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Page 1
Covalent binders in drug discovery.
Vasudevan A, Argiriadi MA, Baranczak A, Friedman MM, Gavrilyuk J, Hobson AD, Hulce JJ, Osman S, Wilson NS. Vasudevan A, et al. Among authors: gavrilyuk j. Prog Med Chem. 2019;58:1-62. doi: 10.1016/bs.pmch.2018.12.002. Epub 2019 Mar 11. Prog Med Chem. 2019. PMID: 30879472
Design, Synthesis, and Biological Investigation of Thailanstatin A and Spliceostatin D Analogues Containing Tetrahydropyran, Tetrahydrooxazine, and Fluorinated Structural Motifs.
Nicolaou KC, Rekula SR, Kumar SM, Podilapu AR, Matuszak RP, Jung PM, Lam LT, Phillips AC, Lyssikatos J, Munneke S, Gu C, Sarvaiya H, Sandoval J, Hammond M, Aujay M, Purcell JW, Reilly RM, Gavrilyuk J. Nicolaou KC, et al. Among authors: gavrilyuk j. J Org Chem. 2021 Feb 5;86(3):2499-2521. doi: 10.1021/acs.joc.0c02643. Epub 2021 Jan 8. J Org Chem. 2021. PMID: 33417458
Streamlined Total Synthesis of Trioxacarcins and Its Application to the Design, Synthesis, and Biological Evaluation of Analogues Thereof. Discovery of Simpler Designed and Potent Trioxacarcin Analogues.
Nicolaou KC, Chen P, Zhu S, Cai Q, Erande RD, Li R, Sun H, Pulukuri KK, Rigol S, Aujay M, Sandoval J, Gavrilyuk J. Nicolaou KC, et al. Among authors: gavrilyuk j. J Am Chem Soc. 2017 Nov 1;139(43):15467-15478. doi: 10.1021/jacs.7b08820. Epub 2017 Oct 20. J Am Chem Soc. 2017. PMID: 29052423
Evaluation of PNU-159682 antibody drug conjugates (ADCs).
Holte D, Lyssikatos JP, Valdiosera AM, Swinney Z, Sisodiya V, Sandoval J, Lee C, Aujay MA, Tchelepi RB, Hamdy OM, Gu C, Lin B, Sarvaiya H, Pysz MA, Laysang A, Williams S, Jun Lee D, Holda MK, Purcell JW, Gavrilyuk J. Holte D, et al. Among authors: gavrilyuk j. Bioorg Med Chem Lett. 2020 Dec 15;30(24):127640. doi: 10.1016/j.bmcl.2020.127640. Epub 2020 Oct 28. Bioorg Med Chem Lett. 2020. PMID: 33127540
Design, Synthesis, and Biological Evaluation of Tubulysin Analogues, Linker-Drugs, and Antibody-Drug Conjugates, Insights into Structure-Activity Relationships, and Tubulysin-Tubulin Binding Derived from X-ray Crystallographic Analysis.
Nicolaou KC, Pan S, Pulukuri KK, Ye Q, Rigol S, Erande RD, Vourloumis D, Nocek BP, Munneke S, Lyssikatos J, Valdiosera A, Gu C, Lin B, Sarvaiaya H, Trinidad J, Sandoval J, Lee C, Hammond M, Aujay M, Taylor N, Pysz M, Purcell JW, Gavrilyuk J. Nicolaou KC, et al. Among authors: gavrilyuk j. J Org Chem. 2021 Feb 19;86(4):3377-3421. doi: 10.1021/acs.joc.0c02755. Epub 2021 Feb 5. J Org Chem. 2021. PMID: 33544599
Design, Synthesis, and Biological Investigation of Epothilone B Analogues Featuring Lactone, Lactam, and Carbocyclic Macrocycles, Epoxide, Aziridine, and 1,1-Difluorocyclopropane and Other Fluorine Residues.
Nicolaou KC, Shelke YG, Dherange BD, Kempema A, Lin B, Gu C, Sandoval J, Hammond M, Aujay M, Gavrilyuk J. Nicolaou KC, et al. Among authors: gavrilyuk j. J Org Chem. 2020 Mar 6;85(5):2865-2917. doi: 10.1021/acs.joc.0c00123. Epub 2020 Feb 17. J Org Chem. 2020. PMID: 32065746
Improved Total Synthesis of Tubulysins and Design, Synthesis, and Biological Evaluation of New Tubulysins with Highly Potent Cytotoxicities against Cancer Cells as Potential Payloads for Antibody-Drug Conjugates.
Nicolaou KC, Erande RD, Yin J, Vourloumis D, Aujay M, Sandoval J, Munneke S, Gavrilyuk J. Nicolaou KC, et al. Among authors: gavrilyuk j. J Am Chem Soc. 2018 Mar 14;140(10):3690-3711. doi: 10.1021/jacs.7b12692. Epub 2018 Jan 30. J Am Chem Soc. 2018. PMID: 29381062
ABBV-011, A Novel, Calicheamicin-Based Antibody-Drug Conjugate, Targets SEZ6 to Eradicate Small Cell Lung Cancer Tumors.
Wiedemeyer WR, Gavrilyuk J, Schammel A, Zhao X, Sarvaiya H, Pysz M, Gu C, You M, Isse K, Sullivan T, French D, Lee C, Dang AT, Zhang Z, Aujay M, Bankovich AJ, Vitorino P. Wiedemeyer WR, et al. Among authors: gavrilyuk j. Mol Cancer Ther. 2022 Jun 1;21(6):986-998. doi: 10.1158/1535-7163.MCT-21-0851. Mol Cancer Ther. 2022. PMID: 35642431 Free PMC article.
Synthesis and Biological Evaluation of Shishijimicin A-Type Linker-Drugs and Antibody-Drug Conjugates.
Nicolaou KC, Li R, Chen Q, Lu Z, Pitsinos EN, Schammel A, Lin B, Gu C, Sarvaiya H, Tchelepi R, Valdiosera A, Clubb J, Barbour N, Sisodiya V, Sandoval J, Lee C, Aujay M, Gavrilyuk J. Nicolaou KC, et al. Among authors: gavrilyuk j. J Am Chem Soc. 2020 Jul 22;142(29):12890-12899. doi: 10.1021/jacs.0c06554. Epub 2020 Jul 14. J Am Chem Soc. 2020. PMID: 32662641
32 results