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Items: 33

1.

A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function.

Fagan V, Johansson C, Gileadi C, Monteiro O, Dunford JE, Nibhani R, Philpott M, Malzahn J, Wells G, Faram R, Cribbs AP, Halidi N, Li F, Chau I, Greschik H, Velupillai S, Allali-Hassani A, Bennett J, Christott T, Giroud C, Lewis AM, Huber KVM, Athanasou N, Bountra C, Jung M, Schüle R, Vedadi M, Arrowsmith C, Xiong Y, Jin J, Fedorov O, Farnie G, Brennan PE, Oppermann U.

J Med Chem. 2019 Oct 24;62(20):9008-9025. doi: 10.1021/acs.jmedchem.9b00562. Epub 2019 Oct 15.

PMID:
31550156
2.

Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3.

Böttcher J, Dilworth D, Reiser U, Neumüller RA, Schleicher M, Petronczki M, Zeeb M, Mischerikow N, Allali-Hassani A, Szewczyk MM, Li F, Kennedy S, Vedadi M, Barsyte-Lovejoy D, Brown PJ, Huber KVM, Rogers CM, Wells CI, Fedorov O, Rumpel K, Zoephel A, Mayer M, Wunberg T, Böse D, Zahn S, Arnhof H, Berger H, Reiser C, Hörmann A, Krammer T, Corcokovic M, Sharps B, Winkler S, Häring D, Cockcroft XL, Fuchs JE, Müllauer B, Weiss-Puxbaum A, Gerstberger T, Boehmelt G, Vakoc CR, Arrowsmith CH, Pearson M, McConnell DB.

Nat Chem Biol. 2019 Aug;15(8):822-829. doi: 10.1038/s41589-019-0310-x. Epub 2019 Jul 8.

PMID:
31285596
3.

Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening.

Resnick E, Bradley A, Gan J, Douangamath A, Krojer T, Sethi R, Geurink PP, Aimon A, Amitai G, Bellini D, Bennett J, Fairhead M, Fedorov O, Gabizon R, Gan J, Guo J, Plotnikov A, Reznik N, Ruda GF, Díaz-Sáez L, Straub VM, Szommer T, Velupillai S, Zaidman D, Zhang Y, Coker AR, Dowson CG, Barr HM, Wang C, Huber KVM, Brennan PE, Ovaa H, von Delft F, London N.

J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.

4.

A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.

Scheer S, Ackloo S, Medina TS, Schapira M, Li F, Ward JA, Lewis AM, Northrop JP, Richardson PL, Kaniskan HÜ, Shen Y, Liu J, Smil D, McLeod D, Zepeda-Velazquez CA, Luo M, Jin J, Barsyte-Lovejoy D, Huber KVM, De Carvalho DD, Vedadi M, Zaph C, Brown PJ, Arrowsmith CH.

Nat Commun. 2019 Jan 3;10(1):19. doi: 10.1038/s41467-018-07905-4.

5.

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors.

Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs AP, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB, Vasta JD, Thezenas ML, Bonham S, Kessler B, Bennett J, Fedorov O, Raynaud F, Donovan A, Blagg J, Bavetsias V, Oppermann U, Bountra C, Kawamura A, Brennan PE.

Angew Chem Int Ed Engl. 2019 Jan 8;58(2):515-519. doi: 10.1002/anie.201810179. Epub 2018 Dec 7.

6.

Discovery of an MLLT1/3 YEATS Domain Chemical Probe.

Moustakim M, Christott T, Monteiro OP, Bennett J, Giroud C, Ward J, Rogers CM, Smith P, Panagakou I, Díaz-Sáez L, Felce SL, Gamble V, Gileadi C, Halidi N, Heidenreich D, Chaikuad A, Knapp S, Huber KVM, Farnie G, Heer J, Manevski N, Poda G, Al-Awar R, Dixon DJ, Brennan PE, Fedorov O.

Angew Chem Int Ed Engl. 2018 Dec 10;57(50):16302-16307. doi: 10.1002/anie.201810617. Epub 2018 Nov 16.

7.

Chemical Instability and Promiscuity of Arylmethylidenepyrazolinone-Based MDMX Inhibitors.

Stefaniak J, Lewis AM, Conole D, Galan SRG, Bataille CJR, Wynne GM, Castaldi MP, Lundbäck T, Russell AJ, Huber KVM.

ACS Chem Biol. 2018 Oct 19;13(10):2849-2854. doi: 10.1021/acschembio.8b00665. Epub 2018 Sep 19.

8.

Small molecule inhibitors reveal an indispensable scaffolding role of RIPK2 in NOD2 signaling.

Hrdinka M, Schlicher L, Dai B, Pinkas DM, Bufton JC, Picaud S, Ward JA, Rogers C, Suebsuwong C, Nikhar S, Cuny GD, Huber KV, Filippakopoulos P, Bullock AN, Degterev A, Gyrd-Hansen M.

EMBO J. 2018 Sep 3;37(17). pii: e99372. doi: 10.15252/embj.201899372. Epub 2018 Jul 19.

9.

Creation of a Novel Class of Potent and Selective MutT Homologue 1 (MTH1) Inhibitors Using Fragment-Based Screening and Structure-Based Drug Design.

Rahm F, Viklund J, Trésaugues L, Ellermann M, Giese A, Ericsson U, Forsblom R, Ginman T, Günther J, Hallberg K, Lindström J, Persson LB, Silvander C, Talagas A, Díaz-Sáez L, Fedorov O, Huber KVM, Panagakou I, Siejka P, Gorjánácz M, Bauser M, Andersson M.

J Med Chem. 2018 Mar 22;61(6):2533-2551. doi: 10.1021/acs.jmedchem.7b01884. Epub 2018 Mar 7.

PMID:
29485874
10.

Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.

Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Hartnett JR, Ingold MR, Zimmerman K, Machleidt T, Kirkland TA, Huwiler KG, Ohana RF, Slater M, Otto P, Cong M, Wells CI, Berger BT, Hanke T, Glas C, Ding K, Drewry DH, Huber KVM, Willson TM, Knapp S, Müller S, Meisenheimer PL, Fan F, Wood KV, Robers MB.

Cell Chem Biol. 2018 Feb 15;25(2):206-214.e11. doi: 10.1016/j.chembiol.2017.10.010. Epub 2017 Nov 22.

11.

Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action.

Fernández-Montalván AE, Berger M, Kuropka B, Koo SJ, Badock V, Weiske J, Puetter V, Holton SJ, Stöckigt D, Ter Laak A, Centrella PA, Clark MA, Dumelin CE, Sigel EA, Soutter HH, Troast DM, Zhang Y, Cuozzo JW, Keefe AD, Roche D, Rodeschini V, Chaikuad A, Díaz-Sáez L, Bennett JM, Fedorov O, Huber KVM, Hübner J, Weinmann H, Hartung IV, Gorjánácz M.

ACS Chem Biol. 2017 Nov 17;12(11):2730-2736. doi: 10.1021/acschembio.7b00708. Epub 2017 Oct 24.

12.

Lapatinib potentiates cytotoxicity of  YM155 in neuroblastoma via inhibition of the ABCB1 efflux transporter.

Radic-Sarikas B, Halasz M, Huber KVM, Winter GE, Tsafou KP, Papamarkou T, Brunak S, Kolch W, Superti-Furga G.

Sci Rep. 2017 Jun 8;7(1):3091. doi: 10.1038/s41598-017-03129-6.

13.

Global survey of the immunomodulatory potential of common drugs.

Vladimer GI, Snijder B, Krall N, Bigenzahn JW, Huber KVM, Lardeau CH, Sanjiv K, Ringler A, Berglund UW, Sabler M, de la Fuente OL, Knöbl P, Kubicek S, Helleday T, Jäger U, Superti-Furga G.

Nat Chem Biol. 2017 Jun;13(6):681-690. doi: 10.1038/nchembio.2360. Epub 2017 Apr 24.

14.

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.

15.

Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family.

Bataille CJ, Brennan MB, Byrne S, Davies SG, Durbin M, Fedorov O, Huber KV, Jones AM, Knapp S, Liu G, Nadali A, Quevedo CE, Russell AJ, Walker RG, Westwood R, Wynne GM.

Bioorg Med Chem. 2017 May 1;25(9):2657-2665. doi: 10.1016/j.bmc.2017.02.056. Epub 2017 Feb 28.

PMID:
28341403
16.

Target engagement: Shining a light.

Huber KV.

Nat Chem Biol. 2017 Jan 19;13(2):133-134. doi: 10.1038/nchembio.2295. No abstract available.

PMID:
28103226
17.

Combinatorial Drug Screening Identifies Ewing Sarcoma-specific Sensitivities.

Radic-Sarikas B, Tsafou KP, Emdal KB, Papamarkou T, Huber KV, Mutz C, Toretsky JA, Bennett KL, Olsen JV, Brunak S, Kovar H, Superti-Furga G.

Mol Cancer Ther. 2017 Jan;16(1):88-101. doi: 10.1158/1535-7163.MCT-16-0235. Epub 2016 Nov 15.

18.

Discovery of a PCAF Bromodomain Chemical Probe.

Moustakim M, Clark PG, Trulli L, Fuentes de Arriba AL, Ehebauer MT, Chaikuad A, Murphy EJ, Mendez-Johnson J, Daniels D, Hou CD, Lin YH, Walker JR, Hui R, Yang H, Dorrell L, Rogers CM, Monteiro OP, Fedorov O, Huber KV, Knapp S, Heer J, Dixon DJ, Brennan PE.

Angew Chem Int Ed Engl. 2017 Jan 16;56(3):827-831. doi: 10.1002/anie.201610816. Epub 2016 Dec 14.

19.

Artemisinins Target GABAA Receptor Signaling and Impair α Cell Identity.

Li J, Casteels T, Frogne T, Ingvorsen C, Honoré C, Courtney M, Huber KVM, Schmitner N, Kimmel RA, Romanov RA, Sturtzel C, Lardeau CH, Klughammer J, Farlik M, Sdelci S, Vieira A, Avolio F, Briand F, Baburin I, Májek P, Pauler FM, Penz T, Stukalov A, Gridling M, Parapatics K, Barbieux C, Berishvili E, Spittler A, Colinge J, Bennett KL, Hering S, Sulpice T, Bock C, Distel M, Harkany T, Meyer D, Superti-Furga G, Collombat P, Hecksher-Sørensen J, Kubicek S.

Cell. 2017 Jan 12;168(1-2):86-100.e15. doi: 10.1016/j.cell.2016.11.010. Epub 2016 Dec 1.

20.

Heme drives hemolysis-induced susceptibility to infection via disruption of phagocyte functions.

Martins R, Maier J, Gorki AD, Huber KV, Sharif O, Starkl P, Saluzzo S, Quattrone F, Gawish R, Lakovits K, Aichinger MC, Radic-Sarikas B, Lardeau CH, Hladik A, Korosec A, Brown M, Vaahtomeri K, Duggan M, Kerjaschki D, Esterbauer H, Colinge J, Eisenbarth SC, Decker T, Bennett KL, Kubicek S, Sixt M, Superti-Furga G, Knapp S.

Nat Immunol. 2016 Dec;17(12):1361-1372. doi: 10.1038/ni.3590. Epub 2016 Oct 31.

PMID:
27798618
21.

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
22.

Profiling of Small Molecules by Chemical Proteomics.

Huber KVM, Superti-Furga G.

Methods Mol Biol. 2016;1394:211-218. doi: 10.1007/978-1-4939-3341-9_15.

PMID:
26700051
23.

Corrigendum: The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Ross R, Roth B, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Nov;11(11):887. doi: 10.1038/nchembio1115-887c. No abstract available.

PMID:
26485080
24.

Proteome-wide drug and metabolite interaction mapping by thermal-stability profiling.

Huber KV, Olek KM, Müller AC, Tan CS, Bennett KL, Colinge J, Superti-Furga G.

Nat Methods. 2015 Nov;12(11):1055-7. doi: 10.1038/nmeth.3590. Epub 2015 Sep 21.

25.

Erratum: Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.

Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G, Stukalov A, Huber KV, Schönegger A, Marcellus R, Bilban M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G.

Nat Chem Biol. 2015 Oct;11(10):815. doi: 10.1038/nchembio1015-815b. No abstract available.

PMID:
26379026
26.

The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Aug;11(8):536-41. doi: 10.1038/nchembio.1867. No abstract available. Erratum in: Nat Chem Biol. 2015 Aug;11(8):541. Roth, Brian [Corrected to Roth, Bryan] and Frederiksen, Mathias [Added]. Nat Chem Biol. 2015 Nov;11(11):887.

27.

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.

Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G, Stukalov A, Huber KVM, Schönegger A, Marcellus R, Bilban M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G.

Nat Chem Biol. 2015 Aug;11(8):571-578. doi: 10.1038/nchembio.1859. Epub 2015 Jul 13. Erratum in: Nat Chem Biol. 2015 Oct;11(10):815.

28.

A cellular screen identifies ponatinib and pazopanib as inhibitors of necroptosis.

Fauster A, Rebsamen M, Huber KV, Bigenzahn JW, Stukalov A, Lardeau CH, Scorzoni S, Bruckner M, Gridling M, Parapatics K, Colinge J, Bennett KL, Kubicek S, Krautwald S, Linkermann A, Superti-Furga G.

Cell Death Dis. 2015 May 21;6:e1767. doi: 10.1038/cddis.2015.130.

29.

Target profiling of an antimetastatic RAPTA agent by chemical proteomics: relevance to the mode of action.

Babak MV, Meier SM, Huber KVM, Reynisson J, Legin AA, Jakupec MA, Roller A, Stukalov A, Gridling M, Bennett KL, Colinge J, Berger W, Dyson PJ, Superti-Furga G, Keppler BK, Hartinger CG.

Chem Sci. 2015 Apr 1;6(4):2449-2456. doi: 10.1039/c4sc03905j. Epub 2015 Feb 9.

30.

SLC38A9 is a component of the lysosomal amino acid sensing machinery that controls mTORC1.

Rebsamen M, Pochini L, Stasyk T, de Araújo ME, Galluccio M, Kandasamy RK, Snijder B, Fauster A, Rudashevskaya EL, Bruckner M, Scorzoni S, Filipek PA, Huber KV, Bigenzahn JW, Heinz LX, Kraft C, Bennett KL, Indiveri C, Huber LA, Superti-Furga G.

Nature. 2015 Mar 26;519(7544):477-81. doi: 10.1038/nature14107. Epub 2015 Jan 7.

31.

The solute carrier SLC35F2 enables YM155-mediated DNA damage toxicity.

Winter GE, Radic B, Mayor-Ruiz C, Blomen VA, Trefzer C, Kandasamy RK, Huber KVM, Gridling M, Chen D, Klampfl T, Kralovics R, Kubicek S, Fernandez-Capetillo O, Brummelkamp TR, Superti-Furga G.

Nat Chem Biol. 2014 Sep;10(9):768-773. doi: 10.1038/nchembio.1590. Epub 2014 Jul 27.

32.

Evaluating the promiscuous nature of tyrosine kinase inhibitors assessed in A431 epidermoid carcinoma cells by both chemical- and phosphoproteomics.

Giansanti P, Preisinger C, Huber KV, Gridling M, Superti-Furga G, Bennett KL, Heck AJ.

ACS Chem Biol. 2014 Jul 18;9(7):1490-8. doi: 10.1021/cb500116c. Epub 2014 May 14.

PMID:
24804581
33.

Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy.

Huber KV, Salah E, Radic B, Gridling M, Elkins JM, Stukalov A, Jemth AS, Göktürk C, Sanjiv K, Strömberg K, Pham T, Berglund UW, Colinge J, Bennett KL, Loizou JI, Helleday T, Knapp S, Superti-Furga G.

Nature. 2014 Apr 10;508(7495):222-7. doi: 10.1038/nature13194. Epub 2014 Apr 2.

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