Molecular Design of Unimolecular Tetra-Receptor Agonists
Dinsmore, T.C.; Cortigiano, J.E.; Xiang, S.; Spenciner, M.V.; Dobbins, A.R.; Zhao, R.L; Waldman, B.M.; Beinborn, M.; Kumar, K. J. Am. Chem. Soc. 2025, 147, 20819–20832
Selected Publications
Potent and Protease Resistant Azapeptide Agonists of the GLP-1 and GIP Receptors
Dinsmore, T.C; Liu, J.; Miao, J.; Ünsal, Ö.; Sürmeli, D.; Beinborn, M.; Lin, Y.-S.; Kumar, K. Angew. Chem. Int. Ed. 2024, e202410237. [PubMed]
Prolonged Activation of the GLP-1 Receptor via Covalent Capture
Ünsal, Ö.; Bacaksiz, Z.S.; Khamraev, V.; Montanari, V.; Beinborn, M.; Kumar, K. ACS Chem. Biol. 2024, 19, 1453–1465. [PubMed]
A Robust Platform for the Molecular Design of Potent, Protease-Stable, Long-Acting GIP Analogues
Sicinski, K. M.; Sürmeli, D.; Du, J.; Raman, V. S.; Montanari, V.; Lee, M.; Harwood, B.; Kopin, A. S.; Beinborn, M.; Kumar, K. J. Med. Chem. 2024, 67, 4998-5010. [PubMed]
A Non-Perturbative Molecular Grafting Strategy for Stable and Potent Therapeutic Peptide Ligands
Sicinski, K. M.; Montanari, V.; Raman, V. S.; Doyle, J. R.; Harwood, B. N.; Song, Y.-C.; Fagan, M. P.; Rios, M.; Haines, D. R.; Kopin, A. S.; Beinborn, M.; Kumar, K. ACS Cent. Sci. 2021, 7, 454-466. [PubMed]
Molecular design of peptide therapeutics via N-terminal modification
Sürmeli, D.; Dinsmore, T. C.; Anchukaitis, H. M.; Montanari, V.; Beinborn, M.; Kumar, K. Methods Enzymol. 2024, 698, 195-219.[PubMed]
Towards Non-stick Silk: Tuning the Hydrophobicity of Silk Fibroin Protein
Fountain, J. N.; Hawker, M. J.; Hartle, L.; Wu, J.; Montanari, V.; Sahoo, J. K.; Davis, L. M.; Kaplan, D. L.; Kumar, K. ChemBioChem 2022, e202200429.[PubMed]
Exploiting Existing Molecular Scaffolds for Long-Term COVID Treatment
Kumar, K.; Lupoli, T. ACS Med. Chem. Lett. 2020, 11, 1357-1360. [PubMed]
2025 – 2019
Molecular Design of Unimolecular Tetra-Receptor Agonists
Dinsmore, T.C.; Cortigiano, J.E.; Xiang, S.; Spenciner, M.V.; Dobbins, A.R.; Zhao, R.L; Waldman, B.M.; Beinborn, M.; Kumar, K. J. Am. Chem. Soc. 2025, 147, 20819–20832
Potent and Protease Resistant Azapeptide Agonists of the GLP-1 and GIP Receptors
Dinsmore, T.C.; Liu, J.; Miao, J.; Ünsal, Ö.; Sürmeli, D.; Beinborn, M.; Lin, Y.-S.; Kumar, K. Angew. Chem. Int. Ed. 2024, e202410237. [PubMed]
Prolonged Activation of the GLP-1 Receptor via Covalent Capture
Ünsal, Ö.; Bacaksiz, Z.S.; Khamraev, V.; Montanari, V.; Beinborn, M.; Kumar, K. ACS Chem. Biol. 2024, 19, 1453–1465. [PubMed]
A Robust Platform for the Molecular Design of Potent, Protease-Stable, Long-Acting GIP Analogues
Sicinski, K. M.; Sürmeli, D.; Du, J.; Raman, V. S.; Montanari, V.; Lee, M.; Harwood, B.; Kopin, A. S.; Beinborn, M.; Kumar, K. in A Robust Platform for the Molecular Design of Potent, Protease Stable, Long-Acting GIP Analogues. J. Med. Chem. 2024, 67, 4998-5010.[PubMed]
Molecular design of peptide therapeutics via N-terminal modification
Sürmeli, D.; Dinsmore, T. C.; Anchukaitis, H. M.; Montanari, V.; Beinborn, M.; Kumar, K. Methods Enzymol. 2024, 698, 195-219.[PubMed]
Towards Non-stick Silk: Tuning the Hydrophobicity of Silk Fibroin Protein
Fountain, J. N.; Hawker, M. J.; Hartle, L.; Wu, J.; Montanari, V.; Sahoo, J. K.; Davis, L. M.; Kaplan, D. L.; Kumar, K. ChemBioChem 2022, e202200429.[PubMed]
Future Perspectives on Peptide Therapeutics
Liu, J.; Ünsal, Ö.; Sicinski, K.M.; Kumar, K. in Peptide and Peptidomimetic Therapeutics: From Bench to Bedside Qvit, N.; Rubin, S.J.S. Eds., Academic Press 2022, pp. 699-726. [URL]
A Non-Perturbative Molecular Grafting Strategy for Stable and Potent Therapeutic Peptide Ligands
Sicinski, K. M.; Montanari, V.; Raman, V. S.; Doyle, J. R.; Harwood, B. N.; Song, Y.-C.; Fagan, M. P.; Rios, M.; Haines, D. R.; Kopin, A. S.; Beinborn, M.; Kumar, K. ACS Cent. Sci. 2021, 7, 454-466. [PubMed]
Exploiting Existing Molecular Scaffolds for Long-Term COVID Treatment
Kumar, K.; Lupoli, T. ACS Med. Chem. Lett. 2020, 11, 1357-1360.
Chemical Biology and Supramolecular Chemistry of Fluorinated Molecules.
Sicinski, K.; Montanari, V.; Kumar, K. Frontiers in Organofluorine Chemistry. Ojima, I. Ed., World Scientific 2020, pp. 561-584.
Discovery of Peptide Antibiotics Composed of D-Amino Acids.
Adailgil, E.; Patil, K.; Rodenstein, M.; Kumar, K. ACS Chem. Biol. 2019, 14, 1498-1506. [PubMed]
2016 – 2014
De Novo Design of Protein Mimics of B-DNA.
Yüksel, D.; Bianco, P. R.; Kumar, K. Mol. Biosyst. 2016, 12 (1), 169–177. [PubMed]
Designing Convergent Chemistry Curricula.
Charkoudian, L. K.; Sampson, N. S.; Kumar, K.; Kritzer, J. A. Nat. Chem. Biol. 2016, 12, 382. [PubMed]
Novel Probes Establish MrgprX1 Variants as Loss and Gain of Function Receptors.
Heller, D.; Doyle, J. R.; Raman, V. S.; Beinborn, M.; Kumar, K.; Kopin, A. S. J. Pharmacol. Exp. Ther. 2015, . [PubMed]
Sialidases as Regulators of Bioengineered Cellular Surfaces.
Zamora, C. Y.; Ryan, M. J.; d’Alarcao, M.; Kumar, K. Glycobiology 2015, 25 (7), 784–791. [PubMed]
Total Synthesis of Trifluorobutyryl-Modified, Protected Sialyl Lewis X by a Convergent [2+2] Approach.
Akçay, G.; Ramphal, J. Y.; d’Alarcao, M.; Kumar, K. Tetrahedron Lett. 2015, 56 (1), 109–114. [PubMed]
A Two-Step Strategy to Enhance Activity of Low Potency Peptides.
Doyle, J. R.; Harwood, B. N.; Krishnaji, S. T.; Krishnamurthy, V. M.; Lin, W.-E.; Fortin, J.-P.; Kumar, K.; Kopin, A. S. PLoS One 2014, 9 (11), e110502. [PubMed]
An Air- and Water-Stable Iodonium Salt Promoter for Facile Thioglycoside Activation.
Chu, A.-H. A.; Minciunescu, A.; Montanari, V.; Kumar, K.; Bennett, C. S. Org. Lett. 2014, 16 (6), 1780–1782. [PubMed]
Development of a Membrane-Anchored Chemerin Receptor Agonist as a Novel Modulator of Allergic Airway Inflammation and Neuropathic Pain.
Doyle, J. R.; Krishnaji, S. T.; Zhu, G.; Xu, Z.-Z.; Heller, D.; Ji, R.-R.; Levy, B. D.; Kumar, K.; Kopin, A. J. Biol. Chem. 2014, 289 (19), 13385–13396. [PubMed]
2013 – 2011
Colocalization of the Ganglioside GM1 and Cholesterol Detected by Secondary Ion Mass Spectrometry.
Lozano, M. M.; Liu, Z.; Sunnick, E.; Janshoff, A.; Kumar, K.; Boxer, S. G. J. Am. Chem. Soc. 2013, 135 (15), 5620–5630. [PubMed]
Fluorogenic Sialic Acid Glycosides for Quantification of Sialidase Activity upon Unnatural Substrates.
Zamora, C. Y.; d’Alarcao, M.; Kumar, K. Bioorg. Med. Chem. Lett. 2013, 23 (11), 3406–3410. [PubMed]
Fluorination in the Design of Membrane Protein Assemblies.
Krishnamurthy, V. M.; Kumar, K. Methods Mol. Biol. 2013, 1063, 227-243. [PubMed]
Ligand-Induced Protein Mobility in Complexes of Carbonic Anhydrase II and Benzenesulfonamides with Oligoglycine Chains.
Krishnamurthy, V. M.; Raman, V. S.; Mowery, R. A.; Hentz, M.; Baleja, J. D.; Shaw, B. F.; Kumar, K. PLoS One 2013, 8 (3), e57629. [PubMed]
Cross-Strand Interactions of Fluorinated Amino Acids in β-Hairpin Constructs.
Clark, G. A.; Baleja, J. D.; Kumar, K. J. Am. Chem. Soc. 2012, 134 (43), 17912–17921. [PubMed]
A Model System for Cell Adhesion Mediated by Weak Carbohydrate-Carbohydrate Interactions.
Lorenz, B.; de Cienfuegos, L. Á.; Oelkers, M.; Kriemen, E.; Brand, C.; Stephan, M.; Sunnick, E.; Yüksel, D.; Kalsani, V.; Kumar, K.; et al. J. Am. Chem. Soc. 2012, 134 (7), 3326–3329. [PubMed]
Chemical Biology Using Fluorinated Building Blocks.
Zamora, C. Y.; Dafik, L.; Kumar, K. in Supramolecular Chemistry: From Molecules to Nanomaterials. Gale, P. A. and Steed, J. W. Eds., John Wiley & Sons 2012, Chichester, UK, 1947-1964.
2010 – 2008
β-Peptide Bundles with Fluorous Cores.
Molski, M. A.; Goodman, J. L.; Craig, C. J.; Meng, H.; Kumar, K.; Schepartz, A. J. Am. Chem. Soc. 2010, 132 (11), 3658–3659. [PubMed]
Modulation of Cellular Adhesion by Glycoengineering.
Dafik, L.; d’Alarcao, M.; Kumar, K.J. Med. Chem. 2010, 53 (10), 4277–4284. [PubMed]
Trifluoromethyl Derivatization of the Ganglioside, GM1.
Liu, Z.; Kumar, K. Synthesis. 2010, 1905–1908.
A New Paradigm for Protein Design and Biological Self-Assembly.
Akçay, G.; Kumar, K. J. Fluor. Chem. 2009, 130 (12), 1178–1182. [PebMed]
Fluorinated Lipid Constructs Permit Facile Passage of Molecular Cargo into Living Cells.
Dafik, L.; Kalsani, V.; Leung, A. K. L.; Kumar, K. J. Am. Chem. Soc. 2009, 131 (34), 12091–12093. [PubMed]
Protein Design Using Non-Canonical Amino Acids.
Yüksel,D.; Pamuk, D.; Ivanova, Y.; Kumar, K. in Protein Engineering and Design Park, S.; Cochran, J. Eds.,Taylor & Francis 2009, 205-222.
Lipopeptides Derived from HIV and SIV Mimicking the Prehairpin Intermediate of gp41 on Solid Supported Lipid Bilayers.
Schuy, S.; Schäfer, E.; Yoder, N. C.; Kumar, K.; Vogel, R.; Janshoff, A. J. Struct. Biol. 2009, 168 (1), 125–136. [PubMed]
Fluorinated Amino Acids and Biomolecules in Protein Design and Chemical Biology.
Meng, H.; Clark, G. A.; Kumar, K. Fluorine in Medicinal Chemistry and Chemical Biology. Ojima, I. and Taguchi, T. Eds., John Wiley & Sons 2009, 411-446.
Engineering and Characterization of a Single Chain Surrogate Light Chain Variable Domain.
Morstadt, L.; Bohm, A.; Yüksel, D.; Kumar, K.; Stollar, B. D.; Baleja, J. D. Protein Sci. 2009, 17 (3), 458–465. [PubMed]
Biosynthesis and Stability of Coiled-Coil Peptides Containing (2S,4R)-5,5,5-Trifluoroleucine and (2S,4S)-5,5,5-Trifluoroleucine.
Montclare, J. K.; Son, S.; Clark, G. A.; Kumar, K.; Tirrell, D. A. ChemBioChem 2008, 10 (1), 84–86. [PubMed]
Coiled-Coil Lipopeptides Mimicking the Prehairpin Intermediate of Glycoprotein gp41.
Schuy, S.; Schäfer, E.; Yoder, N. C.; Hobe, S.; Kumar, K.; Vogel, R.; Janshoff, A. Angew. Chemie Int. Ed. 2008, 48 (4), 751–754. [PubMed]
Influence of Selective Fluorination on the Biological Activity and Proteolytic Stability of Glucagon-like Peptide-1.
Meng, H.; Krishnaji, S. T.; Beinborn, M.; Kumar, K. J. Med. Chem. 2008, 51 (22), 7303–7307. [PubMed]
Fluorination of Mammalian Cell Surfaces via the Sialic Acid Biosynthetic Pathway.
Dafik, L.; d’Alarcao, M.; Kumar, K. Bioorg. Med. Chem. Lett. 2008, 18 (22), 5945–5947. [PubMed]
Structure and Thermotropic Phase Behavior of Fluorinated Phospholipid Bilayers: A Combined Attenuated Total Reflection FTIR Spectroscopy and Imaging Ellipsometry Study.
Schuy, S.; Faiss, S.; Yoder, N. C.; Kalsani, V.; Kumar, K.; Janshoff, A.; Vogel, R. J. Phys. Chem. B 2008, 112 (28), 8250–8256. [PubMed]
Peptide Tertiary Structure Nucleation by Side-Chain Crosslinking with Metal Complexation and Double “Click” Cycloaddition.
Torres, O.; Yüksel, D.; Bernardina, M.; Kumar, K.; Bong, D. ChemBioChem 2008, 9 (11), 1701–1705. [PubMed]
2007 – 2005
Antimicrobial Activity and Protease Stability of Peptides Containing Fluorinated Amino Acids.
Meng, H.; Kumar, K. J. Am. Chem. Soc. 2007, 129 (50), 15615–15622. [PubMed]
Nanoscale Patterning in Mixed Fluorocarbon−Hydrocarbon Phospholipid Bilayers.
Yoder, N. C.; Kalsani, V.; Schuy, S.; Vogel, R.; Janshoff, A.; Kumar, K. J. Am. Chem. Soc. 2007, 129 (29), 9037–9043. [PubMed]
The Role of Conserved Histidines in the Structure and Stability of Human Papillomavirus Type 16 E2 DNA-Binding Domain.
Bose, K.; Yoder, N. C.; Kumar, K.; Baleja, J. D. Biochemistry 2007, 46 (5), 1402–1411. [PubMed]
Fluorinated Amino Acids and Reagents in Protein Design and Biomolecule Separation.
Meng, H.; Kalsani, V.; Kumar, K. In Current Fluoroorganic Chemistry; ACS Symposium Series; American Chemical Society, 2007; 949, 31–487.
Bioorthogonal Noncovalent Chemistry: Fluorous Phases in Chemical Biology.
Yoder, N. C.; Yüksel, D.; Dafik, L.; Kumar, K.Curr. Opin. Chem. Biol. 2006, 10 (6), 576–583. [PubMed]
Fluorinated Interfaces Drive Self-Association of Transmembrane α Helices in Lipid Bilayers.
Naarmann, N.; Bilgiçer, B.; Meng, H.; Kumar, K.; Steinem, C. Angew. Chemie Int. Ed. 2006, 45 (16), 2588–2591. [PubMed]
A Fluorous Capping Strategy for Fmoc-Based Automated and Manual Solid-Phase Peptide Synthesis.
Montanari, V.; Kumar, K. European J. Org. Chem. 2006, 4, 874–877.
Selective Protein−Protein Interactions Driven by a Phenylalanine Interface.
Yoder, N. C.; Kumar, K. J. Am. Chem. Soc. 2006, 128 (1), 188–191. [PubMed]
Enabling Routine Fluorous Capping in Solid Phase Peptide Synthesis.
Montanari, V.; Kumar, K. J. Fluor. Chem. 2006, 127 (4), 565–570.
Controlling Association of Vesicle Embedded Peptides by Alteration of the Physical State of the Lipid Matrix.
Naarmann, N.; Bilgiçer, B.; Kumar, K.; Steinem, C. Biochemistry 2005, 44 (13), 5188–5195. [PubMed]
2004 – 2000
De Novo Design of Defined Helical Bundles in Membrane Environments.
Bilgiçer, B.; Kumar, K. Proc. Natl. Acad. Sci. U. S. A. 2004, 101 (43), 15324-15329. [PubMed]
Alternative Translations of a Single RNA Message: An Identity Switch of (2S,3R)-4,4,4-Trifluorovaline between Valine and Isoleucine Codons.
Wang, P.; Fichera, A.; Kumar, K.; Tirrell, D. A. Angew. Chemie Int. Ed. 2004, 43 (28), 3664–3666. [PubMed]
Just Add Water: A New Fluorous Capping Reagent for Facile Purification of Peptides Synthesized on the Solid Phase.
Montanari, V.; Kumar, K. J. Am. Chem. Soc. 2004, 126 (31), 9528–9529. [PubMed]
A Highly Stereospecific and Efficient Synthesis of Homopentafluoro- Phenylalanine.
Babu, I. R.; Hamill, E. K.; Kumar, K. J. Org. Chem. 2004, 69 (16), 5468–5470. [PubMed]
Protein Design Using Unnatural Amino Acids.
Bilgiçer, B.; Kumar, K. J. Chem. Educ. 2003, 80 (11), 1275.
Fluorinated Amino Acids in Protein Design and Engineering.
Yoder, N. C.; Kumar, K. Chem. Soc. Rev. 2002, 31 (6), 335–341. [PubMed]
A Simple and Efficient Method for the Resolution of All Four Diastereomers of 4,4,4-Trifluorovaline and 5,5,5-Trifluoroleucine.
Xing, X.; Fichera, A.; Kumar, K. J. Org. Chem. 2002, 67 (5), 1722–1725. [PubMed]
Synthesis and Thermodynamic Characterization of Self-Sorting Coiled Coils.
Bilgiçer, B.; Kumar, K. Tetrahedron 2002, 58 (20), 4105–4112.
Programmed Self-Sorting of Coiled Coils with Leucine and Hexafluoroleucine Cores.
Bilgiçer, B.; Xing, X.; Kumar, K. J. Am. Chem. Soc. 2001, 123 (47), 11815–11816. [PubMed]
A Coiled Coil with a Fluorous Core.
Bilgiçer, B.; Fichera, A.; Kumar, K. J. Am. Chem. Soc. 2001, 123 (19), 4393–4399. [PubMed]
A Novel Synthesis of Enantiomerically Pure 5,5,5,5‘,5‘,5‘-Hexafluoroleucine.
Xing, X.; Fichera, A.; Kumar, K. Org. Lett. 2001, 3 (9), 1285–1286. [PubMed]
Fluorophobic Acceleration of Diels−Alder Reactions.
Myers, K. E.; Kumar, K. J. Am. Chem. Soc. 2000, 122 (48), 12025–12026.