Unhooking the Hook: Optimization of the Aurora A Targeting PROTAC JB170 to CCT400028, an In Vitro Degrader Chemical Probe.

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Title: Unhooking the Hook: Optimization of the Aurora A Targeting PROTAC JB170 to CCT400028, an In Vitro Degrader Chemical Probe.
Authors: O'Hanlon JA; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.; Cancer Research UK Children's Brain Tumour Centre of Excellence, The Institute of Cancer Research, London SM2 5NG, U.K., Gutsche K; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K., Müller JE; Institute of Biochemistry, University of Kiel, Rudolf-Höber-Straße 1, Kiel 24118, Germany., Ranjan Prusty N; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K., Mirza A; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K., Roumeliotis TI; Functional Proteomics Group, Institute of Cancer Research, Chester Beatty Laboratories, 237 Fulham Road, SW3 6JB London, U.K., Yang H; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K., Stubbs M; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K., Hallett ST; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K., Eing L; Chair of Biochemistry and Molecular Biology, University of Würzburg, Am Hubland, Würzburg 97074, Germany., McAndrew PC; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K., Choudhary JS; Functional Proteomics Group, Institute of Cancer Research, Chester Beatty Laboratories, 237 Fulham Road, SW3 6JB London, U.K., Le Bihan YV; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.; Division of Structural Biology, The Institute of Cancer Research, London SM2 5NG, U.K., Caldwell J; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K., van Montfort RLM; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.; Division of Structural Biology, The Institute of Cancer Research, London SM2 5NG, U.K., Workman P; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.; Cancer Research UK Children's Brain Tumour Centre of Excellence, The Institute of Cancer Research, London SM2 5NG, U.K., Wolf E; Institute of Biochemistry, University of Kiel, Rudolf-Höber-Straße 1, Kiel 24118, Germany., Newton GK; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.; Cancer Research UK Children's Brain Tumour Centre of Excellence, The Institute of Cancer Research, London SM2 5NG, U.K., Evans LE; Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.; Cancer Research UK Children's Brain Tumour Centre of Excellence, The Institute of Cancer Research, London SM2 5NG, U.K.
Source: Journal of medicinal chemistry [J Med Chem] 2026 Jan 22; Vol. 69 (2), pp. 1552-1567. Date of Electronic Publication: 2026 Jan 12.
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.5c03024