PUBLICATIONS

  1. “ValCitGlyPro-Dexamethasone Antibody Conjugates Selectively Suppress the Activation of Human Monocytes“, Justin M Howe, Siteng Fang, Kelsey A. Watts, Fanny Xu, Samantha R Benjamin and L. Nathan Tumey. RSC Med. Chem., 2023, Accepted Manuscript.   https://pubs.rsc.org/en/content/articlelanding/2023/md/d3md00336a
  2. “Synthesis and Optimization of 1-Substituted Imidazo[4,5-c]quinoline TLR7 Agonists”, Emma G. DeYoung, Justin M. Howe, Siteng Fang, Mullapudi Mohan Reddy, Jillian P. Handel, Jared T. Gillen Miller, Daniel R. Wheeler, and L. Nathan Tumey. ACS Med. Chem. Lett. 2023, XXXX, XXX, XXX-XXX https://pubs.acs.org/doi/full/10.1021/acsmedchemlett.3c00260
  3.  “Evaluation of an ester-linked immunosuppressive payload: A case study in understanding the stability and cleavability of ester-containing ADC linkers”, Courtney P. Jackson, Siteng Fang, Samantha R. Benjamin, Tchilabalo Alayi, Yetrib Hathout, Sarah M. Gillen, Jillian P. Handel, Brittany M. Brems, Justin M. Howe, L. Nathan Tumey*; Bioorganic and Medicinal Chemistry Letters, 75, 2022. DOI: 10.1016/j.bmcl.2022.128953
  4. “Design and Characterization of Immune-Stimulating Imidazo[4,5-c]quinoline Antibody-Drug Conjugates”, Siteng Fang, Brittany M Brems, Emmanuel O Olawode, Jared T Miller, Tracy A Brooks, L Nathan Tumey*; Molecular Pharmaceutics, 2022, 19, 9, 3228–3241. https://doi.org/10.1021/acs.molpharmaceut.2c00392
  5. “Indoloquinoline-Mediated Targeted Downregulation of KRAS through Selective Stabilization of the Mid-Promoter G-Quadruplex Structure”, AM Psaras, RK Carty, JT Miller, LN Tumey, TA Brooks; Genes 2022, 13 (8), 1440
  6. “ADC Linker Strategies for the Release of Alcohol-Containing Payloads”, Miller, Jared T., Tumey, L. Nathan*, Chemical Linkers in Antibody-Drug Conjugates (ADCs); Royal Society of Chemistry; 2021, pg 232-262.
  7. “The design and development of antibody-drug conjugates (ADCs) for the treatment of cancer”, Tumey, L. Nathan*, Burger’s Medicinal Chemistry, Drug Discovery and Development; Wiley Publishing, 2021. https://doi.org/10.1002/0471266949.bmc283
  8. “Enzyme-Agnostic Lysosomal Screen Identifies New Legumain-Cleavable ADC Linkers”, Jared T Miller, Caitlin N Vitro, Siteng Fang, Samantha R Benjamin, L Nathan Tumey; Bioconjugate Chemistry, 2021, 32, 4, 842-858. DOI: https://doi.org/10.1021/acs.bioconjchem.1c00124
  9. “Development of Highly Optimized Antibody–Drug Conjugates against CD33 and CD123 for Acute Myeloid Leukemia”, Yoon-Chi Han, Jennifer Kahler, Nicole Piché-Nicholas, Wenyue Hu, Stephane Thibault, Fan Jiang, Mauricio Leal, Madan Katragadda, Andreas Maderna, Russell Dushin, Nadira Prashad, Manoj B Charati, Tracey Clark, L. Nathan Tumey, Xingzhi Tan, Andreas Giannakou, Edward Rosfjord, Hans-Peter Gerber, Lioudmila Tchistiakova, Frank Loganzo, Christopher J O’Donnell, Puja Sapra, Clinical Cancer Research, 2021, 27(2), 622-631. DOI: 10.1158/1078-0432.CCR-20-2149
  10. “PF-06804103, A Site-specific Anti-HER2 Antibody–Drug Conjugate for the Treatment of HER2-expressing Breast, Gastric, and Lung Cancers”; Edmund I Graziani, Matthew Sung, Dangshe Ma, Bitha Narayanan, Kimberly Marquette, Sujiet Puthenveetil, L Nathan Tumey, Jack Bikker, Jeffrey Casavant, Eric M Bennett, Manoj B Charati, Jonathon Golas, Christine Hosselet, Cynthia M Rohde, George Hu, Magali Guffroy, Hadi Falahatpisheh, Martin Finkelstein, Tracey Clark, Frank Barletta, Lioudmila Tchistiakova, Judy Lucas, Edward Rosfjord, Frank Loganzo, Christopher J O’Donnell, Hans-Peter Gerber, Puja Sapra; Molecular Cancer Therapeutics, 2020, 19, 10, 2068-2078. DOI: 10.1158/1535-7163.MCT-20-0237
  11. “Expanding the Versatility of Microbial Transglutaminase Using α-Effect Nucleophiles as Noncanonical Substrates.” Tak Ian Chio; Breanna R. Demestichas; Brittany M. Brems; Susan L. Bane*; L. Nathan Tumey*, Angew. Chemie, 59, 13814–13820, 2020. DOI: 10.1002/anie.202001830
  12. “An Overview of the Current ADC Discovery Landscape” (book chapter); L. N. Tumey; Antibody-Drug Conjugates (Methods in Molecular Biology), Humana, New York, NY, 2020. Page 1-22. DOI:10.1007/978-1-4939-9929-3_1
  13. “Detection and Removal of Small Molecule and Endotoxin Contaminants in ADC Preparations” (book chapter); J. Casavant, A. S. Ratnayake, S. Puthenveetil, L. N. Tumey; Antibody-Drug Conjugates (Methods in Molecular Biology), Humana, New York, NY, 2020. Page 291-299. DOI:10.1007/978-1-4939-9929-3_20
  14. “Case report: Albendazole associated psychosis”, Doughty, Bennett; Tumey, L. Nathan; Williams, Karen; Mental Health Clinician, November 2019, 9, 6, 397-400. DOI: 10.9740/mhc.2019.11.397
  15. “Antibody-Drug-Conjugates: Methods and Protocols”, Springer Publishing, 2019. (lead editor)
  16. “Thiolation of Q295: Site-specific conjugation of hydrophobic payloads without the need for genetic engineering”, Benjamin, Samantha R.; Jackson, Courtney P.; Fang,  Siteng; Carlson, Dane P.; Guo, Zhongyuan; Tumey, L. Nathan*, Molecular Pharmaceutics, 2019, 16,6, 2795-2807. DOI: 10.1021/acs.molpharmaceut.9b00323
  17. “Site-Specific Bioconjugation and Multi-Bioorthogonal Labeling via Rapid Formation of a Boron–Nitrogen Heterocycle”, Choi, Tak Ian; Gu, Han; Mukherjee, Kamalika; Tumey, L. Nathan Tumey*; Bane, Susan L. * (co-corresponding authors), Bioconjugate Chemistry, 2019, 30, 5, 1554-1564. DOI: 10.1021/acs.bioconjchem.9b00246
  18. “Natural Product Bis-​Intercalator Depsipeptides as a New Class of Payloads for Antibody-​Drug Conjugates”, Ratnayake, Anokha S.; Chang, Li-ping; Tumey, L. Nathan; Loganzo, Frank; Chemler, Joseph A.; Wagenaar, Melissa; Musto, Sylvia; Li, Fengping; Janso, Jeffrey E.; Ballard, T. Eric; Rago, Brian; Steele, Greg L.; Ding, WeiDong; Feng, Xidong; Hosselet, Christine; Buklan, Vlad; Lucas, Judy; Koehn, Frank E.; O’Donnell, Christopher J.; Graziani, Edmund I., Bioconjugate Chemistry, 2019, 30(1), 200-209.  DOI:10.1021/acs.bioconjchem.8b00843
  19. “Novel PIKK inhibitor antibody-drug conjugates: Synthesis and anti-tumor activity”, Zhou, Dahui; Casavant, Jeffrey; Graziani, Edmund I.; He, Haiyin; Janso, Jeffrey; Loganzo, Frank; Musto, Sylvia; Tumey, Nathan; O’Donnell, Christopher J.; Dushin, Russell, Bioorganic & Medicinal Chemistry Letters, 2019, 29(7), 943-957. DOI:10.1016/j.bmcl.2019.01.009
  20. “Next generation payloads for ADCs” (book chapter), L. Nathan Tumey*, Springer Publishing, “Innovations for Next-Generation Antibody-Drug Conjugates”, 2018.
  21. “ADME Considerations for the Development of Biopharmaceutical Conjugates Using Cleavable Linkers”, L. Nathan Tumey* and Sean Han, Current Topics in Medicinal Chemistry, 2017, 17(32), 3444-3462.
  22. “Multivalent peptidic linker enables identification of preferred sites of conjugation for a potent thialanstatin antibody drug conjugate”, Puthenveetil, Sujiet; He, Haiyin; Loganzo, Frank; Musto, Sylvia; Teske, Jesse; Green, Michael; Tan, Xingzhi; Hosselet, Christine; Lucas, Judy; Tumey, L. Nathan; Sapra, Puja; Subramanyam, Chakrapani; O’Donnell, Christopher J.; Graziani, Edmund I, 2017, PLoS One, 12(5), e0178452/1-e0178452/16. DOI:10.1371/journal.pone.0178452
  23. “Thinking Small and Dreaming Big: Medicinal Chemistry Strategies for Designing Optimal ADCs”, L. Nathan Tumey*, 2017, Medicinal Chemistry Reviews, Chapter 19, 2017, 52, 363-379.
  24. “Site selection: A case study in the identification of optimal cysteine engineered ADCs.”, L. Nathan Tumey*, Fengping Li, Brian Rago, Xiaogang Han, Frank Loganzo, Sylvia Musto, Edmund I. Graziani, Sujiet Puthenveetil, Jeffrey Casavant, Kimberly Marquette, Tracey Clark, Jack Bikker, Eric M. Bennett, Frank Barletta, Nicole Piche-Nicholas, Amy Tam, Christopher J. O’Donnell, Hans Peter Gerber, and Lioudmila Tchistiakova; AAPS Journal, 2017, 19(4), 1123-1135.
  25. “Quantitative Conjugated Payload Measurement Using Enzymatic Release of Antibody-Drug Conjugate with Cleavable Linker.”, Brian Rago, L. Nathan Tumey, Cong Wei, Frank Barletta, Tracey Clark, Steve Hansel, and Xiaogang Han; Bioconjugate Chemistry, 2017, 28(2), 620-626.
  26. “Optimization of Tubulysin Antibody-Drug-Conjugates: A Case Study in Addressing ADC Metabolism”, L. Nathan Tumey, Carolyn A. Leverett, Beth Vetelino, Fengping Li, Brian Rago, Xiaogang Han, Frank Loganzo, Sylvia Musto, Guoyun Bai, Sai Chetan K. Sukuru, Edmund I. Graziani, Sujiet Puthenveetil, Jeffrey Casavant, Anokha Ratnayake, Kimberly Marquette, Sarah Hudson†, Venkata Ramana Doppala-pudi, Joseph Stock‡, Lioudmilla Tchistiakov, Andrew J. Bessire, Tracey Clark, Judy Lucas, Christine Hosselet, Christopher J. O’Donnell, and Chakrapani Subramanyam; ACS Medicinal Chemistry Letters, 2016, 7(11), 977-982. [Selected as cover article for November 2016 edition]
  27. “Calculated conjugated payload from immunoassay and LC–MS intact protein analysis measurements of antibody-drug conjugate”, Brian Rago, Tracey Clark, Lindsay King, Jenny Zhang, L. Nathan Tumey, Fengping Li, Frank Barletta, Cong Wei, Mauricio Leal, Steve Hansel*, & Xiaogang Han; Bioanalysis, 2016, 8(21), 2205-2217.
  28. “Natural Product Splicing Inhibitors: A New Class of Antibody-​Drug Conjugate (ADC) Payloads”, Puthenveetil, Sujiet; Loganzo, Frank; He, Haiyin; Dirico, Ken; Green, Michael; Teske, Jesse; Musto, Sylvia; Clark, Tracey; Rago, Brian; Koehn, Frank; Veneziale, Robert; Falahaptisheh, Hadi; Han, Xiaogang; Barletta, Frank; Lucas, Judy; Subramanyam, Chakrapani; O’Donnell, Christopher J.; Tumey, L. Nathan; Sapra, Puja; Gerber, Hans Peter; Ma, Dangshe; Graziani, Edmund I; Bioconjugate Chemistry, 2016, 27(8), 1880-1888.
  29. “Where Did the Linker-​Payload Go? A Quantitative Investigation on the Destination of the Released Linker-​Payload from an Antibody-​Drug Conjugate with a Maleimide Linker in Plasma”, Wei, Cong; Zhang, Guodong; Clark, Tracey; Barletta, Frank; Tumey, L. Nathan; Rago, Brian; Hansel, Steven; Han, Xiaogang; Analytical Chemistry, 2016, 88(9), 4979.
  30. “Development of Solid-​Phase Site-​Specific Conjugation and Its Application toward Generation of Dual Labeled Antibody and Fab Drug Conjugates”, Puthenveetil, Sujiet; Musto, Sylvia; Loganzo, Frank; Tumey, L. Nathan; O’Donnell, Christopher J.; Graziani, Edmund; Bioconjugate Chemistry, 2016, 27(4) 1030.
  31. “In vivo biotransformations of antibody-​drug conjugates”, Tumey, L. Nathan; Rago, Brian; Han, Xiaogang; Bioanalysis, 2015, 7(13), 1649.
  32. “Mild method for succinimide hydrolysis on ADCs: Impact on ADC potency, stability, exposure, and efficacy”, L. Nathan Tumey, Manoj Charati, Tao He, Eric Sousa, Dangshe Ma, Xiaogang Han, Tracey Clark, Jeff Casavant, Frank Loganzo, Frank Barletta, Judy Lucas, and Edmund I. Graziani; Bioconjugate Chemistry, 2014, 25(10), p1871-1880.
  33. “Identification and optimization of indolo[2,3-c]quinoline inhibitors of IRAK4” Tumey, L. Nathan; Boschelli, Diane H.; Bhagirath, Niala; Shim, Jaechul; Murphy, Elizabeth A.; Goodwin, Deborah; Bennett, Eric M.; Wang, Mengmeng; Lin, Lih-Ling; Press, Barry; Shen, Marina; Frisbie, Richard K.; Morgan, Paul; Mohan, Shashi; Shin, Julia; Rao, Vikram R., Bioorganic and Medicinal Chemistry Letters, 2014, 24, 2066-2072.
  34.  “Recent advances in antibody-​drug conjugates” Graziani, Edmund I.; Tumey, L. Nathan, RSC Drug Discovery Series, 2013, 36 (Biotherapeutics), 145-175.
  35. “CRTH2 antagonists” Tumey, L. Nathan, RSC Drug Discovery Series, 2012, 26 (Anti-Inflammatory Drug Discovery), 104-134.
  36. “5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCθ: Optimization of enzymatic and functional activity.”, Tumey, L. Nathan; Bhagirath, Niala; Brennan, Agnes; Brooijmans, Natasja; Lee, Julie; Yang, Xiaoke; Boschelli, Diane H., Bioorg. Med. Chem, 2009, 17, 7933-7948.
  37. “First generation 5-vinyl-3-pyridinecarbonitrile PKC-theta inhibitors”, Niu, Chuansheng; Boschelli, Diane H.; Tumey, L. Nathan; Bhagirath, Niala; Subrath, Joan; Shim, Jaechul; Wang, Yan; Wu, Biqi; Eid, Clark; Lee, Julie; Yang, Xiaoke; Brennan, Agnes; Chaudhary, Divya, Bioorg. Med. Chem. Lett., 2009, 19(20), 5829-5832.
  38. “2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKC-theta”, Tumey, L. Nathan; Boschelli, Diane H.; Lee, Julie; Chaudhary, Divya.  Bioorg. Med. Chem. Lett.,2008, 18(15), 4420-4423.
  39. “A facile, scalable preparation of 4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carbonitriles”, Tumey, L. Nathan; Bhagirath, Niala; Wu, Biqi; Boschelli, Diane H., Tetrahedron Lett., 2008, 49(48), 6850-6852.
  40. “Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.”, Robarge, Michael J.; Bom, David C.; Tumey, L. Nathan; Varga, Norbert; Gleason, Elizabeth; Silver, Daniel; Song, Jianping; Murphy, Steven M.; Eckema, George; Doucette, Chris; Hanniford, Doug; Palmer, Marc; Pawlowski, Gary; Danzig, Joel; Loftus, Margaret; Hunady, Karen; Sherf, Bruce A; Mays, Robert W; Stricker-Krongrad, Alain; Brunden, Kurt R; Harrington, John J; Bennani, Youssef L, Bioorg. Med. Chem. Lett. 2005, 15(6), 1749-1753.
  41. “The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors”, Tumey, L. N.; Bom, D.; Huck, B.; Gleason, E.; Wang, J.; Silver, D.; Brunden, K.; Boozer, S.; Rundlett, S.; Sherf, B.; Murphy, S.; Dent, T.; Leventhal, C.; Bailey, A; Harrington, J; Bennani, Y. L.”, Bioorg. Med. Chem. Lett. 2005, 15(2), 277-81.
  42. “The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors”, Tumey, L.N.; Huck, B.; Gleason, E.; Wang, J.; Silver, D.; Brunden, K.; Boozer, S.; Rundlett, S.; Sherf, B.; Murphy, S.; Bailey, A.; Dent, T.; Leventhal, C.; Harrington, J.; Bennani, Y.L., Bioorg. Med. Chem. Lett., 2004, 14(19), 4915-8.
  43. “High-Throughput Catch-and-Release Synthesis of Oxazoline Hydroxamates. Structure-Activity Relationships in Novel Inhibitors of Escherichia coli LpxC: In Vitro Enzyme Inhibition and Antibacterial Properties”, Pirrung, M. C.; Tumey, L. N.; McClerren, A. L.; Raetz, C. R. H., J. Am. Chem. Soc., 2003, 125 (6), 1575-1586.
  44. “Inhibition of the antibacterial target UDP-(3-O-acyl)-N-acetylglucosamine deacetylase (LpxC): isoxazoline zinc amidase inhibitors bearing diverse metal binding groups”, Pirrung, M.C.; Tumey, L.N.; Raetz, C.R.; Jackman, J.E.; Snehalatha, K.; McClerren, A.L,; Fierke, C.A.; Gantt, S.L.; Rusche, K.M., J. Med. Chem., 2002, 45(19), 4359-70.
  45. “19F-Encoded Combinatorial Libraries:  Discovery of Selective Metal Binding and Catalytic Peptoids”, Michael C Pirrung; Kaapjoo Park; L Nathan Tumey, J. Comb. Chem., 2002, 4, 4, 329-344.
  46. “Antibacterial agents that target lipid A biosynthesis in gram-negative bacteria. Inhibition of diverse UDP-3-O-(r-3-hydroxymyristoyl)-n-acetylglucosamine deacetylases by substrate analogs containing zinc binding motifs.”, Jackman JE; Fierke CA; Tumey LN; Pirrung M; Uchiyama T; Tahir SH; Hindsgaul O; Raetz CR., J. Biol. Chem., 2000, 275(15), 11002-9.
  47. “Oxazoline Synthesis from Hydroxyamides by Resin Capture and Ring-Forming Release”, Michael C. Pirrung; L. Nathan Tumey, J. Comb. Chem., 2000, 2, 6, 675-680.