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A combined approach of structure-based virtual screening and NMR to interrupt the PD-1/PD-L1 axis: Biphenyl-benzimidazole containing compounds as novel PD-L1 inhibitors.
Donati G, Viviano M, D'Amore VM, Cipriano A, Diakogiannaki I, Amato J, Tomassi S, Brancaccio D, Russomanno P, Di Leva FS, Arosio D, Seneci P, Taliani S, Magiera-Mularz K, Musielak B, Skalniak L, Holak TA, Castellano S, La Pietra V, Marinelli L. Donati G, et al. Among authors: holak ta. Arch Pharm (Weinheim). 2024 Mar;357(3):e2300583. doi: 10.1002/ardp.202300583. Epub 2023 Dec 18. Arch Pharm (Weinheim). 2024. PMID: 38110703 Free article.
Structural and biological characterization of pAC65, a macrocyclic peptide that blocks PD-L1 with equivalent potency to the FDA-approved antibodies.
Rodriguez I, Kocik-Krol J, Skalniak L, Musielak B, Wisniewska A, Ciesiołkiewicz A, Berlicki Ł, Plewka J, Grudnik P, Stec M, Siedlar M, Holak TA, Magiera-Mularz K. Rodriguez I, et al. Among authors: holak ta. Mol Cancer. 2023 Sep 7;22(1):150. doi: 10.1186/s12943-023-01853-4. Mol Cancer. 2023. PMID: 37679783 Free PMC article.
1,5-Disubstituted tetrazoles as PD-1/PD-L1 antagonists.
van der Straat R, Draijer R, Surmiak E, Butera R, Land L, Magiera-Mularz K, Musielak B, Plewka J, Holak TA, Dömling A. van der Straat R, et al. Among authors: holak ta. RSC Med Chem. 2024 Feb 21;15(4):1210-1215. doi: 10.1039/d3md00746d. eCollection 2024 Apr 24. RSC Med Chem. 2024. PMID: 38665826 Free PMC article.
C2-Symmetrical Terphenyl Derivatives as Small Molecule Inhibitors of Programmed Cell Death 1/Programmed Death Ligand 1 Protein-Protein Interaction.
Klimek J, Kruc O, Ceklarz J, Kamińska B, Musielak B, van der Straat R, Dӧmling A, Holak TA, Muszak D, Kalinowska-Tłuścik J, Skalniak Ł, Surmiak E. Klimek J, et al. Among authors: holak ta. Molecules. 2024 Jun 4;29(11):2646. doi: 10.3390/molecules29112646. Molecules. 2024. PMID: 38893521 Free PMC article.
Solubilizer Tag Effect on PD-L1/Inhibitor Binding Properties for m-Terphenyl Derivatives.
Surmiak E, Ząber J, Plewka J, Wojtanowicz G, Kocik-Krol J, Kruc O, Muszak D, Rodríguez I, Musielak B, Viviano M, Castellano S, Skalniak L, Magiera-Mularz K, Holak TA, Kalinowska-Tłuścik J. Surmiak E, et al. Among authors: holak ta. ACS Med Chem Lett. 2023 Dec 14;15(1):36-44. doi: 10.1021/acsmedchemlett.3c00306. eCollection 2024 Jan 11. ACS Med Chem Lett. 2023. PMID: 38229762 Free PMC article.
Discovery of Inhibitory Fragments That Selectively Target Spire2-FMN2 Interaction.
Kitel R, Surmiak E, Borggräfe J, Kalinowska-Tluscik J, Golik P, Czub M, Uzar W, Musielak B, Madej M, Popowicz GM, Dubin G, Holak TA. Kitel R, et al. Among authors: holak ta. J Med Chem. 2023 Dec 14;66(23):15715-15727. doi: 10.1021/acs.jmedchem.3c00877. Epub 2023 Dec 1. J Med Chem. 2023. PMID: 38039505 Free PMC article.
200 results