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Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis

Research output: Contribution to journalJournal article

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Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis. / Wyllie, Susan; Thomas, Michael; Patterson, Stephen; Crouch, Sabrinia; De Rycker, Manu; Lowe, Rhiannon; Gresham, Stephanie; Urbaniak, Michael Daniel; Otto, Thomas D.; Stojanovski, Laste; Simeons, Frederick R. C.; Manthri, Sujatha; MacLean, Lorna M.; Zuccotto, Fabio; Homeyer, Nadine; Pflaumer, Hannah; Boesche, Markus; Sastry, Lalitha; Connolly, Paul ; Albrecht, Sebastian; Berriman, Matt; Drewes, Gerard; Gray, David W.; Ghidelli-Disse, Sonja; Dixon, Susan; Fiandor, Jose M.; Wyatt, Paul G.; Ferguson, Michael A. J.; Fairlamb, Alan H.; Miles, Timothy J.; Read, Kevin D.; Gilbert, Ian H.

In: Nature, Vol. 560, 25.07.2018, p. 192-197.

Research output: Contribution to journalJournal article

Harvard

Wyllie, S, Thomas, M, Patterson, S, Crouch, S, De Rycker, M, Lowe, R, Gresham, S, Urbaniak, MD, Otto, TD, Stojanovski, L, Simeons, FRC, Manthri, S, MacLean, LM, Zuccotto, F, Homeyer, N, Pflaumer, H, Boesche, M, Sastry, L, Connolly, P, Albrecht, S, Berriman, M, Drewes, G, Gray, DW, Ghidelli-Disse, S, Dixon, S, Fiandor, JM, Wyatt, PG, Ferguson, MAJ, Fairlamb, AH, Miles, TJ, Read, KD & Gilbert, IH 2018, 'Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis', Nature, vol. 560, pp. 192-197. https://doi.org/10.1038/s41586-018-0356-z

APA

Wyllie, S., Thomas, M., Patterson, S., Crouch, S., De Rycker, M., Lowe, R., ... Gilbert, I. H. (2018). Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis. Nature, 560, 192-197. https://doi.org/10.1038/s41586-018-0356-z

Vancouver

Wyllie S, Thomas M, Patterson S, Crouch S, De Rycker M, Lowe R et al. Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis. Nature. 2018 Jul 25;560:192-197. https://doi.org/10.1038/s41586-018-0356-z

Author

Wyllie, Susan ; Thomas, Michael ; Patterson, Stephen ; Crouch, Sabrinia ; De Rycker, Manu ; Lowe, Rhiannon ; Gresham, Stephanie ; Urbaniak, Michael Daniel ; Otto, Thomas D. ; Stojanovski, Laste ; Simeons, Frederick R. C. ; Manthri, Sujatha ; MacLean, Lorna M. ; Zuccotto, Fabio ; Homeyer, Nadine ; Pflaumer, Hannah ; Boesche, Markus ; Sastry, Lalitha ; Connolly, Paul ; Albrecht, Sebastian ; Berriman, Matt ; Drewes, Gerard ; Gray, David W. ; Ghidelli-Disse, Sonja ; Dixon, Susan ; Fiandor, Jose M. ; Wyatt, Paul G. ; Ferguson, Michael A. J. ; Fairlamb, Alan H. ; Miles, Timothy J. ; Read, Kevin D. ; Gilbert, Ian H. / Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis. In: Nature. 2018 ; Vol. 560. pp. 192-197.

Bibtex

@article{00e9f9cc35ac491daf31fd3611dd6047,
title = "Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis",
abstract = "Visceral leishmaniasis causes considerable mortality and morbidity in many parts of the world. There is an urgent need for the development of new, effective treatments for this disease. Here we describe the development of an anti-leishmanial drug-like chemical series based on a pyrazolopyrimidine scaffold. The leading compound from this series (7, DDD853651/GSK3186899) is efficacious in a mouse model of visceral leishmaniasis, has suitable physicochemical, pharmacokinetic and toxicological properties for further development, and has been declared a preclinical candidate. Detailed mode-of-action studies indicate that compounds from this series act principally by inhibiting the parasite cdc-2-related kinase 12 (CRK12), thus defining a druggable target for visceral leishmaniasis.",
author = "Susan Wyllie and Michael Thomas and Stephen Patterson and Sabrinia Crouch and {De Rycker}, Manu and Rhiannon Lowe and Stephanie Gresham and Urbaniak, {Michael Daniel} and Otto, {Thomas D.} and Laste Stojanovski and Simeons, {Frederick R. C.} and Sujatha Manthri and MacLean, {Lorna M.} and Fabio Zuccotto and Nadine Homeyer and Hannah Pflaumer and Markus Boesche and Lalitha Sastry and Paul Connolly and Sebastian Albrecht and Matt Berriman and Gerard Drewes and Gray, {David W.} and Sonja Ghidelli-Disse and Susan Dixon and Fiandor, {Jose M.} and Wyatt, {Paul G.} and Ferguson, {Michael A. J.} and Fairlamb, {Alan H.} and Miles, {Timothy J.} and Read, {Kevin D.} and Gilbert, {Ian H.}",
year = "2018",
month = "7",
day = "25",
doi = "10.1038/s41586-018-0356-z",
language = "English",
volume = "560",
pages = "192--197",
journal = "Nature",
issn = "0028-0836",
publisher = "Nature Publishing Group",

}

RIS

TY - JOUR

T1 - Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis

AU - Wyllie, Susan

AU - Thomas, Michael

AU - Patterson, Stephen

AU - Crouch, Sabrinia

AU - De Rycker, Manu

AU - Lowe, Rhiannon

AU - Gresham, Stephanie

AU - Urbaniak, Michael Daniel

AU - Otto, Thomas D.

AU - Stojanovski, Laste

AU - Simeons, Frederick R. C.

AU - Manthri, Sujatha

AU - MacLean, Lorna M.

AU - Zuccotto, Fabio

AU - Homeyer, Nadine

AU - Pflaumer, Hannah

AU - Boesche, Markus

AU - Sastry, Lalitha

AU - Connolly, Paul

AU - Albrecht, Sebastian

AU - Berriman, Matt

AU - Drewes, Gerard

AU - Gray, David W.

AU - Ghidelli-Disse, Sonja

AU - Dixon, Susan

AU - Fiandor, Jose M.

AU - Wyatt, Paul G.

AU - Ferguson, Michael A. J.

AU - Fairlamb, Alan H.

AU - Miles, Timothy J.

AU - Read, Kevin D.

AU - Gilbert, Ian H.

PY - 2018/7/25

Y1 - 2018/7/25

N2 - Visceral leishmaniasis causes considerable mortality and morbidity in many parts of the world. There is an urgent need for the development of new, effective treatments for this disease. Here we describe the development of an anti-leishmanial drug-like chemical series based on a pyrazolopyrimidine scaffold. The leading compound from this series (7, DDD853651/GSK3186899) is efficacious in a mouse model of visceral leishmaniasis, has suitable physicochemical, pharmacokinetic and toxicological properties for further development, and has been declared a preclinical candidate. Detailed mode-of-action studies indicate that compounds from this series act principally by inhibiting the parasite cdc-2-related kinase 12 (CRK12), thus defining a druggable target for visceral leishmaniasis.

AB - Visceral leishmaniasis causes considerable mortality and morbidity in many parts of the world. There is an urgent need for the development of new, effective treatments for this disease. Here we describe the development of an anti-leishmanial drug-like chemical series based on a pyrazolopyrimidine scaffold. The leading compound from this series (7, DDD853651/GSK3186899) is efficacious in a mouse model of visceral leishmaniasis, has suitable physicochemical, pharmacokinetic and toxicological properties for further development, and has been declared a preclinical candidate. Detailed mode-of-action studies indicate that compounds from this series act principally by inhibiting the parasite cdc-2-related kinase 12 (CRK12), thus defining a druggable target for visceral leishmaniasis.

U2 - 10.1038/s41586-018-0356-z

DO - 10.1038/s41586-018-0356-z

M3 - Journal article

VL - 560

SP - 192

EP - 197

JO - Nature

JF - Nature

SN - 0028-0836

ER -