The York Research Database

Small molecule ERK5 kinase inhibitors paradoxically activate ERK5 signalling: be careful what you wish for...

Cook, S., Tucker, J. A. & Lochhead, P., 11 Sep 2020

Article in Biochemical Society transactions

Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors

Lochhead, P., Tucker, J. A., Tatum, N., Wang, J., Oxley, D., Kidger, A., Johnson, V., Cassidy, M., Gray, N., Noble, M. E. M. & Cook, S., 13 Mar 2020

Article in Nature Communications

Mechanism of homodimeric cytokine receptor activation and dysregulation by oncogenic mutations

Wilmes, S., Hafer, M., Vuorio, J., Tucker, J. A., Winkelmann, H., Lochte, S., Stanly, T. A., Pulgar Prieto, K. D., Poojari, C., Sharma, V., Richter, C. P., Kurre, R., Hubbard, S. R., Garcia, K. C., Moraga, I., Vattulainen, I., Hitchcock, I. S. & Piehler, J., 7 Feb 2020

Article in Science

Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4

Tucker, J. A., Myers, S. M., Miller, D. C., Molyneux, L., Arasta, M., Bawn, R. H., Blackburn, T. J., Cook, S. J., Edwards, N., Endicott, J. A., Golding, B. T., Griffin, R. J., Hammonds, T., Hardcastle, I. R., Harnor, S. J., Heptinstall, A. B., Lochhead, P. A., Martin, M. P., Martin, N. C., Newell, D. R. & 10 others, Owen, P. J., Pang, L. C., Reuillon, T., Rigoreau, L. J. M., Thomas, H. D., Wang, L-Z., Wong, A-C., Noble, M. E. M., Wedge, S. R. & Cano, C., 15 Sep 2019

Article in European Journal of Medicinal Chemistry

Novel Thienopyrimidine Inhibitors of Leishmania N-Myristoyltransferase with On-Target Activity in Intracellular Amastigotes

Bell, A. S., Yu, Z., Hutton, J. A., Wright, M. H., Brannigan, J. A., Paape, D., Roberts, S. M., Sutherell, C. L., Ritzefeld, M., Wilkinson, A. J., Smith, D. F., Leatherbarrow, R. J. & Tate, E. W., 23 Jul 2020

Article in JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of Calcium Dependent Protein Kinase 1 (CDPK1) by Pyrazolopyrimidine Analogs Decreases Establishment and Reoccurrence of Central Nervous System Disease by Toxoplasma gondii.

Rutaganira, F. U., Barks, J., Dhason, M. S., Wang, Q., Lopez, M. S., Long, S., Radke, J. B., Jones, N. G., Maddirala, A. R., Janetka, J. W., El Bakkouri, M., Hui, R., Shokat, K. M. & Sibley, L. D., 28 Dec 2017

Article in JOURNAL OF MEDICINAL CHEMISTRY

Insulin-like Growth Factor 1 Analogs Clicked in the C Domain: Chemical Synthesis and Biological Activities

Macháčková, K., Collinsová, M., Chrudinová, M., Selicharová, I., Pícha, J., Buděšínský, M., Vaněk, V., Žáková, L., Brzozowski, A. M. & Jiráček, J., 28 Dec 2017

Article in JOURNAL OF MEDICINAL CHEMISTRY

Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1)

Williamson, D. S., Smith, G. P., Acheson-Dossang, P., Bedford, S. T., Chell, V., Chen, I-J., Daechsel, J. C. A., Daniels, Z., David, L., Dokurno, P., Hentzer, M., Herzig, M. C., Hubbard, R. E., Moore, J. D., Murray, J. B., Newland, S., Ray, S. C., Shaw, T., Surgenor, A. E., Terry, L. & 3 others, Thirstrup, K., Wang, Y. & Christensen, K. V., 12 Oct 2017

Article in JOURNAL OF MEDICINAL CHEMISTRY