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The structural basis of ZMPSTE24-dependent laminopathies.
Quigley A, Dong YY, Pike AC, Dong L, Shrestha L, Berridge G, Stansfeld PJ, Sansom MS, Edwards AM, Bountra C, von Delft F, Bullock AN, Burgess-Brown NA, Carpenter EP. Quigley A, et al. Among authors: bountra c. Science. 2013 Mar 29;339(6127):1604-7. doi: 10.1126/science.1231513. Science. 2013. PMID: 23539603
Structures of ABCB10, a human ATP-binding cassette transporter in apo- and nucleotide-bound states.
Shintre CA, Pike AC, Li Q, Kim JI, Barr AJ, Goubin S, Shrestha L, Yang J, Berridge G, Ross J, Stansfeld PJ, Sansom MS, Edwards AM, Bountra C, Marsden BD, von Delft F, Bullock AN, Gileadi O, Burgess-Brown NA, Carpenter EP. Shintre CA, et al. Among authors: bountra c. Proc Natl Acad Sci U S A. 2013 Jun 11;110(24):9710-5. doi: 10.1073/pnas.1217042110. Epub 2013 May 28. Proc Natl Acad Sci U S A. 2013. PMID: 23716676 Free PMC article.
The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery.
Bradley AR, Echalier A, Fairhead M, Strain-Damerell C, Brennan P, Bullock AN, Burgess-Brown NA, Carpenter EP, Gileadi O, Marsden BD, Lee WH, Yue W, Bountra C, von Delft F. Bradley AR, et al. Among authors: bountra c. Essays Biochem. 2017 Nov 8;61(5):495-503. doi: 10.1042/EBC20170051. Print 2017 Nov 8. Essays Biochem. 2017. PMID: 29118096 Free PMC article. Review.
The precompetitive space: time to move the yardsticks.
Norman T, Edwards A, Bountra C, Friend S. Norman T, et al. Among authors: bountra c. Sci Transl Med. 2011 Mar 30;3(76):76cm10. doi: 10.1126/scitranslmed.3002399. Sci Transl Med. 2011. PMID: 21451121
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J. Bavetsias V, et al. Among authors: bountra c. J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7. J Med Chem. 2016. PMID: 26741168 Free PMC article.
Preclinical target validation using patient-derived cells.
Edwards AM, Arrowsmith CH, Bountra C, Bunnage ME, Feldmann M, Knight JC, Patel DD, Prinos P, Taylor MD, Sundström M; SGC Open Source Target-Discovery Partnership. Edwards AM, et al. Among authors: bountra c. Nat Rev Drug Discov. 2015 Mar;14(3):149-50. doi: 10.1038/nrd4565. Epub 2015 Feb 20. Nat Rev Drug Discov. 2015. PMID: 25722227
Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.
Tumber A, Nuzzi A, Hookway ES, Hatch SB, Velupillai S, Johansson C, Kawamura A, Savitsky P, Yapp C, Szykowska A, Wu N, Bountra C, Strain-Damerell C, Burgess-Brown NA, Ruda GF, Fedorov O, Munro S, England KS, Nowak RP, Schofield CJ, La Thangue NB, Pawlyn C, Davies F, Morgan G, Athanasou N, Müller S, Oppermann U, Brennan PE. Tumber A, et al. Among authors: bountra c. Cell Chem Biol. 2017 Mar 16;24(3):371-380. doi: 10.1016/j.chembiol.2017.02.006. Epub 2017 Mar 2. Cell Chem Biol. 2017. PMID: 28262558 Free PMC article.
An Activity-Based Probe Targeting Non-Catalytic, Highly Conserved Amino Acid Residues within Bromodomains.
D'Ascenzio M, Pugh KM, Konietzny R, Berridge G, Tallant C, Hashem S, Monteiro O, Thomas JR, Schirle M, Knapp S, Marsden B, Fedorov O, Bountra C, Kessler BM, Brennan PE. D'Ascenzio M, et al. Among authors: bountra c. Angew Chem Int Ed Engl. 2019 Jan 21;58(4):1007-1012. doi: 10.1002/anie.201807825. Epub 2018 Dec 27. Angew Chem Int Ed Engl. 2019. PMID: 30589164 Free PMC article.
121 results