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Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Fairhurst RA, Knoepfel T, Buschmann N, Leblanc C, Mah R, Todorov M, Nimsgern P, Ripoche S, Niklaus M, Warin N, Luu VH, Madoerin M, Wirth J, Graus-Porta D, Weiss A, Kiffe M, Wartmann M, Kinyamu-Akunda J, Sterker D, Stamm C, Adler F, Buhles A, Schadt H, Couttet P, Blank J, Galuba I, Trappe J, Voshol J, Ostermann N, Zou C, Berghausen J, Del Rio Espinola A, Jahnke W, Furet P. Fairhurst RA, et al. Among authors: berghausen j. J Med Chem. 2020 Nov 12;63(21):12542-12573. doi: 10.1021/acs.jmedchem.0c01019. Epub 2020 Oct 1. J Med Chem. 2020. PMID: 32930584
Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
Thoma G, Veenstra S, Strang R, Blanz J, Vangrevelinghe E, Berghausen J, Lee CC, Zerwes HG. Thoma G, et al. Among authors: berghausen j. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4642-7. doi: 10.1016/j.bmcl.2015.08.037. Epub 2015 Aug 18. Bioorg Med Chem Lett. 2015. PMID: 26320624
Ionic liquid versus prodrug strategy to address formulation challenges.
Balk A, Widmer T, Wiest J, Bruhn H, Rybak JC, Matthes P, Müller-Buschbaum K, Sakalis A, Lühmann T, Berghausen J, Holzgrabe U, Galli B, Meinel L. Balk A, et al. Among authors: berghausen j. Pharm Res. 2015 Jun;32(6):2154-67. doi: 10.1007/s11095-014-1607-9. Epub 2014 Dec 23. Pharm Res. 2015. PMID: 25534684
The Foundational Data Initiative for Parkinson Disease: Enabling efficient translation from genetic maps to mechanism.
Bressan E, Reed X, Bansal V, Hutchins E, Cobb MM, Webb MG, Alsop E, Grenn FP, Illarionova A, Savytska N, Violich I, Broeer S, Fernandes N, Sivakumar R, Beilina A, Billingsley KJ, Berghausen J, Pantazis CB, Pitz V, Patel D, Daida K, Meechoovet B, Reiman R, Courtright-Lim A, Logemann A, Antone J, Barch M, Kitchen R, Li Y, Dalgard CL; American Genome Center; Rizzu P, Hernandez DG, Hjelm BE, Nalls M, Gibbs JR, Finkbeiner S, Cookson MR, Van Keuren-Jensen K, Craig DW, Singleton AB, Heutink P, Blauwendraat C. Bressan E, et al. Among authors: berghausen j. Cell Genom. 2023 Feb 6;3(3):100261. doi: 10.1016/j.xgen.2023.100261. eCollection 2023 Mar 8. Cell Genom. 2023. PMID: 36950378 Free PMC article.
Current Approaches for Predicting Human PK for Small Molecule Development Candidates: Findings from the IQ Human PK Prediction Working Group Survey.
Petersson C, Zhou X, Berghausen J, Cebrian D, Davies M, DeMent K, Eddershaw P, Riedmaier AE, Leblanc AF, Manveski N, Marathe P, Mavroudis PD, McDougall R, Parrott N, Reichel A, Rotter C, Tess D, Volak LP, Xiao G, Yang Z, Baker J. Petersson C, et al. Among authors: berghausen j. AAPS J. 2022 Jul 19;24(5):85. doi: 10.1208/s12248-022-00735-9. AAPS J. 2022. PMID: 35854202 Review.
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