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An allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance.
Hagenbeek TJ, Zbieg JR, Hafner M, Mroue R, Lacap JA, Sodir NM, Noland CL, Afghani S, Kishore A, Bhat KP, Yao X, Schmidt S, Clausen S, Steffek M, Lee W, Beroza P, Martin S, Lin E, Fong R, Di Lello P, Kubala MH, Yang MN, Lau JT, Chan E, Arrazate A, An L, Levy E, Lorenzo MN, Lee HJ, Pham TH, Modrusan Z, Zang R, Chen YC, Kabza M, Ahmed M, Li J, Chang MT, Maddalo D, Evangelista M, Ye X, Crawford JJ, Dey A. Hagenbeek TJ, et al. Among authors: di lello p. Nat Cancer. 2023 Jun;4(6):812-828. doi: 10.1038/s43018-023-00577-0. Epub 2023 Jun 5. Nat Cancer. 2023. PMID: 37277530 Free PMC article.
USP7 small-molecule inhibitors interfere with ubiquitin binding.
Kategaya L, Di Lello P, Rougé L, Pastor R, Clark KR, Drummond J, Kleinheinz T, Lin E, Upton JP, Prakash S, Heideker J, McCleland M, Ritorto MS, Alessi DR, Trost M, Bainbridge TW, Kwok MCM, Ma TP, Stiffler Z, Brasher B, Tang Y, Jaishankar P, Hearn BR, Renslo AR, Arkin MR, Cohen F, Yu K, Peale F, Gnad F, Chang MT, Klijn C, Blackwood E, Martin SE, Forrest WF, Ernst JA, Ndubaku C, Wang X, Beresini MH, Tsui V, Schwerdtfeger C, Blake RA, Murray J, Maurer T, Wertz IE. Kategaya L, et al. Among authors: di lello p. Nature. 2017 Oct 26;550(7677):534-538. doi: 10.1038/nature24006. Epub 2017 Oct 18. Nature. 2017. PMID: 29045385
Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists.
Zhang Y, Ultsch M, Skelton NJ, Burdick DJ, Beresini MH, Li W, Kong-Beltran M, Peterson A, Quinn J, Chiu C, Wu Y, Shia S, Moran P, Di Lello P, Eigenbrot C, Kirchhofer D. Zhang Y, et al. Among authors: di lello p. Nat Struct Mol Biol. 2017 Oct;24(10):848-856. doi: 10.1038/nsmb.3453. Epub 2017 Aug 21. Nat Struct Mol Biol. 2017. PMID: 28825733
Mitigation of reactive metabolite formation for a series of 3-amino-2-pyridone inhibitors of Bruton's tyrosine kinase (BTK).
Lou Y, Lopez F, Jiang Y, Han X, Brotherton C, Billedeau R, Gabriel S, Gleason S, Goldstein DM, Hilgenkamp R, Kocer B, Orzechowski L, Tan J, Wovkulich P, Wen B, Fry D, Di Lello P, Chen L, Zhang FJ, Fretland J, Nangia A, Yang T, Owens TD. Lou Y, et al. Among authors: di lello p. Bioorg Med Chem Lett. 2017 Feb 1;27(3):632-635. doi: 10.1016/j.bmcl.2016.11.092. Epub 2016 Dec 2. Bioorg Med Chem Lett. 2017. PMID: 28025004
Crystal Structures of the Human Doublecortin C- and N-terminal Domains in Complex with Specific Antibodies.
Burger D, Stihle M, Sharma A, Di Lello P, Benz J, D'Arcy B, Debulpaep M, Fry D, Huber W, Kremer T, Laeremans T, Matile H, Ross A, Rufer AC, Schoch G, Steinmetz MO, Steyaert J, Rudolph MG, Thoma R, Ruf A. Burger D, et al. Among authors: di lello p. J Biol Chem. 2016 Jul 29;291(31):16292-306. doi: 10.1074/jbc.M116.726547. Epub 2016 May 10. J Biol Chem. 2016. PMID: 27226599 Free PMC article.
36 results