1. The role of ZA channel water-mediated interactions in the design of bromodomain-selective BET inhibitors. Bharatham N, Slavish PJ, Shadrick WR, Young BM, Young BM, Shelat AA. J Mol Graph Model 81 197-210 (2018)
  2. Interactions between BRD4S, LOXL2, and MED1 drive cell cycle transcription in triple-negative breast cancer. Pascual-Reguant L, Serra-Camprubí Q, Datta D, Cianferoni D, Kourtis S, Gañez-Zapater A, Cannatá C, Espinar L, Querol J, García-López L, Musa-Afaneh S, Guirola M, Gkanogiannis A, Miró Canturri A, Guzman M, Rodríguez O, Herencia-Ropero A, Arribas J, Serra V, Serrano L, Tian TV, Peiró S, Sdelci S. EMBO Mol Med 15 e18459 (2023)


Reviews citing this publication (15)

  1. NanoLuc: A Small Luciferase Is Brightening Up the Field of Bioluminescence. England CG, Ehlerding EB, Cai W. Bioconjug Chem 27 1175-1187 (2016)
  2. Bromodomain inhibitors and cancer therapy: From structures to applications. Pérez-Salvia M, Esteller M. Epigenetics 12 323-339 (2017)
  3. Lysine Acetylation Goes Global: From Epigenetics to Metabolism and Therapeutics. Ali I, Conrad RJ, Verdin E, Ott M. Chem Rev 118 1216-1252 (2018)
  4. 1001 lights: luciferins, luciferases, their mechanisms of action and applications in chemical analysis, biology and medicine. Kaskova ZM, Tsarkova AS, Yampolsky IV. Chem Soc Rev 45 6048-6077 (2016)
  5. Bromodomain biology and drug discovery. Zaware N, Zhou MM. Nat Struct Mol Biol 26 870-879 (2019)
  6. Biological function and histone recognition of family IV bromodomain-containing proteins. Lloyd JT, Glass KC. J Cell Physiol 233 1877-1886 (2018)
  7. Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology. Galdeano C, Ciulli A. Future Med Chem 8 1655-1680 (2016)
  8. Bromodomains in Protozoan Parasites: Evolution, Function, and Opportunities for Drug Development. Jeffers V, Yang C, Huang S, Sullivan WJ. Microbiol Mol Biol Rev 81 e00047-16 (2017)
  9. Chemical probes and inhibitors of bromodomains outside the BET family. Moustakim M, Clark PGK, Hay DA, Dixon DJ, Brennan PE. Medchemcomm 7 2246-2264 (2016)
  10. Progress in the Development of non-BET Bromodomain Chemical Probes. Theodoulou NH, Tomkinson NC, Prinjha RK, Humphreys PG. ChemMedChem 11 477-487 (2016)
  11. Targeting BRD9 for Cancer Treatment: A New Strategy. Zhu X, Liao Y, Tang L. Onco Targets Ther 13 13191-13200 (2020)
  12. Selective targeting of epigenetic reader domains. Greschik H, Schüle R, Günther T. Expert Opin Drug Discov 12 449-463 (2017)
  13. Structural features and inhibitors of bromodomains. Meslamani J, Smith SG, Sanchez R, Zhou MM. Drug Discov Today Technol 19 3-15 (2016)
  14. Targeting bromodomain-containing proteins: research advances of drug discovery. Pan Z, Zhao Y, Wang X, Xie X, Liu M, Zhang K, Wang L, Bai D, Foster LJ, Shu R, He G. Mol Biomed 4 13 (2023)
  15. Bromodomain inhibitors and therapeutic applications. Gajjela BK, Zhou MM. Curr Opin Chem Biol 75 102323 (2023)

Articles citing this publication (23)

  1. Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. Theodoulou NH, Bamborough P, Bannister AJ, Becher I, Bit RA, Che KH, Chung CW, Dittmann A, Drewes G, Drewry DH, Gordon L, Grandi P, Leveridge M, Lindon M, Michon AM, Molnar J, Robson SC, Tomkinson NC, Kouzarides T, Prinjha RK, Humphreys PG. J Med Chem 59 1425-1439 (2016)
  2. Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. Palmer WS, Poncet-Montange G, Liu G, Petrocchi A, Reyna N, Subramanian G, Theroff J, Yau A, Kost-Alimova M, Bardenhagen JP, Leo E, Shepard HE, Tieu TN, Shi X, Zhan Y, Zhao S, Barton MC, Draetta G, Toniatti C, Jones P, Geck Do M, Andersen JN. J Med Chem 59 1440-1454 (2016)
  3. The Bromodomain: A New Target in Emerging Epigenetic Medicine. Smith SG, Zhou MM. ACS Chem Biol 11 598-608 (2016)
  4. Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. Bennett J, Fedorov O, Tallant C, Monteiro O, Meier J, Gamble V, Savitsky P, Nunez-Alonso GA, Haendler B, Rogers C, Brennan PE, Müller S, Knapp S. J Med Chem 59 1642-1647 (2016)
  5. Dose-dependent activation of gene expression is achieved using CRISPR and small molecules that recruit endogenous chromatin machinery. Chiarella AM, Butler KV, Gryder BE, Lu D, Wang TA, Yu X, Pomella S, Khan J, Jin J, Hathaway NA. Nat Biotechnol 38 50-55 (2020)
  6. 9H-purine scaffold reveals induced-fit pocket plasticity of the BRD9 bromodomain. Picaud S, Strocchia M, Terracciano S, Lauro G, Mendez J, Daniels DL, Riccio R, Bifulco G, Bruno I, Filippakopoulos P. J Med Chem 58 2718-2736 (2015)
  7. Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains. Bouché L, Christ CD, Siegel S, Fernández-Montalván AE, Holton SJ, Fedorov O, Ter Laak A, Sugawara T, Stöckigt D, Tallant C, Bennett J, Monteiro O, Díaz-Sáez L, Siejka P, Meier J, Pütter V, Weiske J, Müller S, Huber KVM, Hartung IV, Haendler B. J Med Chem 60 4002-4022 (2017)
  8. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain. Bamborough P, Barnett HA, Becher I, Bird MJ, Chung CW, Craggs PD, Demont EH, Diallo H, Fallon DJ, Gordon LJ, Grandi P, Hobbs CI, Hooper-Greenhill E, Jones EJ, Law RP, Le Gall A, Lugo D, Michon AM, Mitchell DJ, Prinjha RK, Sheppard RJ, Watson AJ, Watson RJ. ACS Med Chem Lett 7 552-557 (2016)
  9. Identification of Covalent Bromodomain Binders through DNA Display of Small Molecules. Daguer JP, Zambaldo C, Abegg D, Barluenga S, Tallant C, Müller S, Adibekian A, Winssinger N. Angew Chem Int Ed Engl 54 6057-6061 (2015)
  10. Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation. Meier JC, Tallant C, Fedorov O, Witwicka H, Hwang SY, van Stiphout RG, Lambert JP, Rogers C, Yapp C, Gerstenberger BS, Fedele V, Savitsky P, Heidenreich D, Daniels DL, Owen DR, Fish PV, Igoe NM, Bayle ED, Haendler B, Oppermann UCT, Buffa F, Brennan PE, Müller S, Gingras AC, Odgren PR, Birnbaum MJ, Knapp S. ACS Chem Biol 12 2619-2630 (2017)
  11. Cross-talk between chromatin acetylation and SUMOylation of tripartite motif-containing protein 24 (TRIM24) impacts cell adhesion. Appikonda S, Thakkar KN, Shah PK, Dent SYR, Andersen JN, Barton MC. J Biol Chem 293 7476-7485 (2018)
  12. Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance. Crawford TD, Vartanian S, Côté A, Bellon S, Duplessis M, Flynn EM, Hewitt M, Huang HR, Kiefer JR, Murray J, Nasveschuk CG, Pardo E, Romero FA, Sandy P, Tang Y, Taylor AM, Tsui V, Wang J, Wang S, Zawadzke L, Albrecht BK, Magnuson SR, Cochran AG, Stokoe D. Bioorg Med Chem Lett 27 3534-3541 (2017)
  13. Chemical Space Expansion of Bromodomain Ligands Guided by in Silico Virtual Couplings (AutoCouple). Batiste L, Unzue A, Dolbois A, Hassler F, Wang X, Deerain N, Zhu J, Spiliotopoulos D, Nevado C, Caflisch A. ACS Cent Sci 4 180-188 (2018)
  14. Activity of bromodomain protein inhibitors/binders against asexual-stage Plasmodium falciparum parasites. Chua MJ, Robaa D, Skinner-Adams TS, Sippl W, Andrews KT. Int J Parasitol Drugs Drug Resist 8 189-193 (2018)
  15. Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study. Li X, Zhang Y, Jiang Y, Wu J, Inks ES, Chou CJ, Gao S, Hou J, Ding Q, Li J, Wang X, Huang Y, Xu W. Eur J Med Chem 134 185-206 (2017)
  16. The polar warhead of a TRIM24 bromodomain inhibitor rearranges a water-mediated interaction network. Liu J, Li F, Bao H, Jiang Y, Zhang S, Ma R, Gao J, Wu J, Ruan K. FEBS J 284 1082-1095 (2017)
  17. Inhibition of the TRIM24 bromodomain reactivates latent HIV-1. Horvath RM, Brumme ZL, Sadowski I. Sci Rep 13 556 (2023)
  18. An epigenetic regulator-related score (EpiScore) predicts survival in patients with diffuse large B cell lymphoma and identifies patients who may benefit from epigenetic therapy. Szablewski V, Bret C, Kassambara A, Devin J, Cartron G, Costes-Martineau V, Moreaux J. Oncotarget 9 19079-19099 (2018)
  19. Virtual screen to NMR (VS2NMR): Discovery of fragment hits for the CBP bromodomain. Spiliotopoulos D, Zhu J, Wamhoff EC, Deerain N, Marchand JR, Aretz J, Rademacher C, Caflisch A. Bioorg Med Chem Lett 27 2472-2478 (2017)
  20. NMR Molecular Replacement Provides New Insights into Binding Modes to Bromodomains of BRD4 and TRIM24. Torres F, Walser R, Kaderli J, Rossi E, Bobby R, Packer MJ, Sarda S, Walker G, Hitchin JR, Milbradt AG, Orts J. J Med Chem 65 5565-5574 (2022)
  21. Pharmacophore-based virtual screening, molecular docking, molecular dynamics simulation, and biological evaluation for the discovery of novel BRD4 inhibitors. Yan G, Hou M, Luo J, Pu C, Hou X, Lan S, Li R. Chem Biol Drug Des 91 478-490 (2018)
  22. Rational Design and Development of Selective BRD7 Bromodomain Inhibitors and Their Activity in Prostate Cancer. Ordonez-Rubiano SC, Maschinot CA, Wang S, Sood S, Baracaldo-Lancheros LF, Strohmier BP, McQuade AJ, Smith BC, Dykhuizen EC. J Med Chem 66 11250-11270 (2023)
  23. Development and Biological Evaluation of the First Highly Potent and Specific Benzamide-Based Radiotracer [18F]BA3 for Imaging of Histone Deacetylases 1 and 2 in Brain. Clauß O, Schäker-Hübner L, Wenzel B, Toussaint M, Deuther-Conrad W, Gündel D, Teodoro R, Dukić-Stefanović S, Ludwig FA, Kopka K, Brust P, Hansen FK, Scheunemann M. Pharmaceuticals (Basel) 15 324 (2022)


Quick links