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Catalytic in vivo protein knockdown by small-molecule PROTACs.
Bondeson DP, Mares A, Smith IE, Ko E, Campos S, Miah AH, Mulholland KE, Routly N, Buckley DL, Gustafson JL, Zinn N, Grandi P, Shimamura S, Bergamini G, Faelth-Savitski M, Bantscheff M, Cox C, Gordon DA, Willard RR, Flanagan JJ, Casillas LN, Votta BJ, den Besten W, Famm K, Kruidenier L, Carter PS, Harling JD, Churcher I, Crews CM. Bondeson DP, et al. Among authors: campos s. Nat Chem Biol. 2015 Aug;11(8):611-7. doi: 10.1038/nchembio.1858. Epub 2015 Jun 10. Nat Chem Biol. 2015. PMID: 26075522 Free PMC article.
Discovery of novel irreversible inhibitors of interleukin (IL)-2-inducible tyrosine kinase (Itk) by targeting cysteine 442 in the ATP pocket.
Harling JD, Deakin AM, Campos S, Grimley R, Chaudry L, Nye C, Polyakova O, Bessant CM, Barton N, Somers D, Barrett J, Graves RH, Hanns L, Kerr WJ, Solari R. Harling JD, et al. Among authors: campos s. J Biol Chem. 2013 Sep 27;288(39):28195-206. doi: 10.1074/jbc.M113.474114. Epub 2013 Aug 9. J Biol Chem. 2013. PMID: 23935099 Free PMC article.
Acetylation of the Catalytic Lysine Inhibits Kinase Activity in PI3Kδ.
Fournier JCL, Evans JP, Zappacosta F, Thomas DA, Patel VK, White GV, Campos S, Tomkinson NCO. Fournier JCL, et al. Among authors: campos s. ACS Chem Biol. 2021 Sep 17;16(9):1644-1653. doi: 10.1021/acschembio.1c00225. Epub 2021 Aug 16. ACS Chem Biol. 2021. PMID: 34397208 Free article.
MCT2 mediates concentration-dependent inhibition of glutamine metabolism by MOG.
Fets L, Driscoll PC, Grimm F, Jain A, Nunes PM, Gounis M, Doglioni G, Papageorgiou G, Ragan TJ, Campos S, Silva Dos Santos M, MacRae JI, O'Reilly N, Wright AJ, Benes CH, Courtney KD, House D, Anastasiou D. Fets L, et al. Among authors: campos s. Nat Chem Biol. 2018 Nov;14(11):1032-1042. doi: 10.1038/s41589-018-0136-y. Epub 2018 Oct 8. Nat Chem Biol. 2018. PMID: 30297875 Free PMC article.
4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.
Liddle J, Bamborough P, Barker MD, Campos S, Cousins RP, Cutler GJ, Hobbs H, Holmes DS, Ioannou C, Mellor GW, Morse MA, Payne JJ, Pritchard JM, Smith KJ, Tape DT, Whitworth C, Williamson RA. Liddle J, et al. Among authors: campos s. Bioorg Med Chem Lett. 2009 May 1;19(9):2504-8. doi: 10.1016/j.bmcl.2009.03.034. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19349179
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
Liddle J, Bamborough P, Barker MD, Campos S, Chung CW, Cousins RP, Faulder P, Heathcote ML, Hobbs H, Holmes DS, Ioannou C, Ramirez-Molina C, Morse MA, Osborn R, Payne JJ, Pritchard JM, Rumsey WL, Tape DT, Vicentini G, Whitworth C, Williamson RA. Liddle J, et al. Among authors: campos s. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5222-6. doi: 10.1016/j.bmcl.2012.06.065. Epub 2012 Jun 26. Bioorg Med Chem Lett. 2012. PMID: 22801646
872 results