Publications

Potent and Prolonged Innate Immune Activation by Enzyme-Responsive Imidazoquinoline TLR7/8 Agonist Prodrug Vesicles. Wang B, Van Herck S, Chen Y, Bai X, Zhong Z, Deswarte K, Lambrecht BN, Sanders NN, Lienenklaus S, Scheeren HW, David SA, Kiessling F, Lammers T, De Geest BG, Shi Y. J. Am. Chem. Soc. 2020 Jun 30. doi: 10.1021/jacs.0c01928.

Control over Imidazoquinoline Immune Stimulation by pH-Degradable Poly(norbornene) Nanogels. Kockelmann J, Stickdorn J, Kasmi S, De Vrieze J, Pieszka M, Ng DYW, David SA, De Geest BG, Nuhn L. Biomacromolecules. 2020 Jun 8;21(6):2246-2257.

Potent Lymphatic Translocation and Spatial Control Over Innate Immune Activation by Polymer-Lipid Amphiphile Conjugates of Small-Molecule TLR7/8 Agonists. J De Vrieze, B Louage, K Deswarte, Z Zhong, R De Coen, S Van Herck, L Nuhn, C Kaas Frich, AN Zelikin, S Lienenklaus, NN Sanders, BN Lambrecht, SA David, BG De Geest BG. Angew Chem Int Ed Engl (2019) 58:15390-15395.

Transiently Thermoresponsive Acetal Polymers for Safe and Effective Administration of Amphotericin B as a Vaccine Adjuvant. S Van Herck, L Van Hoecke, B Louage, L Lybaert, R De Coen, S Kasmi, AP Esser-Kahn, SA David, L Nuhn, B Schepens, X Saelens & BG De Geest. Bioconjug. Chem. (2018) 29:748-760.

Potent anti-viral vaccine adjuvant based on pH-degradable nanogels with covalently linked small molecule imidazoquinoline TLR7/8 agonist. L Nuhn, L Van Hoecke, K Deswarte, B Schepens, Y Li, BN Lambrecht, S De Koker, SA David, X Saelens & BG De Geest. Biomaterials (2018) 178:643-651.

Transcriptomal signatures of vaccine adjuvants and accessory immunostimulation of sentinel cells by toll-like receptor 2/6 agonists. ACD Salyer & SA David. Hum. Vaccin. Immunother. (2018) 14:1686-1696.

Hyaluronic Acid Conjugates of TLR7/8 Agonists for Targeted Delivery to Secondary Lymphoid Tissue. E Yoo, ACD Salyer, MJH Brush, Y Li, KL Trautman, NM Shukla, A De Beuckelaer, S Lienenklaus, K Deswarte, BN Lambrecht, BG De Geest & SA David. Bioconjug. Chem. (2018) 29:2741-2754.

Nanoparticle-Conjugate TLR7/8 Agonist Localized Immunotherapy Provokes Safe Antitumoral Responses. L Nuhn, S De Koker, S Van Lint, Z Zhong, JP Catani, F Combes, K Deswarte, Y Li, BN Lambrecht, S Lienenklaus, NN Sanders, SA David, J Tavernier & BG De Geest. Adv. Mater. (2018) 30:e1803397.

Lymph-Node-Targeted Immune Activation by Engineered Block Copolymer Amphiphiles-TLR7/8 Agonist Conjugates. S Van Herck, K Deswarte, L Nuhn, Z Zhong, JP Catani, Y Li, NN Sanders, S Lienenklaus, S De Koker, BN Lambrecht, SA David & BG De Geest. J. Am. Chem. Soc. (2018)  140:14300-14307.

Structural Analyses of Toll-like Receptor 7 Reveal Detailed RNA Sequence Specificity and Recognition Mechanism of Agonistic Ligands. Zhang Z, Ohto U, Shibata T, Taoka M, Yamauchi Y, Sato R, Shukla NM, David SA, Isobe T, Miyake K & Shimizu T. Cell Rep. (2018) 25:3371-3381.

Identification of Human Toll-like Receptor 2-Agonistic Activity in Dihydropyridine-Quinolone Carboxamides. Z Hu, J Banothu, M Beesu, CJ Gustafson, MJH Brush, KL Trautman, ACD Salyer, B Pathakumari, & SA David. ACS Med. Chem. Lett. (2018) 10:132-136.

Syntheses of Human TLR8-Specific Small-Molecule Agonists. M Beesu, HP Kokatla & SA David. Methods Mol. Biol. (2017)1494:29-44.

Identification of High-potency Human TLR8 and Dual TLR7/TLR8 Agonists in Pyrimidine-2,4-diamines. M Beesu, AC Salyer, MJ Brush, KL Trautman, JK Hill & SA David. J Med. Chem. (2017) 60:2084-2098.

Identification of Adjuvantic Activity of Amphotericin B in a Novel, Multiplexed, Poly-TLR/NLR High-Throughput Screen. AC Salyer, G Caruso, KK Khetani, LM Fox, SS Malladi & SA David. PLoS One. (2016)11(2):e0149848.

Identification of a Human Toll-Like Receptor (TLR) 8-Specific Agonist and a Functional Pan-TLR Inhibitor in 2-Aminoimidazoles. M Beesu, G Caruso, AC Salyer, NM Shukla, KK Khetani, LJ Smith, LM Fox, H Tanji, U Ohto, T Shimizu & SA David. J. Med. Chem. (2016) 59:3311-30.

pH-degradable imidazoquinoline-ligated nanogels for lymph node-focused immune activation. L Nuhn, N Vanparijs, A De Beuckelaer, L Lybaert, G Verstraete, K Deswarte, S Lienenklaus, NM Shukla, AC Salyer, BN Lambrecht, J Grooten, SA David, S De Koker & BG De Geest. Proc. Natl. Acad. Sci. USA. (2016) 113:8098-103.

Human Toll-like Receptor (TLR) 8-Specific Agonistic Activity in Substituted Pyrimidine-2,4-diamines. M Beesu, AC Salyer, KL Trautman, JK Hill & SA David. J. Med. Chem. (2016) 59:8082-93.

The Imidazoquinoline Toll-Like Receptor-7/8 Agonist Hybrid-2 Potently Induces Cytokine Production by Human Newborn and Adult Leukocytes. L Ganapathi, S Van Haren, DJ Dowling, I Bergelson, NM Shukla, SS Malladi, R Balakrishna, H Tanji, U Ohto, T Shimizu, SA David & O Levy. PLoS One. (2015) 10:e0134640.

Structure-Based Design of Human TLR8-Specific Agonists with Augmented Potency and Adjuvanticity. M Beesu, G Caruso, AC Salyer, KK Khetani, D Sil, M Weerasinghe, H Tanji, U Ohto, T Shimizu & SA David. J. Med. Chem. (2015) 58:7833-49.

Structure-based Ligand Design of Novel Human Toll-like Receptor 8 Agonists. HP Kokatla, D Sil, H Tanji, U Ohto, SS Malladi, LM Fox, T Shimizu & SA David. ChemMedChem. (2014) 9:719-723.

Determinants of Activity at Human Toll-like Receptors 7 and 8: QSAR of Diverse Heterocyclic Scaffolds. E Yoo, DB Salunke, D Sil, X Guo, ACD Salyer, AR Hermanson, M Kumar, SS Malladi, R Balakrishna, WH Thompson, H Tanji, U Ohto, T Shimizu & SA David. J. Med. Chem. (2014) 57:7955-7970.

Human Toll-like Receptor 8-Selective Agonistic Activities in 1-Alkyl-1H-benzimidazol-2-amines. M Beesu, SS Malladi, CD Jones & SA David. J. Med. Chem. (2014) 57:7325-7341.

Toll-like receptor-8 agonistic activities in C2, C4, and C8 modified thiazolo[4,5-c]quinolines HP Kokatla, E Yoo, DB Salunke, D Sil, CF Ng, R Balakrishna, SS Malladi, LM Fox & SA David. Org. Biomol. Chem. (2013) 11:1179-1198.

Exquisite Selectivity For Human Toll-like Receptor 8 in Substituted Furo[2,3-c]quinolines. HP Kokatla, D Sil, SS Malladi, R Balakrishna, AR Hermanson, LM Fox, X Wang, A Dixit & SA David. J. Med. Chem. (2013) 56:6871-6885.

Design and Development of Hydrolytically-stable, Water-soluble, Human Toll-like Receptor 2-Specific, Monoacyl Lipopeptides as Candidate Vaccine Adjuvants. DB Salunke, SW Connelly, NM Shukla, AR Hermanson, LM Fox & SA David. J. Med. Chem. (2013) 56:5885-5900.

Structure-Activity Relationships in Toll-like Receptor 7 Agonistic 1H-Imidazo[4,5-c]pyridines. E Yoo, BM Crall, LM Fox, R Balakrishna, SS Malladi, AR Hermanson & SA David. Org. Biomol. Chem. (2013) 11:6526-6545.

TLR7- and TLR8-Modulatory Activities of dimeric Imidazoquinolines. NM Shukla, CA Mutz, SS Malladi, HJ Warshakoon, R Balakrishna & SA David. J. Med. Chem. (2012) 55:1106-1116.

Potent Adjuvantic Activity of a CCR1-agonistic Bis-Quinoline. R Ukani, TC Lewis , TP Day, W Wu, SS Malladi, HJ Warshakoon & SA David. Bioorg. Med. Chem. Lett. (2012) 22:293-295.

Structure-Activity Relationships in Human Toll-like Receptor 2-Specific Monoacyl Lipopeptides. DB Salunke, NM Shukla, E Yoo, BM Crall, R Balakrishna, SS Malladi & SA David. J. Med. Chem. (2012) 55:3353-3363.

Structure-activity relationships in human Toll-like receptor 8-active 2,3-diamino-furo[2,3-c]pyridines. DB Salunke, E Yoo, NM Shukla, R Balakrishna, SS Malladi, KJ Serafin, VW Day, X Wang & SA David. J. Med. Chem. (2012) 55:8137-8151.

Potent adjuvanticity of a pure TLR7-agonistic imidazoquinoline dendrimer. NM Shukla, DB Salunke, R Balakrishna, CA Mutz, SS Malladi & SA David. PLoS One. 2012;7(8):e43612. doi: 10.1371/journal.pone.0043612.

Structure-Activity Relationships in Nucleotide Oligomerization Domain-1 (Nod1)-Agonistic γ-Glutamyl-diaminopimelic Acid Derivatives. G Agnihotri, R Ukani, SS Malladi, HJ Warshakoon, R Balakrishna, X Wang & SA David. J. Med. Chem. (2011) 54:1490-1510.

Toward self-adjuvanting subunit vaccines: Model peptide and protein antigens incorporating covalently bound toll-like receptor-7 agonistic imidazoquinolines. NM Shukla, TC Lewis, TP Day, CA Mutz, R Ukani, CD Hamilton, R Balakrishna & SA David. Bioorg. Med. Chem. Lett. (2011) 21:3232-3236.

Preliminary Evaluation of a 3H Imidazoquinoline Library as Dual TLR7/TLR8 Antagonists. NM Shukla, S Malladi, V Day & SA David. Bioorg. Med. Chem. (2011) 19:3801-3811.

Structure-activity relationships in Toll-like receptor 2-agonists leading to simplified monoacyl lipopeptides. G Agnihotri, BM Crall, TC Lewis, TP Day, R Balakrishna, HJ Warshakoon, SS Malladi, & SA. David. J. Med. Chem. (2011) 54:8148-8160.

Regioisomerism-dependent TLR7 Agonism and Antagonism in an Imidazoquinoline. NM Shukla, MR Kimbrell, SS Malladi & SA David. Bioorg. Med. Chem. Lett. (2009) 19:2211-2214.

Structure-activity relationships in toll-like receptor-2 agonistic diacylthioglycerol lipopeptides. W Wu, R Li, SS Malladi, HJ Warshakoon, MR Kimbrell, MW Amolins, R Ukani, A Datta & SA David. J. Med. Chem. (2010) 53:3198-3213.

Immunoprofiling Toll-Like Receptor Ligands: Comparison of Immunostimulatory and Proinflammatory Profiles in ex vivo Human Blood Models. JD Hood, HJ Warshakoon, MR Kimbrell, NM Shukla, S Malladi, X Wang & SA David. Hum. Vacc. (2010) 6:322-325.

Structure-Activity Relationships in Human Toll-like Receptor 7-Active Imidazoquinoline Analogues. NM Shukla, SS Malladi, CA Mutz, R Balakrishna & SA David. J. Med. Chem. (2010) 53:3198-3213.

Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7. NM Shukla, CA Mutz, R Ukani, HJ Warshakoon, DS Moore & SA David. Bioorg. Med. Chem. Lett. (2010) 20:6384-6386.