5cfw › Citations

Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities.

Chekler EL, Pellegrino JA, Lanz TA, Denny RA, Flick AC, Coe J, Langille J, Basak A, Liu S, Stock IA, Sahasrabudhe P, Bonin PD, Lee K, Pletcher MT, Jones LH
Chem Biol 22 1588-96 (2015)
Cited: 26 times
EuropePMC logo PMID: 26670081

Abstract

Bromodomains are involved in transcriptional regulation through the recognition of acetyl lysine modifications on diverse proteins. Selective pharmacological modulators of bromodomains are lacking, although the largely hydrophobic nature of the pocket makes these modules attractive targets for small-molecule inhibitors. This work describes the structure-based design of a highly selective inhibitor of the CREB binding protein (CBP) bromodomain and its use in cell-based transcriptional profiling experiments. The inhibitor downregulated a number of inflammatory genes in macrophages that were not affected by a selective BET bromodomain inhibitor. In addition, the CBP bromodomain inhibitor modulated the mRNA level of the regulator of G-protein signaling 4 (RGS4) gene in neurons, suggesting a potential therapeutic opportunity for CBP inhibitors in the treatment of neurological disorders.

Articles - 5cfw mentioned but not cited (2)

  1. qFit-ligand Reveals Widespread Conformational Heterogeneity of Drug-Like Molecules in X-Ray Electron Density Maps. van Zundert GCP, Hudson BM, de Oliveira SHP, Keedy DA, Fonseca R, Heliou A, Suresh P, Borrelli K, Day T, Fraser JS, van den Bedem H. J Med Chem 61 11183-11198 (2018)
  2. Identification of Markers for Diagnosis and Treatment of Diabetic Kidney Disease Based on the Ferroptosis and Immune. Ma J, Li C, Liu T, Zhang L, Wen X, Liu X, Fan W. Oxid Med Cell Longev 2022 9957172 (2022)


Reviews citing this publication (11)

  1. Bromodomain inhibitors and cancer therapy: From structures to applications. Pérez-Salvia M, Esteller M. Epigenetics 12 323-339 (2017)
  2. Clinical progress and pharmacology of small molecule bromodomain inhibitors. Theodoulou NH, Tomkinson NC, Prinjha RK, Humphreys PG. Curr Opin Chem Biol 33 58-66 (2016)
  3. 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)
  4. ETS-targeted therapy: can it substitute for MEK inhibitors? Tetsu O, McCormick F. Clin Transl Med 6 16 (2017)
  5. 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)
  6. Progress in the Development of non-BET Bromodomain Chemical Probes. Theodoulou NH, Tomkinson NC, Prinjha RK, Humphreys PG. ChemMedChem 11 477-487 (2016)
  7. Regulating the regulators: Epigenetic, transcriptional, and post-translational regulation of RGS proteins. Alqinyah M, Hooks SB. Cell Signal 42 77-87 (2018)
  8. Targeting Histone Acetylation: Readers and Writers in Leukemia and Cancer. Benton CB, Fiskus W, Bhalla KN. Cancer J 23 286-291 (2017)
  9. Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy. Zhu H, Wei T, Cai Y, Jin J. Molecules 25 E578 (2020)
  10. Allosteric regulation of epigenetic modifying enzymes. Zucconi BE, Cole PA. Curr Opin Chem Biol 39 109-115 (2017)
  11. Selective Targeting of Epigenetic Readers and Histone Deacetylases in Autoimmune and Inflammatory Diseases: Recent Advances and Future Perspectives. Ghiboub M, Elfiky AMI, de Winther MPJ, Harker NR, Tough DF, de Jonge WJ. J Pers Med 11 336 (2021)

Articles citing this publication (13)

  1. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). Taylor AM, Côté A, Hewitt MC, Pastor R, Leblanc Y, Nasveschuk CG, Romero FA, Crawford TD, Cantone N, Jayaram H, Setser J, Murray J, Beresini MH, de Leon Boenig G, Chen Z, Conery AR, Cummings RT, Dakin LA, Flynn EM, Huang OW, Kaufman S, Keller PJ, Kiefer JR, Lai T, Li Y, Liao J, Liu W, Lu H, Pardo E, Tsui V, Wang J, Wang Y, Xu Z, Yan F, Yu D, Zawadzke L, Zhu X, Zhu X, Sims RJ, Cochran AG, Bellon S, Audia JE, Magnuson S, Albrecht BK. ACS Med Chem Lett 7 531-536 (2016)
  2. The transcriptional coactivator CBP/p300 is an evolutionarily conserved node that promotes longevity in response to mitochondrial stress. Li TY, Sleiman MB, Li H, Gao AW, Mottis A, Bachmann AM, El Alam G, Li X, Goeminne LJE, Schoonjans K, Auwerx J. Nat Aging 1 165-178 (2021)
  3. Anxiolytic effects of Formononetin in an inflammatory pain mouse model. Wang XS, Guan SY, Liu A, Yue J, Hu LN, Zhang K, Yang LK, Lu L, Tian Z, Zhao MG, Liu SB. Mol Brain 12 36 (2019)
  4. Histone acetyltransferase and Polo-like kinase 3 inhibitors prevent rat galactose-induced cataract. Kanada F, Takamura Y, Miyake S, Kamata K, Inami M, Inatani M, Oki M. Sci Rep 9 20085 (2019)
  5. Y08197 is a novel and selective CBP/EP300 bromodomain inhibitor for the treatment of prostate cancer. Zou LJ, Xiang QP, Xue XQ, Zhang C, Li CC, Wang C, Li Q, Wang R, Wu S, Zhou YL, Zhang Y, Xu Y. Acta Pharmacol Sin 40 1436-1447 (2019)
  6. Beyond the BET Family: Targeting CBP/p300 with 4-Acyl Pyrroles. Hügle M, Lucas X, Ostrovskyi D, Regenass P, Gerhardt S, Einsle O, Hau M, Jung M, Breit B, Günther S, Wohlwend D. Angew Chem Int Ed Engl 56 12476-12480 (2017)
  7. Editorial An industry perspective on drug target validation. Jones LH. Expert Opin Drug Discov 11 623-625 (2016)
  8. Development of Dimethylisoxazole-Attached Imidazo[1,2-a]pyridines as Potent and Selective CBP/P300 Inhibitors. Muthengi A, Wimalasena VK, Yosief HO, Bikowitz MJ, Sigua LH, Wang T, Li D, Gaieb Z, Dhawan G, Liu S, Erickson J, Amaro RE, Schönbrunn E, Qi J, Zhang W. J Med Chem 64 5787-5801 (2021)
  9. Discovery of novel CBP bromodomain inhibitors through TR-FRET-based high-throughput screening. Zhang FC, Sun ZY, Liao LP, Zuo Y, Zhang D, Wang J, Chen YT, Xiao SH, Jiang H, Lu T, Xu P, Yue LY, Du DH, Zhang H, Liu CP, Luo C. Acta Pharmacol Sin 41 286-292 (2020)
  10. Dissecting the impact of bromodomain inhibitors on the Interferon Regulatory Factor 4-MYC oncogenic axis in multiple myeloma. Agnarelli A, Mitchell S, Caalim G, Wood CD, Milton-Harris L, Chevassut T, West MJ, Mancini EJ. Hematol Oncol 40 417-429 (2022)
  11. 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)
  12. Selectivity Mechanism of Pyrrolopyridone Analogues Targeting Bromodomain 2 of Bromodomain-Containing Protein 4 from Molecular Dynamics Simulations. Shi M, Zheng X, Zhou Y, Yin Y, Lu Z, Zou Z, Hu Y, Liang Y, Chen T, Yang Y, Jing M, Lei D, Yang P, Li X. ACS Omega 8 33658-33674 (2023)
  13. Systematic literature review reveals suboptimal use of chemical probes in cell-based biomedical research. Sterling J, Baker JR, McCluskey A, Munoz L. Nat Commun 14 3228 (2023)


Quick links