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Items: 8

1.

Privileged Structures and Polypharmacology within and between Protein Families.

Meyers J, Chessum NEA, Ali S, Mok NY, Wilding B, Pasqua AE, Rowlands M, Tucker MJ, Evans LE, Rye CS, O'Fee L, Le Bihan YV, Burke R, Carter M, Workman P, Blagg J, Brown N, van Montfort RLM, Jones K, Cheeseman MD.

ACS Med Chem Lett. 2018 Nov 16;9(12):1199-1204. doi: 10.1021/acsmedchemlett.8b00364. eCollection 2018 Dec 13.

2.

HSF1 Is Essential for Myeloma Cell Survival and A Promising Therapeutic Target.

Fok JHL, Hedayat S, Zhang L, Aronson LI, Mirabella F, Pawlyn C, Bright MD, Wardell CP, Keats JJ, De Billy E, Rye CS, Chessum NEA, Jones K, Morgan GJ, Eccles SA, Workman P, Davies FE.

Clin Cancer Res. 2018 May 15;24(10):2395-2407. doi: 10.1158/1078-0432.CCR-17-1594. Epub 2018 Feb 1.

3.

Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).

Chessum NEA, Sharp SY, Caldwell JJ, Pasqua AE, Wilding B, Colombano G, Collins I, Ozer B, Richards M, Rowlands M, Stubbs M, Burke R, McAndrew PC, Clarke PA, Workman P, Cheeseman MD, Jones K.

J Med Chem. 2018 Feb 8;61(3):918-933. doi: 10.1021/acs.jmedchem.7b01406. Epub 2018 Jan 5.

4.

Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.

Cheeseman MD, Chessum NE, Rye CS, Pasqua AE, Tucker MJ, Wilding B, Evans LE, Lepri S, Richards M, Sharp SY, Ali S, Rowlands M, O'Fee L, Miah A, Hayes A, Henley AT, Powers M, Te Poele R, De Billy E, Pellegrino L, Raynaud F, Burke R, van Montfort RL, Eccles SA, Workman P, Jones K.

J Med Chem. 2017 Jan 12;60(1):180-201. doi: 10.1021/acs.jmedchem.6b01055. Epub 2016 Dec 22.

5.

Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9.

Rye CS, Chessum NE, Lamont S, Pike KG, Faulder P, Demeritt J, Kemmitt P, Tucker J, Zani L, Cheeseman MD, Isaac R, Goodwin L, Boros J, Raynaud F, Hayes A, Henley AT, de Billy E, Lynch CJ, Sharp SY, Te Poele R, Fee LO, Foote KM, Green S, Workman P, Jones K.

Medchemcomm. 2016 Aug 1;7(8):1580-1586. Epub 2016 Jun 13.

6.

A model β-sheet interaction and thermodynamic analysis of β-strand mimetics.

Robinson CW, Rye CS, Chessum NE, Jones K.

Org Biomol Chem. 2015 Jul 21;13(27):7402-7. doi: 10.1039/c5ob00886g.

PMID:
26088610
7.

Synthesis and in vivo evaluation of bicyclic gababutins.

Blakemore DC, Bryans JS, Carnell P, Carr CL, Chessum NE, Field MJ, Kinsella N, Osborne SA, Warren AN, Williams SC.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):461-4. doi: 10.1016/j.bmcl.2009.11.118. Epub 2009 Nov 27.

PMID:
20005103
8.

Synthesis and in vivo evaluation of 3-substituted gababutins.

Blakemore DC, Bryans JS, Carnell P, Chessum NE, Field MJ, Kinsella N, Kinsora JK, Osborne SA, Williams SC.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):362-5. doi: 10.1016/j.bmcl.2009.10.089. Epub 2009 Oct 25.

PMID:
19897364

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