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Items: 41

1.

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.

Angew Chem Int Ed Engl. 2019 Jan 21;58(4):1007-1012. doi: 10.1002/anie.201807825. Epub 2018 Dec 27.

2.

Identifying Small-Molecule Binding Sites for Epigenetic Proteins at Domain-Domain Interfaces.

Bowkett D, Talon R, Tallant C, Schofield C, von Delft F, Knapp S, Bruton G, Brennan PE.

ChemMedChem. 2018 May 23;13(10):1051-1057. doi: 10.1002/cmdc.201800030. Epub 2018 Apr 17.

3.

Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.

Shadrick WR, Slavish PJ, Chai SC, Waddell B, Connelly M, Low JA, Tallant C, Young BM, Bharatham N, Knapp S, Boyd VA, Morfouace M, Roussel MF, Chen T, Lee RE, Kiplin Guy R, Shelat AA, Potter PM.

Bioorg Med Chem. 2018 Jan 1;26(1):25-36. doi: 10.1016/j.bmc.2017.10.042. Epub 2017 Nov 4.

4.

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. 2017 Oct 20;12(10):2619-2630. doi: 10.1021/acschembio.7b00481. Epub 2017 Sep 12.

5.

Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins.

Igoe N, Bayle ED, Tallant C, Fedorov O, Meier JC, Savitsky P, Rogers C, Morias Y, Scholze S, Boyd H, Cunoosamy D, Andrews DM, Cheasty A, Brennan PE, Müller S, Knapp S, Fish PV.

J Med Chem. 2017 Aug 24;60(16):6998-7011. doi: 10.1021/acs.jmedchem.7b00611. Epub 2017 Aug 10.

PMID:
28714688
6.

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. 2017 May 11;60(9):4002-4022. doi: 10.1021/acs.jmedchem.7b00306. Epub 2017 May 1.

7.

Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease.

Batson J, Toop HD, Redondo C, Babaei-Jadidi R, Chaikuad A, Wearmouth SF, Gibbons B, Allen C, Tallant C, Zhang J, Du C, Hancox JC, Hawtrey T, Da Rocha J, Griffith R, Knapp S, Bates DO, Morris JC.

ACS Chem Biol. 2017 Mar 17;12(3):825-832. doi: 10.1021/acschembio.6b01048. Epub 2017 Feb 6.

8.

Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.

Igoe N, Bayle ED, Fedorov O, Tallant C, Savitsky P, Rogers C, Owen DR, Deb G, Somervaille TC, Andrews DM, Jones N, Cheasty A, Ryder H, Brennan PE, Müller S, Knapp S, Fish PV.

J Med Chem. 2017 Jan 26;60(2):668-680. doi: 10.1021/acs.jmedchem.6b01583. Epub 2017 Jan 9.

PMID:
28068087
9.

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.

Picaud S, Leonards K, Lambert JP, Dovey O, Wells C, Fedorov O, Monteiro O, Fujisawa T, Wang CY, Lingard H, Tallant C, Nikbin N, Guetzoyan L, Ingham R, Ley SV, Brennan P, Muller S, Samsonova A, Gingras AC, Schwaller J, Vassiliou G, Knapp S, Filippakopoulos P.

Sci Adv. 2016 Oct 12;2(10):e1600760. eCollection 2016 Oct.

10.

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.

Popp TA, Tallant C, Rogers C, Fedorov O, Brennan PE, Müller S, Knapp S, Bracher F.

J Med Chem. 2016 Oct 13;59(19):8889-8912. Epub 2016 Sep 27.

PMID:
27673482
11.

Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis.

Myrianthopoulos V, Gaboriaud-Kolar N, Tallant C, Hall ML, Grigoriou S, Brownlee PM, Fedorov O, Rogers C, Heidenreich D, Wanior M, Drosos N, Mexia N, Savitsky P, Bagratuni T, Kastritis E, Terpos E, Filippakopoulos P, Müller S, Skaltsounis AL, Downs JA, Knapp S, Mikros E.

J Med Chem. 2016 Oct 13;59(19):8787-8803. Epub 2016 Sep 27.

12.

Acute, Severe Cryptosporidiosis in an Immunocompetent Pediatric Patient.

Tallant C, Huddleston P, Alshanberi A, Misra S.

Clin Pract. 2016 Jul 4;6(2):837. doi: 10.4081/cp.2016.837. eCollection 2016 Apr 26.

13.

Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability.

Lori L, Pasquo A, Lori C, Petrosino M, Chiaraluce R, Tallant C, Knapp S, Consalvi V.

PLoS One. 2016 Jul 12;11(7):e0159180. doi: 10.1371/journal.pone.0159180. eCollection 2016.

14.

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor.

Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ.

Angew Chem Weinheim Bergstr Ger. 2015 May 18;127(21):6315-6319. Epub 2015 Apr 13.

15.

BET inhibition as a new strategy for the treatment of gastric cancer.

Montenegro RC, Clark PG, Howarth A, Wan X, Ceroni A, Siejka P, Nunez-Alonso GA, Monteiro O, Rogers C, Gamble V, Burbano R, Brennan PE, Tallant C, Ebner D, Fedorov O, O'Neill E, Knapp S, Dixon D, Müller S.

Oncotarget. 2016 Jul 12;7(28):43997-44012. doi: 10.18632/oncotarget.9766.

16.

Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk.

Sdelci S, Lardeau CH, Tallant C, Klepsch F, Klaiber B, Bennett J, Rathert P, Schuster M, Penz T, Fedorov O, Superti-Furga G, Bock C, Zuber J, Huber KV, Knapp S, Müller S, Kubicek S.

Nat Chem Biol. 2016 Jul;12(7):504-10. doi: 10.1038/nchembio.2080. Epub 2016 May 9.

PMID:
27159579
17.

Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex.

Sutherell CL, Tallant C, Monteiro OP, Yapp C, Fuchs JE, Fedorov O, Siejka P, Müller S, Knapp S, Brenton JD, Brennan PE, Ley SV.

J Med Chem. 2016 May 26;59(10):5095-101. doi: 10.1021/acs.jmedchem.5b01997. Epub 2016 May 11.

18.

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.

Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers C, Parikh M, Taylor A, Samas B, O'Mahony A, Berg E, Pallares G, Torrey AD, Treiber DK, Samardjiev IJ, Nasipak BT, Padilla-Benavides T, Wu Q, Imbalzano AN, Nickerson JA, Bunnage ME, Müller S, Knapp S, Owen DR.

J Med Chem. 2016 May 26;59(10):4800-11. doi: 10.1021/acs.jmedchem.6b00012. Epub 2016 May 3.

19.

Spontaneous pneumoperitoneum in pediatric patients: A case series.

Tallant C, Tallant A, Nirgiotis J, Meller J.

Int J Surg Case Rep. 2016;22:55-8. doi: 10.1016/j.ijscr.2016.03.017. Epub 2016 Mar 19.

20.

Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib.

Mathea S, Abdul Azeez KR, Salah E, Tallant C, Wolfreys F, Konietzny R, Fischer R, Lou HJ, Brennan PE, Schnapp G, Pautsch A, Kessler BM, Turk BE, Knapp S.

ACS Chem Biol. 2016 Jun 17;11(6):1595-602. doi: 10.1021/acschembio.6b00043. Epub 2016 Mar 31.

21.

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.

Martin LJ, Koegl M, Bader G, Cockcroft XL, Fedorov O, Fiegen D, Gerstberger T, Hofmann MH, Hohmann AF, Kessler D, Knapp S, Knesl P, Kornigg S, Müller S, Nar H, Rogers C, Rumpel K, Schaaf O, Steurer S, Tallant C, Vakoc CR, Zeeb M, Zoephel A, Pearson M, Boehmelt G, McConnell D.

J Med Chem. 2016 May 26;59(10):4462-75. doi: 10.1021/acs.jmedchem.5b01865. Epub 2016 Mar 10.

22.

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.

Fedorov O, Castex J, Tallant C, Owen DR, Martin S, Aldeghi M, Monteiro O, Filippakopoulos P, Picaud S, Trzupek JD, Gerstenberger BS, Bountra C, Willmann D, Wells C, Philpott M, Rogers C, Biggin PC, Brennan PE, Bunnage ME, Schüle R, Günther T, Knapp S, Müller S.

Sci Adv. 2015 Nov 13;1(10):e1500723. doi: 10.1126/sciadv.1500723. eCollection 2015 Nov.

23.

New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.

Baud MG, Lin-Shiao E, Zengerle M, Tallant C, Ciulli A.

J Med Chem. 2016 Feb 25;59(4):1492-500. doi: 10.1021/acs.jmedchem.5b01135. Epub 2015 Oct 1.

24.

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.

Hammitzsch A, Tallant C, Fedorov O, O'Mahony A, Brennan PE, Hay DA, Martinez FO, Al-Mossawi MH, de Wit J, Vecellio M, Wells C, Wordsworth P, Müller S, Knapp S, Bowness P.

Proc Natl Acad Sci U S A. 2015 Aug 25;112(34):10768-73. doi: 10.1073/pnas.1501956112. Epub 2015 Aug 10.

25.

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. 2016 Feb 25;59(4):1642-7. doi: 10.1021/acs.jmedchem.5b00458. Epub 2015 May 20.

26.

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor.

Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ.

Angew Chem Int Ed Engl. 2015 May 18;54(21):6217-21. doi: 10.1002/anie.201501394. Epub 2015 Apr 13.

27.

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.

Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH.

J Med Chem. 2016 Feb 25;59(4):1410-24. doi: 10.1021/acs.jmedchem.5b00209. Epub 2015 Apr 6.

28.

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. 2015 May 11;54(20):6057-61. doi: 10.1002/anie.201412276. Epub 2015 Mar 13.

PMID:
25772490
29.

Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B.

Drouin L, McGrath S, Vidler LR, Chaikuad A, Monteiro O, Tallant C, Philpott M, Rogers C, Fedorov O, Liu M, Akhtar W, Hayes A, Raynaud F, Müller S, Knapp S, Hoelder S.

J Med Chem. 2015 Mar 12;58(5):2553-9. doi: 10.1021/jm501963e. Epub 2015 Feb 26.

30.

Molecular basis of histone tail recognition by human TIP5 PHD finger and bromodomain of the chromatin remodeling complex NoRC.

Tallant C, Valentini E, Fedorov O, Overvoorde L, Ferguson FM, Filippakopoulos P, Svergun DI, Knapp S, Ciulli A.

Structure. 2015 Jan 6;23(1):80-92. doi: 10.1016/j.str.2014.10.017. Epub 2014 Dec 18.

31.

Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes.

Baud MGJ, Lin-Shiao E, Cardote T, Tallant C, Pschibul A, Chan KH, Zengerle M, Garcia JR, Kwan TT, Ferguson FM, Ciulli A.

Science. 2014 Oct 31;346(6209):638-641. doi: 10.1126/science.1249830. Epub 2014 Oct 16.

32.

MRI of the knee and shoulder performed before radiography.

George E, Tsipas S, Wozniak G, Rubin DA, Seidenwurm DJ, Raghavan K, Golden W, Tallant C, Bhargavan-Chatfield M, Burleson J, Rybicki FJ.

J Am Coll Radiol. 2014 Nov;11(11):1053-8. doi: 10.1016/j.jacr.2014.05.014. Epub 2014 Jul 31.

PMID:
25086957
33.

Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains.

Hay DA, Fedorov O, Martin S, Singleton DC, Tallant C, Wells C, Picaud S, Philpott M, Monteiro OP, Rogers CM, Conway SJ, Rooney TP, Tumber A, Yapp C, Filippakopoulos P, Bunnage ME, Müller S, Knapp S, Schofield CJ, Brennan PE.

J Am Chem Soc. 2014 Jul 2;136(26):9308-19. doi: 10.1021/ja412434f. Epub 2014 Jun 19.

34.

Performance measures in radiology.

You-Ling Shyu J, Burleson J, Tallant C, Seidenwurm DJ, Rybicki FJ.

J Am Coll Radiol. 2014 May;11(5):456-63. doi: 10.1016/j.jacr.2013.11.019.

35.

A Bacillus anthracis strain deleted for six proteases serves as an effective host for production of recombinant proteins.

Pomerantsev AP, Pomerantseva OM, Moayeri M, Fattah R, Tallant C, Leppla SH.

Protein Expr Purif. 2011 Nov;80(1):80-90. doi: 10.1016/j.pep.2011.05.016. Epub 2011 Aug 7.

36.

On the relevance of the Met-turn methionine in metzincins.

Tallant C, García-Castellanos R, Baumann U, Gomis-Rüth FX.

J Biol Chem. 2010 Apr 30;285(18):13951-7. doi: 10.1074/jbc.M109.083378. Epub 2010 Mar 4.

37.

Unique structure and stability of HmuY, a novel heme-binding protein of Porphyromonas gingivalis.

Wójtowicz H, Guevara T, Tallant C, Olczak M, Sroka A, Potempa J, Solà M, Olczak T, Gomis-Rüth FX.

PLoS Pathog. 2009 May;5(5):e1000419. doi: 10.1371/journal.ppat.1000419. Epub 2009 May 8.

38.

Matrix metalloproteinases: fold and function of their catalytic domains.

Tallant C, Marrero A, Gomis-Rüth FX.

Biochim Biophys Acta. 2010 Jan;1803(1):20-8. doi: 10.1016/j.bbamcr.2009.04.003. Epub 2009 Apr 15. Review.

39.

Activity of ulilysin, an archaeal PAPP-A-related gelatinase and IGFBP protease.

Tallant C, García-Castellanos R, Marrero A, Canals F, Yang Y, Reymond JL, Solà M, Baumann U, Gomis-Rüth FX.

Biol Chem. 2007 Nov;388(11):1243-53.

PMID:
17976018
40.

Substrate specificity of a metalloprotease of the pappalysin family revealed by an inhibitor and a product complex.

García-Castellanos R, Tallant C, Marrero A, Solà M, Baumann U, Gomis-Rüth FX.

Arch Biochem Biophys. 2007 Jan 1;457(1):57-72. Epub 2006 Oct 24.

41.

Molecular analysis of ulilysin, the structural prototype of a new family of metzincin metalloproteases.

Tallant C, García-Castellanos R, Seco J, Baumann U, Gomis-Rüth FX.

J Biol Chem. 2006 Jun 30;281(26):17920-8. Epub 2006 Apr 20.

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