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Kinetic Optimization of Lysine-Targeting Covalent Inhibitors of HSP72.

Pettinger J, Carter M, Jones K, Cheeseman MD.

J Med Chem. 2019 Nov 14. doi: 10.1021/acs.jmedchem.9b01709. [Epub ahead of print]


Correction: Pleiotropic Impacts of Macrophage and Microglial Deficiency on Development in Rats with Targeted Mutation of the Csf1r Locus.

Pridans C, Raper A, Davis GM, Alves J, Sauter KA, Lefevre L, Regan T, Meek S, Sutherland L, Thomson AJ, Clohisey S, Bush SJ, Rojo R, Lisowski ZM, Wallace R, Grabert K, Upton KR, Tsai YT, Brown D, Smith LB, Summers KM, Mabbott NA, Piccardo P, Cheeseman MT, Burdon T, Hume DA.

J Immunol. 2019 Jun 1;202(11):3334-3335. doi: 10.4049/jimmunol.1900420. Epub 2019 Apr 26. No abstract available.


Role of ectodysplasin signalling in middle ear and nasal pathology in rat and mouse models of hypohidrotic ectodermal dysplasia.

Del-Pozo J, MacIntyre N, Azar A, Headon D, Schneider P, Cheeseman M.

Dis Model Mech. 2019 Apr 25;12(4). pii: dmm037804. doi: 10.1242/dmm.037804.


Chronic otitis media is initiated by a bulla cavitation defect in the FBXO11 mouse model.

Del-Pozo J, MacIntyre N, Azar A, Glover J, Milne E, Cheeseman M.

Dis Model Mech. 2019 Mar 21;12(3). pii: dmm038315. doi: 10.1242/dmm.038315.


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.


Reflections on PPI from the 'Action on Living Well: Asking You' advisory network of people with dementia and carers as part of the IDEAL study.

Litherland R, Burton J, Cheeseman M, Campbell D, Hawkins M, Hawkins T, Oliver K, Scott D, Ward J, Nelis SM, Quinn C, Victor C, Clare L.

Dementia (London). 2018 Nov;17(8):1035-1044. doi: 10.1177/1471301218789309.


Pleiotropic Impacts of Macrophage and Microglial Deficiency on Development in Rats with Targeted Mutation of the Csf1r Locus.

Pridans C, Raper A, Davis GM, Alves J, Sauter KA, Lefevre L, Regan T, Meek S, Sutherland L, Thomson AJ, Clohisey S, Bush SJ, Rojo R, Lisowski ZM, Wallace R, Grabert K, Upton KR, Tsai YT, Brown D, Smith LB, Summers KM, Mabbott NA, Piccardo P, Cheeseman MT, Burdon T, Hume DA.

J Immunol. 2018 Nov 1;201(9):2683-2699. doi: 10.4049/jimmunol.1701783. Epub 2018 Sep 24. Erratum in: J Immunol. 2019 Jun 1;202(11):3334-3335.


Loss of the homeostatic protein BPIFA1, leads to exacerbation of otitis media severity in the Junbo mouse model.

Mulay A, Hood DW, Williams D, Russell C, Brown SDM, Bingle L, Cheeseman M, Bingle CD.

Sci Rep. 2018 Feb 15;8(1):3128. doi: 10.1038/s41598-018-21166-7.


Macrophage colony-stimulating factor increases hepatic macrophage content, liver growth, and lipid accumulation in neonatal rats.

Pridans C, Sauter KA, Irvine KM, Davis GM, Lefevre L, Raper A, Rojo R, Nirmal AJ, Beard P, Cheeseman M, Hume DA.

Am J Physiol Gastrointest Liver Physiol. 2018 Mar 1;314(3):G388-G398. doi: 10.1152/ajpgi.00343.2017. Epub 2017 Dec 21.


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.


Understanding the aetiology and resolution of chronic otitis media from animal and human studies.

Bhutta MF, Thornton RB, Kirkham LS, Kerschner JE, Cheeseman MT.

Dis Model Mech. 2017 Nov 1;10(11):1289-1300. doi: 10.1242/dmm.029983. Review.


Lysine-Targeting Covalent Inhibitors.

Pettinger J, Jones K, Cheeseman MD.

Angew Chem Int Ed Engl. 2017 Nov 27;56(48):15200-15209. doi: 10.1002/anie.201707630. Epub 2017 Oct 27. Review.


Targeting secondary protein complexes in drug discovery: studying the druggability and chemical biology of the HSP70/BAG1 complex.

Evans LE, Jones K, Cheeseman MD.

Chem Commun (Camb). 2017 May 4;53(37):5167-5170. doi: 10.1039/c7cc01376k.


Non-Typeable Haemophilus influenzae Infection of the Junbo Mouse.

Cheeseman MT, Hood DW.

Curr Protoc Mouse Biol. 2017 Mar 2;7(1):29-46. doi: 10.1002/cpmo.24.


An Irreversible Inhibitor of HSP72 that Unexpectedly Targets Lysine-56.

Pettinger J, Le Bihan YV, Widya M, van Montfort RL, Jones K, Cheeseman MD.

Angew Chem Int Ed Engl. 2017 Mar 20;56(13):3536-3540. doi: 10.1002/anie.201611907. Epub 2017 Feb 22.


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.


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.


A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms.

Jones AM, Westwood IM, Osborne JD, Matthews TP, Cheeseman MD, Rowlands MG, Jeganathan F, Burke R, Lee D, Kadi N, Liu M, Richards M, McAndrew C, Yahya N, Dobson SE, Jones K, Workman P, Collins I, van Montfort RL.

Sci Rep. 2016 Oct 6;6:34701. doi: 10.1038/srep34701.


Novel gene function revealed by mouse mutagenesis screens for models of age-related disease.

Potter PK, Bowl MR, Jeyarajan P, Wisby L, Blease A, Goldsworthy ME, Simon MM, Greenaway S, Michel V, Barnard A, Aguilar C, Agnew T, Banks G, Blake A, Chessum L, Dorning J, Falcone S, Goosey L, Harris S, Haynes A, Heise I, Hillier R, Hough T, Hoslin A, Hutchison M, King R, Kumar S, Lad HV, Law G, MacLaren RE, Morse S, Nicol T, Parker A, Pickford K, Sethi S, Starbuck B, Stelma F, Cheeseman M, Cross SH, Foster RG, Jackson IJ, Peirson SN, Thakker RV, Vincent T, Scudamore C, Wells S, El-Amraoui A, Petit C, Acevedo-Arozena A, Nolan PM, Cox R, Mallon AM, Brown SD.

Nat Commun. 2016 Aug 18;7:12444. doi: 10.1038/ncomms12444.


Ectodysplasin signalling deficiency in mouse models of hypohidrotic ectodermal dysplasia leads to middle ear and nasal pathology.

Azar A, Piccinelli C, Brown H, Headon D, Cheeseman M.

Hum Mol Genet. 2016 Aug 15;25(16):3564-3577. doi: 10.1093/hmg/ddw202. Epub 2016 Jul 4.


European Court of Human Rights Rulings in Home Birth Set to Cause Trouble for the Future: A Review of Two Cases.

Chen CY, Cheeseman M.

Med Law Rev. 2017 Feb 1;25(1):115-125. doi: 10.1093/medlaw/fwv040.


A genome-wide association scan implicates DCHS2, RUNX2, GLI3, PAX1 and EDAR in human facial variation.

Adhikari K, Fuentes-Guajardo M, Quinto-Sánchez M, Mendoza-Revilla J, Camilo Chacón-Duque J, Acuña-Alonzo V, Jaramillo C, Arias W, Lozano RB, Pérez GM, Gómez-Valdés J, Villamil-Ramírez H, Hunemeier T, Ramallo V, Silva de Cerqueira CC, Hurtado M, Villegas V, Granja V, Gallo C, Poletti G, Schuler-Faccini L, Salzano FM, Bortolini MC, Canizales-Quinteros S, Cheeseman M, Rosique J, Bedoya G, Rothhammer F, Headon D, González-José R, Balding D, Ruiz-Linares A.

Nat Commun. 2016 May 19;7:11616. doi: 10.1038/ncomms11616.


Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70.

Cheeseman MD, Westwood IM, Barbeau O, Rowlands M, Dobson S, Jones AM, Jeganathan F, Burke R, Kadi N, Workman P, Collins I, van Montfort RL, Jones K.

J Med Chem. 2016 May 26;59(10):4625-36. doi: 10.1021/acs.jmedchem.5b02001. Epub 2016 May 11.


On-call hospital pharmacy services in NHS England: service provision and documentation of medicines advice calls.

Cheeseman MP, Rutter P.

Eur J Hosp Pharm. 2016 Jan;23(1):11-15. doi: 10.1136/ejhpharm-2015-000679. Epub 2015 Jun 18.


A new model for non-typeable Haemophilus influenzae middle ear infection in the Junbo mutant mouse.

Hood D, Moxon R, Purnell T, Richter C, Williams D, Azar A, Crompton M, Wells S, Fray M, Brown SD, Cheeseman MT.

Dis Model Mech. 2016 Jan;9(1):69-79. doi: 10.1242/dmm.021659. Epub 2015 Nov 26.


Investigating Apoptozole as a Chemical Probe for HSP70 Inhibition.

Evans LE, Cheeseman MD, Yahya N, Jones K.

PLoS One. 2015 Oct 12;10(10):e0140006. doi: 10.1371/journal.pone.0140006. eCollection 2015.


A genome-wide association study identifies multiple loci for variation in human ear morphology.

Adhikari K, Reales G, Smith AJ, Konka E, Palmen J, Quinto-Sanchez M, Acuña-Alonzo V, Jaramillo C, Arias W, Fuentes M, Pizarro M, Barquera Lozano R, Macín Pérez G, Gómez-Valdés J, Villamil-Ramírez H, Hunemeier T, Ramallo V, Silva de Cerqueira CC, Hurtado M, Villegas V, Granja V, Gallo C, Poletti G, Schuler-Faccini L, Salzano FM, Bortolini MC, Canizales-Quinteros S, Rothhammer F, Bedoya G, Calderón R, Rosique J, Cheeseman M, Bhutta MF, Humphries SE, Gonzalez-José R, Headon D, Balding D, Ruiz-Linares A.

Nat Commun. 2015 Jun 24;6:7500. doi: 10.1038/ncomms8500.


Targeting the PPM1D phenotype; 2,4-bisarylthiazoles cause highly selective apoptosis in PPM1D amplified cell-lines.

Cheeseman MD, Faisal A, Rayter S, Barbeau OR, Kalusa A, Westlake M, Burke R, Swan M, van Montfort R, Linardopoulos S, Jones K.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3469-74. doi: 10.1016/j.bmcl.2014.05.067. Epub 2014 May 29.


Myringotomy in the Junbo mouse model of chronic otitis media alleviates inflammation and cellular hypoxia.

Bhutta MF, Cheeseman MT, Brown SD.

Laryngoscope. 2014 Sep;124(9):E377-83. doi: 10.1002/lary.24698. Epub 2014 May 30.


Surveying the Down syndrome mouse model resource identifies critical regions responsible for chronic otitis media.

Bhutta MF, Cheeseman MT, Herault Y, Yu YE, Brown SD.

Mamm Genome. 2013 Dec;24(11-12):439-45. doi: 10.1007/s00335-013-9475-x. Epub 2013 Sep 26.


Panel 4: Recent advances in otitis media in molecular biology, biochemistry, genetics, and animal models.

Li JD, Hermansson A, Ryan AF, Bakaletz LO, Brown SD, Cheeseman MT, Juhn SK, Jung TT, Lim DJ, Lim JH, Lin J, Moon SK, Post JC.

Otolaryngol Head Neck Surg. 2013 Apr;148(4 Suppl):E52-63. doi: 10.1177/0194599813479772. Review.


Otitis media in the Tgif knockout mouse implicates TGFβ signalling in chronic middle ear inflammatory disease.

Tateossian H, Morse S, Parker A, Mburu P, Warr N, Acevedo-Arozena A, Cheeseman M, Wells S, Brown SD.

Hum Mol Genet. 2013 Jul 1;22(13):2553-65. doi: 10.1093/hmg/ddt103. Epub 2013 Mar 3.


A mouse model for osseous heteroplasia.

Cheeseman MT, Vowell K, Hough TA, Jones L, Pathak P, Tyrer HE, Kelly M, Cox R, Warren MV, Peters J.

PLoS One. 2012;7(12):e51835. doi: 10.1371/journal.pone.0051835. Epub 2012 Dec 19.


A mouse with an N-Ethyl-N-nitrosourea (ENU) Induced Trp589Arg Galnt3 mutation represents a model for hyperphosphataemic familial tumoural calcinosis.

Esapa CT, Head RA, Jeyabalan J, Evans H, Hough TA, Cheeseman MT, McNally EG, Carr AJ, Thomas GP, Brown MA, Croucher PI, Brown SD, Cox RD, Thakker RV.

PLoS One. 2012;7(8):e43205. doi: 10.1371/journal.pone.0043205. Epub 2012 Aug 13.


N-N bond-forming cyclization for the one-pot synthesis of N-aryl[3,4-d]pyrazolopyrimidines.

Evans LE, Cheeseman MD, Jones K.

Org Lett. 2012 Jul 6;14(13):3546-9. doi: 10.1021/ol301561a. Epub 2012 Jun 26.


KATNAL1 regulation of sertoli cell microtubule dynamics is essential for spermiogenesis and male fertility.

Smith LB, Milne L, Nelson N, Eddie S, Brown P, Atanassova N, O'Bryan MK, O'Donnell L, Rhodes D, Wells S, Napper D, Nolan P, Lalanne Z, Cheeseman M, Peters J.

PLoS Genet. 2012;8(5):e1002697. doi: 10.1371/journal.pgen.1002697. Epub 2012 May 24.


EVI1 acts as an inducible negative-feedback regulator of NF-κB by inhibiting p65 acetylation.

Xu X, Woo CH, Steere RR, Lee BC, Huang Y, Wu J, Pang J, Lim JH, Xu H, Zhang W, Konduru AS, Yan C, Cheeseman MT, Brown SD, Li JD.

J Immunol. 2012 Jun 15;188(12):6371-80. doi: 10.4049/jimmunol.1103527. Epub 2012 May 11.


Artificial food color additives and child behavior.

Cheeseman MA.

Environ Health Perspect. 2012 Jan;120(1):A15-6; author reply A17. doi: 10.1289/ehp.1104409. No abstract available.


Myofibrillar myopathy caused by a mutation in the motor domain of mouse MyHC IIb.

Kurapati R, McKenna C, Lindqvist J, Williams D, Simon M, LeProust E, Baker J, Cheeseman M, Carroll N, Denny P, Laval S, Lochmüller H, Ochala J, Blanco G.

Hum Mol Genet. 2012 Apr 15;21(8):1706-24. doi: 10.1093/hmg/ddr605. Epub 2011 Dec 23.


Static respiratory cilia associated with mutations in Dnahc11/DNAH11: a mouse model of PCD.

Lucas JS, Adam EC, Goggin PM, Jackson CL, Powles-Glover N, Patel SH, Humphreys J, Fray MD, Falconnet E, Blouin JL, Cheeseman MT, Bartoloni L, Norris DP, Lackie PM.

Hum Mutat. 2012 Mar;33(3):495-503. doi: 10.1002/humu.22001. Epub 2011 Dec 29.


Oxr1 is essential for protection against oxidative stress-induced neurodegeneration.

Oliver PL, Finelli MJ, Edwards B, Bitoun E, Butts DL, Becker EB, Cheeseman MT, Davies B, Davies KE.

PLoS Genet. 2011 Oct;7(10):e1002338. doi: 10.1371/journal.pgen.1002338. Epub 2011 Oct 20.


HIF-VEGF pathways are critical for chronic otitis media in Junbo and Jeff mouse mutants.

Cheeseman MT, Tyrer HE, Williams D, Hough TA, Pathak P, Romero MR, Hilton H, Bali S, Parker A, Vizor L, Purnell T, Vowell K, Wells S, Bhutta MF, Potter PK, Brown SD.

PLoS Genet. 2011 Oct;7(10):e1002336. doi: 10.1371/journal.pgen.1002336. Epub 2011 Oct 20.


A mouse model for spondyloepiphyseal dysplasia congenita with secondary osteoarthritis due to a Col2a1 mutation.

Esapa CT, Hough TA, Testori S, Head RA, Crane EA, Chan CP, Evans H, Bassett JH, Tylzanowski P, McNally EG, Carr AJ, Boyde A, Howell PG, Clark A, Williams GR, Brown MA, Croucher PI, Nesbit MA, Brown SD, Cox RD, Cheeseman MT, Thakker RV.

J Bone Miner Res. 2012 Feb;27(2):413-28. doi: 10.1002/jbmr.547.


Asymmetric synthesis of chiral δ-lactones containing multiple contiguous stereocenters.

Peed J, Domínguez IP, Davies IR, Cheeseman M, Taylor JE, Kociok-Köhn G, Bull SD.

Org Lett. 2011 Jul 15;13(14):3592-5. doi: 10.1021/ol2012023. Epub 2011 Jun 14.


Minor abnormalities of testis development in mice lacking the gene encoding the MAPK signalling component, MAP3K1.

Warr N, Bogani D, Siggers P, Brixey R, Tateossian H, Dopplapudi A, Wells S, Cheeseman M, Xia Y, Ostrer H, Greenfield A.

PLoS One. 2011 May 3;6(5):e19572. doi: 10.1371/journal.pone.0019572.


Unraveling the genetics of otitis media: from mouse to human and back again.

Rye MS, Bhutta MF, Cheeseman MT, Burgner D, Blackwell JM, Brown SD, Jamieson SE.

Mamm Genome. 2011 Feb;22(1-2):66-82. doi: 10.1007/s00335-010-9295-1. Epub 2010 Nov 25. Review.


Haploinsufficiency of the murine Col3a1 locus causes aortic dissection: a novel model of the vascular type of Ehlers-Danlos syndrome.

Smith LB, Hadoke PW, Dyer E, Denvir MA, Brownstein D, Miller E, Nelson N, Wells S, Cheeseman M, Greenfield A.

Cardiovasc Res. 2011 Apr 1;90(1):182-90. doi: 10.1093/cvr/cvq356. Epub 2010 Nov 10.


Oto-endoscopy: a reliable and validated technique for phenotyping otitis media in the mouse.

Bhutta MF, Hedge EA, Parker A, Cheeseman MT, Brown SD.

Hear Res. 2011 Feb;272(1-2):5-12. doi: 10.1016/j.heares.2010.09.002. Epub 2010 Sep 24.


Xrcc2 modulates spontaneous and radiation-induced tumorigenesis in Apcmin/+ mice.

Haines JW, Coster MR, Adam J, Cheeseman M, Ainsbury EA, Thacker J, Bouffler SD.

Mol Cancer Res. 2010 Sep;8(9):1227-33. doi: 10.1158/1541-7786.MCR-10-0089. Epub 2010 Jul 29.


A mutation in the mitochondrial fission gene Dnm1l leads to cardiomyopathy.

Ashrafian H, Docherty L, Leo V, Towlson C, Neilan M, Steeples V, Lygate CA, Hough T, Townsend S, Williams D, Wells S, Norris D, Glyn-Jones S, Land J, Barbaric I, Lalanne Z, Denny P, Szumska D, Bhattacharya S, Griffin JL, Hargreaves I, Fernandez-Fuentes N, Cheeseman M, Watkins H, Dear TN.

PLoS Genet. 2010 Jun 24;6(6):e1001000. doi: 10.1371/journal.pgen.1001000.

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