Paul Stupple

Dr

19972020
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Research Output 1997 2019

2019

Fragment screening for a protein-protein interaction inhibitor to WDR5

Dennis, M. L., Morrow, B., Dolezal, O., Cuzzupe, A. N., Stupple, A., Newman, J., Bentley, J., Hattarki, M., Nuttall, S. D., Foitzik, R., Street, I. P., Stupple, P. A., Monahan, B. J. & Peat, T. S., 1 Nov 2019, In : Structural Dynamics. 6, 6, 20 p., 064701.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
1 Citation (Scopus)

Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma

AbuHammad, S., Cullinane, C., Martin, C., Bacolas, Z., Ward, T., Chen, H., Slater, A., Ardley, K., Kirby, L., Chan, K. T., Brajanovski, N., Smith, L. K., Rao, A. D., Lelliott, E. J., Kleinschmidt, M., Vergara, I. A., Papenfuss, A. T., Lau, P., Ghosh, P., Haupt, S. & 12 others, Haupt, Y., Sanij, E., Poortinga, G., Pearson, R. B., Falk, H., Curtis, D. J., Stupple, P., Devlin, M., Street, I., Davies, M. A., McArthur, G. A. & Sheppard, K. E., 3 Sep 2019, In : Proceedings of the National Academy of Sciences of the United States of America. 116, 36, p. 17990-18000 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
2017
29 Citations (Scopus)

Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7

Swain, N. A., Batchelor, D., Beaudoin, S., Bechle, B. M., Bradley, P. A., Brown, A. D., Brown, B., Butcher, K. J., Butt, R. P., Chapman, M. L., Denton, S., Ellis, D., Galan, S. R. G., Gaulier, S. M., Greener, B. S., De Groot, M. J., Glossop, M. S., Gurrell, I. K., Hannam, J., Johnson, M. S. & 14 others, Lin, Z., Markworth, C. J., Marron, B. E., Millan, D. S., Nakagawa, S., Pike, A., Printzenhoff, D., Rawson, D. J., Ransley, S. J., Reister, S. M., Sasaki, K., Storer, R. I., Stupple, P. A. & West, C. W., 24 Aug 2017, In : Journal of Medicinal Chemistry. 60, 16, p. 7029-7042 14 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics

Pryde, D. C., Swain, N. A., Stupple, P. A., West, C. W., Marron, B., Markworth, C. J., Printzenhoff, D., Lin, Z., Cox, P. J., Suzuki, R., McMurray, S., Waldron, G. J., Payne, C. E., Warmus, J. S. & Chapman, M. L., 2017, In : MedChemComm. 8, 6, p. 1255-1267 13 p.

Research output: Contribution to journalArticleResearchpeer-review

2016
57 Citations (Scopus)

Subtype-selective small molecule inhibitors reveal a fundamental role for Nav1.7 in nociceptor electrogenesis, axonal conduction and presynaptic release

Alexandrou, A. J., Brown, A. R., Chapman, M. L., Estacion, M., Turner, J., Mis, M. A., Wilbrey, A., Payne, E. C., Gutteridge, A., Cox, P. J., Doyle, R., Printzenhoff, D., Lin, Z., Marron, B. E., West, C., Swain, N. A., Storer, R. I., Stupple, P. A., Castle, N. A., Hounshell, J. A. & 8 others, Rivara, M., Randall, A., Dib-Hajj, S. D., Krafte, D. S., Waxman, S. G., Patel, M. K., Butt, R. P. & Stevens, E. B., 1 Apr 2016, In : PLoS ONE. 11, 4, 22 p., e0152405.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
23 Citations (Scopus)

The Discovery of a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor (PF-06273340) for the Treatment of Pain

Skerratt, S. E., Andrews, M., Bagal, S. K., Bilsland, J., Brown, D., Bungay, P. J., Cole, S., Gibson, K. R., Jones, R., Morao, I., Nedderman, A., Omoto, K., Robinson, C., Ryckmans, T., Skinner, K., Stupple, P. & Waldron, G., 23 Nov 2016, In : Journal of Medicinal Chemistry. 59, 22, p. 10084-10099 16 p.

Research output: Contribution to journalArticleResearchpeer-review

2013
7 Citations (Scopus)

Non-benzimidazole containing inhibitors of respiratory syncytial virus

Pryde, D. C., Tran, T. D., Gardner, I., Bright, H., Stupple, P., Galan, S., Alsop, L., Watson, L., Middleton, D. S., Dayal, S., Platts, M., Murray, E. J., Parkinson, T. & Webster, R., 1 Feb 2013, In : Bioorganic and Medicinal Chemistry Letters. 23, 3, p. 827-833 7 p.

Research output: Contribution to journalArticleResearchpeer-review

116 Citations (Scopus)

Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels

McCormack, K., Santos, S., Chapman, M. L., Krafte, D. S., Marron, B. E., West, C. W., Krambis, M. J., Antonio, B. M., Zellmer, S. G., Printzenhoff, D., Padilla, K. M., Lin, Z., Wagoner, P. K., Swain, N. A., Stupple, P. A., De Groot, M., Butt, R. P. & Castle, N. A., 16 Jul 2013, In : Proceedings of the National Academy of Sciences. 110, 29

Research output: Contribution to journalArticleResearchpeer-review

Open Access
2012
26 Citations (Scopus)

Full efficacy with no CNS side-effects: Unachievable panacea or reality? DMPK considerations in design of drugs with limited brain penetration

Cole, S., Bagal, S. K., El-Kattan, A., Fenner, K., Hay, T., Kempshall, S., Lunn, G., Varma, M., Stupple, P. & Speed, W., Jan 2012, In : Xenobiotica. 42, 1, p. 11-27 17 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

2011
36 Citations (Scopus)

An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: The discovery of N -{(1 S)-1-(3-fluorophenyl)-3-[(3- endo)-3-(5-isobutyryl-2- methyl-4,5,6,7-tetrahydro-1 H -imidazo[4,5- c ]pyridin-1-yl)-8-azabicyclo[3.2.1] oct-8-yl]propyl}acetamide (PF-232798)

Stupple, P. A., Batchelor, D. V., Corless, M., Dorr, P. K., Ellis, D., Fenwick, D. R., Galan, S. R. G., Jones, R. M., Mason, H. J., Middleton, D. S., Perros, M., Perruccio, F., Platts, M. Y., Pryde, D. C., Rodrigues, D., Smith, N. N., Stephenson, P. T., Webster, R., Westby, M. & Wood, A., 13 Jan 2011, In : Journal of Medicinal Chemistry. 54, 1, p. 67-77 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Discovery and Development of Maraviroc and PF-232798: CCR5 Antagonists for the Treatment of HIV-1 Infection

Dorr, P. & Stupple, P., 20 Jun 2011, Antiviral Drugs: From Basic Discovery through Clinical Trials. Kazmierski, W. M. (ed.). Hoboken NJ USA: John Wiley & Sons, p. 117-136 20 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

2009
25 Citations (Scopus)

Pyrazole NNRTIs 1: Design and initial optimisation of a novel template

Mowbray, C. E., Burt, C., Corbau, R., Perros, M., Tran, I., Stupple, P. A., Webster, R. & Wood, A., 1 Oct 2009, In : Bioorganic and Medicinal Chemistry Letters. 19, 19, p. 5599-5602 4 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

Pyrazole NNRTIs 3: Optimisation of physicochemical properties

Mowbray, C. E., Corbau, R., Hawes, M., Jones, L. H., Mills, J. E., Perros, M., Selby, M. D., Stupple, P. A., Webster, R. & Wood, A., 1 Oct 2009, In : Bioorganic and Medicinal Chemistry Letters. 19, 19, p. 5603-5606 4 p.

Research output: Contribution to journalArticleResearchpeer-review

82 Citations (Scopus)

Pyrazole NNRTIs 4: Selection of UK-453,061 (lersivirine) as a Development Candidate

Mowbray, C. E., Burt, C., Corbau, R., Gayton, S., Hawes, M., Perros, M., Tran, I., Price, D. A., Quinton, F. J., Selby, M. D., Stupple, P. A., Webster, R. & Wood, A., 15 Oct 2009, In : Bioorganic and Medicinal Chemistry Letters. 19, 20, p. 5857-5860 4 p.

Research output: Contribution to journalArticleResearchpeer-review

2008
122 Citations (Scopus)

Organocatalytic asymmetric total synthesis of (R)-rolipram and formal synthesis of (3S,4R)-paroxetine

Hynes, P. S., Stupple, P. A. & Dixon, D. J., 3 Apr 2008, In : Organic Letters. 10, 7, p. 1389-1391 3 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Reactions involving metallocarbenes

Hodgson, D. M., Stupple, P. A. & Forbes, D. C., 1 Dec 2008, Second Supplements to the 2nd Edition of Rodd's Chemistry of Carbon Compounds: A Modern Comprehensive Treatise. Elsevier BV, Vol. 5. p. 65-99 35 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

2007
76 Citations (Scopus)

Organocatalytic diastereo- And enantioselective Michael addition reactions of 5-aryl-1,3-dioxolan-4-ones

Hynes, P. S., Stranges, D., Stupple, P. A., Guarna, A. & Dixon, D. J., 24 May 2007, In : Organic Letters. 9, 11, p. 2107-2110 4 p.

Research output: Contribution to journalArticleResearchpeer-review

2003
11 Citations (Scopus)

Enantioselective intramolecular 1,3-dipolar cycloadditions ofdiazocarbonyl-derived oxidopyryliums

Hodgson, D. M., Stupple, P. A. & Johnstone, C., 1 Dec 2003, In : ARKIVOC. 2003, 7, p. 49-58 10 p.

Research output: Contribution to journalArticleResearchpeer-review

2002
9 Citations (Scopus)

High throughput synthesis of functionalised 1,3-diones and subsequent heterocycle formation

Price, D. A., Gayton, S. & Stupple, P. A., 25 Jul 2002, In : Synlett. 7, p. 1170-1172 3 p.

Research output: Contribution to journalArticleResearchpeer-review

2001
288 Citations (Scopus)

Catalytic enantioselective rearrangements and cycloadditions involving ylides from diazo compounds

Hodgson, D. M., Pierard, F. Y. T. M. & Stupple, P. A., 1 Dec 2001, In : Chemical Society Reviews. 30, 1, p. 50-61 12 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

103 Citations (Scopus)

Development of dirhodium(II)-catalyzed generation and enantioselective 1,3-dipolar cycloaddition of carbonyl ylides

Hodgson, D. M., Stupple, P. A., Pierard, F. Y. T. M., Labande, A. H. & Johnstone, C., 15 Oct 2001, In : Chemistry - A European Journal. 7, 20, p. 4465-4476 12 p.

Research output: Contribution to journalArticleResearchpeer-review

1999
80 Citations (Scopus)

Efficient Rh(II) binaphthol phosphate catalysts for enantioselective intramolecular tandem carbonyl ylide formation-cycloaddition of α-diazo-β-keto esters

Hodgson, D. M., Stupple, P. A. & Johnstone, C., 7 Nov 1999, In : Chemical Communications. 21, p. 2185-2186 2 p.

Research output: Contribution to journalArticleResearchpeer-review

1997
9 Citations (Scopus)

Bicyclo[10.2.1]pentadecenone derivatives by free radical macrocyclisation

Robertson, J., Burrows, J. N. & Stupple, P. A., 27 Oct 1997, In : Tetrahedron. 53, 43, p. 14807-14820 14 p.

Research output: Contribution to journalArticleResearchpeer-review

85 Citations (Scopus)

Catalytic enantioselective tandem carbonyl ylide formation-cycloaddition

Hodgson, D. M., Stupple, P. A. & Johnstone, C., 8 Sep 1997, In : Tetrahedron Letters. 38, 36, p. 6471-6472 2 p.

Research output: Contribution to journalArticleResearchpeer-review