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Items: 33

1.

Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells.

Foulkes DM, Byrne DP, Yeung W, Shrestha S, Bailey FP, Ferries S, Eyers CE, Keeshan K, Wells C, Drewry DH, Zuercher WJ, Kannan N, Eyers PA.

Sci Signal. 2018 Sep 25;11(549). pii: eaat7951. doi: 10.1126/scisignal.aat7951.

PMID:
30254057
2.

In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases.

Wells CI, Kapadia NR, Couñago RM, Drewry DH.

Medchemcomm. 2017 Dec 8;9(1):44-66. doi: 10.1039/c7md00510e. eCollection 2018 Jan 1. Review.

PMID:
30108900
3.

GW779439X and Its Pyrazolopyridazine Derivatives Inhibit the Serine/Threonine Kinase Stk1 and Act As Antibiotic Adjuvants against β-Lactam-Resistant Staphylococcus aureus.

Schaenzer AJ, Wlodarchak N, Drewry DH, Zuercher WJ, Rose WE, Ferrer CA, Sauer JD, Striker R.

ACS Infect Dis. 2018 Aug 15. doi: 10.1021/acsinfecdis.8b00136. [Epub ahead of print]

PMID:
30059625
4.

New tools for carbohydrate sulfation analysis: heparan sulfate 2-O-sulfotransferase (HS2ST) is a target for small-molecule protein kinase inhibitors.

Byrne DP, Li Y, Ramakrishnan K, Barsukov IL, Yates EA, Eyers CE, Papy-Garcia D, Chantepie S, Pagadala V, Liu J, Wells C, Drewry DH, Zuercher WJ, Berry NG, Fernig DG, Eyers PA.

Biochem J. 2018 Aug 14;475(15):2417-2433. doi: 10.1042/BCJ20180265.

5.

New tools for evaluating protein tyrosine sulfation: tyrosylprotein sulfotransferases (TPSTs) are novel targets for RAF protein kinase inhibitors.

Byrne DP, Li Y, Ngamlert P, Ramakrishnan K, Eyers CE, Wells C, Drewry DH, Zuercher WJ, Berry NG, Fernig DG, Eyers PA.

Biochem J. 2018 Aug 14;475(15):2435-2455. doi: 10.1042/BCJ20180266.

6.

1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors.

Asquith CRM, Godoi PH, Couñago RM, Laitinen T, Scott JW, Langendorf CG, Oakhill JS, Drewry DH, Zuercher WJ, Koutentis PA, Willson TM, Kalogirou AS.

Molecules. 2018 May 19;23(5). pii: E1221. doi: 10.3390/molecules23051221.

7.

Donated chemical probes for open science.

Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A.

Elife. 2018 Apr 20;7. pii: e34311. doi: 10.7554/eLife.34311.

8.

An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model.

Price DJ, Drewry DH, Schaller LT, Thompson BD, Reid PR, Maloney PR, Liang X, Banker P, Buckholz RG, Selley PK, McDonald OB, Smith JL, Shearer TW, Cox RF, Williams SP, Reid RA, Tacconi S, Faggioni F, Piubelli C, Sartori I, Tessari M, Wang TY.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1958-1963. doi: 10.1016/j.bmcl.2018.03.034. Epub 2018 Apr 5.

PMID:
29653895
9.

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.

10.

A screen for kinase inhibitors identifies antimicrobial imidazopyridine aminofurazans as specific inhibitors of the Listeria monocytogenes PASTA kinase PrkA.

Schaenzer AJ, Wlodarchak N, Drewry DH, Zuercher WJ, Rose WE, Striker R, Sauer JD.

J Biol Chem. 2017 Oct 13;292(41):17037-17045. doi: 10.1074/jbc.M117.808600. Epub 2017 Aug 16.

11.

Novel application of the published kinase inhibitor set to identify therapeutic targets and pathways in triple negative breast cancer subtypes.

Matossian MD, Elliott S, Hoang VT, Burks HE, Phamduy TB, Chrisey DB, Zuercher WJ, Drewry DH, Wells C, Collins-Burow B, Burow ME.

PLoS One. 2017 Aug 3;12(8):e0177802. doi: 10.1371/journal.pone.0177802. eCollection 2017.

12.

Progress towards a public chemogenomic set for protein kinases and a call for contributions.

Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, Luecking U, Michaelides M, Müller S, Muratov E, Denny RA, Saikatendu KS, Treiber DK, Zuercher WJ, Willson TM.

PLoS One. 2017 Aug 2;12(8):e0181585. doi: 10.1371/journal.pone.0181585. eCollection 2017.

13.

EGFR inhibitors identified as a potential treatment for chordoma in a focused compound screen.

Scheipl S, Barnard M, Cottone L, Jorgensen M, Drewry DH, Zuercher WJ, Turlais F, Ye H, Leite AP, Smith JA, Leithner A, Möller P, Brüderlein S, Guppy N, Amary F, Tirabosco R, Strauss SJ, Pillay N, Flanagan AM.

J Pathol. 2016 Jul;239(3):320-34. doi: 10.1002/path.4729. Epub 2016 May 31.

14.

Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni.

Long T, Neitz RJ, Beasley R, Kalyanaraman C, Suzuki BM, Jacobson MP, Dissous C, McKerrow JH, Drewry DH, Zuercher WJ, Singh R, Caffrey CR.

PLoS Negl Trop Dis. 2016 Jan 11;10(1):e0004356. doi: 10.1371/journal.pntd.0004356. eCollection 2016 Jan.

15.

Comprehensive characterization of the Published Kinase Inhibitor Set.

Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S, Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, Teicher BA, Kunkel M, Polley E, Lackey KE, Atkinson FL, Overington JP, Bamborough P, Müller S, Price DJ, Willson TM, Drewry DH, Knapp S, Zuercher WJ.

Nat Biotechnol. 2016 Jan;34(1):95-103. doi: 10.1038/nbt.3374. Epub 2015 Oct 26.

PMID:
26501955
16.

Rational Polypharmacology: Systematically Identifying and Engaging Multiple Drug Targets To Promote Axon Growth.

Al-Ali H, Lee DH, Danzi MC, Nassif H, Gautam P, Wennerberg K, Zuercher B, Drewry DH, Lee JK, Lemmon VP, Bixby JL.

ACS Chem Biol. 2015 Aug 21;10(8):1939-51. doi: 10.1021/acschembio.5b00289. Epub 2015 Jun 24.

17.

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. 2016 Feb 25;59(4):1425-39. doi: 10.1021/acs.jmedchem.5b00256. Epub 2015 Apr 30.

PMID:
25856009
18.

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.

19.

New compound sets identified from high throughput phenotypic screening against three kinetoplastid parasites: an open resource.

Peña I, Pilar Manzano M, Cantizani J, Kessler A, Alonso-Padilla J, Bardera AI, Alvarez E, Colmenarejo G, Cotillo I, Roquero I, de Dios-Anton F, Barroso V, Rodriguez A, Gray DW, Navarro M, Kumar V, Sherstnev A, Drewry DH, Brown JR, Fiandor JM, Julio Martin J.

Sci Rep. 2015 Mar 5;5:8771. doi: 10.1038/srep08771.

20.

Seeding collaborations to advance kinase science with the GSK Published Kinase Inhibitor Set (PKIS).

Drewry DH, Willson TM, Zuercher WJ.

Curr Top Med Chem. 2014;14(3):340-2. Review.

21.

Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays.

Dranchak P, MacArthur R, Guha R, Zuercher WJ, Drewry DH, Auld DS, Inglese J.

PLoS One. 2013;8(3):e57888. doi: 10.1371/journal.pone.0057888. Epub 2013 Mar 7.

22.

A public-private partnership to unlock the untargeted kinome.

Knapp S, Arruda P, Blagg J, Burley S, Drewry DH, Edwards A, Fabbro D, Gillespie P, Gray NS, Kuster B, Lackey KE, Mazzafera P, Tomkinson NC, Willson TM, Workman P, Zuercher WJ.

Nat Chem Biol. 2013 Jan;9(1):3-6. doi: 10.1038/nchembio.1113. No abstract available.

PMID:
23238671
23.

Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.

Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA, Huffman WF, Koretke-Brown KK, Lai ZV, McDonald OB, Nakamura H, Newlander KA, Oleykowski CA, Parrish CA, Patrick DR, Plant R, Sarpong MA, Sasaki K, Schmidt SJ, Silva DJ, Sutton D, Tang J, Thompson CS, Tummino PJ, Wang JC, Xiang H, Yang J, Dhanak D.

J Med Chem. 2010 May 27;53(10):3973-4001. doi: 10.1021/jm901870q.

PMID:
20420387
24.

Enhancements of screening collections to address areas of unmet medical need: an industry perspective.

Drewry DH, Macarron R.

Curr Opin Chem Biol. 2010 Jun;14(3):289-98. doi: 10.1016/j.cbpa.2010.03.024. Epub 2010 Apr 21. Review.

PMID:
20413343
25.

Discovery of thiophene inhibitors of polo-like kinase.

Emmitte KA, Andrews CW, Badiang JG, Davis-Ward RG, Dickson HD, Drewry DH, Emerson HK, Epperly AH, Hassler DF, Knick VB, Kuntz KW, Lansing TJ, Linn JA, Mook RA Jr, Nailor KE, Salovich JM, Spehar GM, Cheung M.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):1018-21. doi: 10.1016/j.bmcl.2008.11.041. Epub 2008 Nov 18.

PMID:
19097784
26.

Kinase-targeted library design through the application of the PharmPrint methodology.

Deanda F, Stewart EL, Reno MJ, Drewry DH.

J Chem Inf Model. 2008 Dec;48(12):2395-403. doi: 10.1021/ci800276t.

PMID:
19053525
27.

Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines.

Wiethe RW, Stewart EL, Drewry DH, Gray DW, Mehbob A, Hoekstra WJ.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3777-9. Epub 2006 May 5.

PMID:
16678409
28.

High-throughput manual parallel synthesis using SynPhase crowns and lanterns.

Gerritz SW, Norman MH, Barger LA, Berman J, Bigham EC, Bishop MJ, Drewry DH, Garrison DT, Heyer D, Hodson SJ, Kakel JA, Linn JA, Marron BE, Nanthakumar SS, Navas FJ 3rd.

J Comb Chem. 2003 Mar-Apr;5(2):110-7.

PMID:
12625700
29.

Optimization of focused chemical libraries using recursive partitioning.

Rusinko A 3rd, Young SS, Drewry DH, Gerritz SW.

Comb Chem High Throughput Screen. 2002 Mar;5(2):125-33.

PMID:
11966421
30.

2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.

Navas F 3rd, Bishop MJ, Garrison DT, Hodson SJ, Speake JD, Bigham EC, Drewry DH, Saussy DL, Liacos JH, Irving PE, Gobel MJ.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):575-9.

PMID:
11844675
31.

2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.

Henke BR, Drewry DH, Jones SA, Stewart EL, Weaver SL, Wiethe RW.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1939-42.

PMID:
11459665
32.

Solid-supported reagents in organic synthesis.

Drewry DH, Coe DM, Poon S.

Med Res Rev. 1999 Mar;19(2):97-148. Review.

PMID:
10189175

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