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Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.
Plenker D, Riedel M, Brägelmann J, Dammert MA, Chauhan R, Knowles PP, Lorenz C, Keul M, Bührmann M, Pagel O, Tischler V, Scheel AH, Schütte D, Song Y, Stark J, Mrugalla F, Alber Y, Richters A, Engel J, Leenders F, Heuckmann JM, Wolf J, Diebold J, Pall G, Peifer M, Aerts M, Gevaert K, Zahedi RP, Buettner R, Shokat KM, McDonald NQ, Kast SM, Gautschi O, Thomas RK, Sos ML. Plenker D, et al. Among authors: knowles pp. Sci Transl Med. 2017 Jun 14;9(394):eaah6144. doi: 10.1126/scitranslmed.aah6144. Sci Transl Med. 2017. PMID: 28615362 Free PMC article.
Structure and chemical inhibition of the RET tyrosine kinase domain.
Knowles PP, Murray-Rust J, Kjaer S, Scott RP, Hanrahan S, Santoro M, Ibáñez CF, McDonald NQ. Knowles PP, et al. J Biol Chem. 2006 Nov 3;281(44):33577-87. doi: 10.1074/jbc.M605604200. Epub 2006 Aug 23. J Biol Chem. 2006. PMID: 16928683 Free article.
A secondary RET mutation in the activation loop conferring resistance to vandetanib.
Nakaoku T, Kohno T, Araki M, Niho S, Chauhan R, Knowles PP, Tsuchihara K, Matsumoto S, Shimada Y, Mimaki S, Ishii G, Ichikawa H, Nagatoishi S, Tsumoto K, Okuno Y, Yoh K, McDonald NQ, Goto K. Nakaoku T, et al. Among authors: knowles pp. Nat Commun. 2018 Feb 12;9(1):625. doi: 10.1038/s41467-018-02994-7. Nat Commun. 2018. PMID: 29434222 Free PMC article.
Adenosine-binding motif mimicry and cellular effects of a thieno[2,3-d]pyrimidine-based chemical inhibitor of atypical protein kinase C isoenzymes.
Kjær S, Linch M, Purkiss A, Kostelecky B, Knowles PP, Rosse C, Riou P, Soudy C, Kaye S, Patel B, Soriano E, Murray-Rust J, Barton C, Dillon C, Roffey J, Parker PJ, McDonald NQ. Kjær S, et al. Among authors: knowles pp. Biochem J. 2013 Apr 15;451(2):329-42. doi: 10.1042/BJ20121871. Biochem J. 2013. PMID: 23418854
39 results