Synthesis and preclinical evaluation of QS-21 variants leading to simplified vaccine adjuvants and mechanistic probes. Chea, E. K.; Fernández-Tejada, A.; Damani, P.; Adams, M. M.; Gardner, J. R.; Livingston, P. O.; Ragupathi, G.; Gin, D. Y. J. Am. Chem. Soc. 2012, 134, 13448-13457.
A High-Throughput Scintillation Proximity-Based Assay for Human DNA Ligase IV. Tseng, H. M.; Shum, D.; Bhinder, B.; Escobar, S.; Veomett, N. J.; Tomkinson, A. E.; Gin, D. Y.; Djaballah, H.; Scheinberg, D. A. Assay Drug Dev. Technol. 2012, 10, 235-249.
Digoxin and its derivatives suppress TH17 cell differentiation by antagonizing RORγt activity. Huh, J. R.; Leung, M. W. L.; Huang, P.; Ryan, D. A.; Krout, M. R.; Malapaka, R.; Chow, J.; Manel, N.; Ciofani, M.; Kim, S. V.; Cuesta, A.; Santori, F. R.; Lafaille, J. J.; Xu, H. E.; Gin, D. Y.; Rastinejad, F.; Littman, D. R. Nature 2011, 472, 486-490.
Natural and Synthetic Saponin Adjuvant QS-21 for Vaccines Against Cancer. Ragupathi, G.; Gardner, J. R.; Livingston, P. O.; Gin, D. Y. Exp. Rev. Vaccines 2011, 10, 463-470..
Preclinical Evaluation of the Synthetic Adjuvant SQS-21 and its Constituent Isomeric Saponins. Ragupathi, G.; Damani, P.; Deng, K.; Adams, M. M.; Hang, J.; George, C.; Livingston, P. O.; Gin, D. Y. Vaccine 2010, 28, 4260-4267.
Annulation of Thioimidates and Vinyl Carbodiimides to Prepare 2-Aminopyrimidines, Competent Nucleophiles for Intramolecular Alkyne Hydroamination. Synthesis of (-)-Crambidine. Perl, N. R.; Ide, N. D.; Prajapati, S.; Perfect, H. H.; Durón; S. G.; Gin, D. Y. J. Am. Chem. Soc. 2010, 132, 1802-1803.
Design and Synthesis of Potent Quillaja Saponin Vaccine Adjuvants. Adams, M. M.; Damani, P.; Perl, N. R.; Won, A.; Hong, F.; Livingston, P. O.; Ragupathi, G.; Gin, D. Y. J. Am. Chem. Soc. 2010, 132, 1939-1945.
Immunologic and Biochemical Features of Human WT1 Peptide Epitope Analogs Containing Non-Natural Amino Acids. Gomez-Nunez, M.; Haro, K.; Dao, T.; Chau, D.; Won, A.; Escobar-Alvarez, S.; Zakhaleva, V.; Korontsvit, T.; Gin, D. Y.; Scheinberg, D. A. PLoS ONE 2008, 3, e3938.
Ring-Opening of Aziridine 2-Carboxamides with Carbohydrate C1-O-Nucleophiles. Stereoselective Preparation of alpha- and beta-O-Glycosyl Serine Conjugates. Ryan, D. A.; Gin, D. Y. J. Am. Chem. Soc. 2008, 130, 15228-15229.
Synthetic Access to the Chlorocyclopentane Cores of the Proposed Original and Revised Structures of Palau'amine. Bultman, M. S.; Ma, J.; Gin, D. Y. Angew. Chem., Int. Ed. 2008, 47, 6821-6824.
Synthesis of QS-21-Xylose. Establishing Immuno-Potentiating Activity of Synthetic QS-21 Adjuvant with a Melanoma Vaccine. Deng, K.; Adams, M. M.; Damani, P.; Livingston, P. O.; Ragupathi, G.; Gin, D. Y. Angew. Chem., Int. Ed. 2008, 47, 6395-6398.
Synthesis and Structure Verification of the Vaccine Adjuvant QS-7-Api. Synthetic Access to Homogeneous Quillaja saponaria Immunostimulants. Deng, K.; Adams, M. M.; Gin, D. Y. J. Am. Chem. Soc. 2008, 130, 5860-5861.
Synthesis of Anti-Proliferative Cephalotaxus Esters and Their Evaluation Against Several Human Hematopoietic and Solid Tumor Cell Lines. Ester Chain Structure in the Modulation of Multi-Drug Resistance. Eckelbarger, J. D.; Wilmot, J. T.; Epperson, M. T.; Thakur, C. S.; Shum, D.; Antczak, C.; Tarassishin, L.; Djaballah, H.; Gin, D. Y. Chem. Eur. J. 2008, 14, 4293-4306.
Application of an Intramolecular Dipolar Cycloaddition to an Asymmetric Synthesis of the Fully Oxygenated Tricyclic Core of the Stemofoline Alkaloids. Carra, R. J.; Epperson, M. T.; Gin, D. Y. Tetrahedron 2008, 64, 3629-3641.
Asymmetric Synthetic Access to the Hetisine Alkaloids. Total Synthesis of (+)-Nominine. Peese, K. M.; Gin, D. Y. Chem. Eur. J. 2008, 14, 1654-1665.
Chemical Glycosylation in the Synthesis of Glycoconjugate Antitumour Vaccines. Galoniæ, D. P.; Gin, D. Y. Nature 2007, 446, 1000-1007.
Total Synthesis of (+)-Batzelladine A and (-)-Batzelladine D via [4+2]-Annulation of Vinyl Carbodiimides with N-Alkyl Imines. Arnold, M. A.; Day, K. A.; Durón, S. G.; Gin, D. Y. J. Am. Chem. Soc. 2006, 128, 13255-13260.
Synthetic Studies of Complex Immunostimulants from Quillaja Saponaria. Synthesis of the Potent Clinical Immunoadjuvant QS-21Aapi. Kim, Y.-J.; Wang, P.; Navarro-Villalobos, M.; Rohde, B. D.; Derryberry, J.; Gin, D. Y. J. Am. Chem. Soc. 2006, 128, 11906-11915.
Strain-Release Rearrangement of N-Vinyl-2-Arylaziridines. Total Synthesis of the Anti-Leukemia Alkaloid (-)-Deoxyharringtonine. Eckelbarger, J. E.; Wilmot, J. T.; Gin, D. Y. J. Am. Chem. Soc. 2006, 128, 10370-10371.
Efficient Synthetic Access to the Hetisine C20-Diterpenoid Alkaloids. A Concise Synthesis of Nominine via Oxidoisoquinolinium-1,3-Dipolar and Dienamine-Diels-Alder Cycloadditions. Peese, K. M.; Gin, D. Y. J. Am. Chem. Soc. 2006, 128, 8734-8735.
Highly Convergent Synthesis of C3- or C2-Symmetric Carbohydrate Macrocycles. Bodine, K. D.; Gin, D. Y.; Gin, M. S. Org. Lett. 2005, 7, 4479-4482.
Conjugation of Selenols with Aziridine-2-Carboxylic Acid-Containing Peptides. Ide, N. D.; Galonic, D. P.; van der Donk, W. A.; Gin, D. Y. Synlett 2005, 2011-2014.
An Enantioselective Approach to the Hetisine Alkaloids. Synthesis of the 3-Methyl-1-aza-tricyclo[5.2.1.03,8]decane Core via Intramolecular Dipolar Cycloaddition. Peese, K. M.; Gin, D. Y. Org. Lett. 2005, 7, 3323-3325.
Sulfoxide Covalent Catalysis in Dehydrative Glycosylation. Probing the Mechanism of Hemiacetal Activation. Boebel, T. A.; Gin, D. Y. J. Org. Chem. 2005, 70, 5818-5826.
Aziridine-2-Carboxylic Acid Containing Peptides. Application to Solution- and Solid-Phase Convergent Site-Selective Peptide Modification. Galonic, D. P.; Ide, N. D.; van der Donk, W. A.; Gin, D. Y. J. Am. Chem. Soc. 2005, 127, 7359-7369. Research Highlights - Nature 2005, 435, 250-251.
Diastereoselective [4+2] Annulation of Vinyl Carbodiimides with N-Alkyl Imines. Asymmetric Synthetic Access to the Batzelladine Alkaloids. Arnold, M. A.; Durón, S. G.; Gin, D. Y. J. Am. Chem. Soc. 2005, 127, 6924-6925.
Site-Selective Conjugation of Thiols with Aziridine-2-Carboxylic Acid Containing Peptides. Galonic, D. P.; van der Donk, W. A.; Gin, D. Y. J. Am. Chem. Soc. 2004, 126, 12712-12713.
Synthesis of the Potent Immunostimulatory Adjuvant QS-21A. Wang, P.; Kim, Y.-J.; Navarro-Villalobos, M.; Rohde, B. D.; Gin, D. Y. J. Am. Chem. Soc. 2005, 127, 3256-3257. “Research Highlights” Nature 2005, 434, 290.
Synthesis of Readily Modifiable Cyclodextrin Analogs via Cyclodimerization of an Alkynyl-Azido Trisaccharide. Bodine, K. D.; Gin, D. Y.; Gin, M. S. J. Am. Chem. Soc. 2004, 126, 1638-1639.
Oligosaccharide-Peptide Ligation of Glycosyl Thiolates with Dehydropeptides. Synthesis of S-Linked Mucin Glycopeptide Conjugates. Galonic, D. P.; van der Donk, W. A.; Gin, D. Y. Chem. Eur. J. 2003, 9, 5997-6006.
Sulfoxide Covalent Catalysis. Application to Glycosidic Bond Formation. Boebel, T. A.; Gin, D. Y. Angew. Chem. Int. Ed. 2003, 42, 5874-5877.
Dehydrative Sialylation with C2-Hemiketal Donors. Haberman, J. M.; Gin, D. Y. Org. Lett. 2003, 5, 2539-2541.
C2-Acetamidomannosylation. Synthesis of 2-N-Acetylamino-2-Deoxy-alpha-D-Mannopyranosides with Glucal Donors. Liu, J.; Gin, D. Y. Tetrahedron Lett. 2003, 44, 4015-4018.
Dehydrative Glycosylation with 1-Hydroxy Donors. Gin, D. Y. J. Carbohydr. Chem. 2002, 21, 645-665.
C2-Amidoglycosylation. Scope and Mechanism of Nitrogen Transfer. Liu, J.; Gin, D. Y. J. Am. Chem. Soc. 2002, 124, 9789-9797.
C2-Hydroxyglycosylation with Glycal Donors. Probing the Mechanism of Sulfonium-Mediated Oxygen Transfer to Glycal Enol Ethers. Honda, E.; Gin, D. Y. J. Am. Chem. Soc. 2002, 124, 7343-7352.
Enantiospecific Synthesis of the Bridged Pyrrolizidine Core of Asparagamine A. Dipolar Cycloadditions of Azomethine Ylides Derived from the Sulfonylation of Vinylogous Amides. Epperson, M. T.; Gin, D. Y. Angew. Chem. Int. Ed. 2002, 41, 1778-1780.
Sulfide-Mediated Dehydrative Glycosylation with 1-Hydroxy Donors. Nguyen, H. M.; Chen, Y.; Durón, S. G.; Gin, D. Y. J. Am. Chem. Soc. 2001, 123, 8766-8772.
C(2)-Acyloxyglycosylation with Glycal Donors. Shi, L.; Kim, Y.-J.; Gin, D. Y. J. Am. Chem. Soc. 2001, 123, 6939-6940.
Synthesis of the Trisaccharide Portion of the Immunologic Adjuvant QS-21A via Sulfonium Mediated Oxidative and Dehydrative Glycosylation. Kim, Y.-J., Gin, D. Y. Org. Lett. 2001, 3, 1801-1804.
A New C(1)-Auxiliary for Anomeric Stereocontrol in the Synthesis of alpha-Sialyl Glycosides. Haberman, J. M.; Gin, D. Y. Org. Lett. 2001, 3, 1665-1668.
Asymmetric Synthesis and Determination of the Absolute Configuration of the Bicyclic Guanidine Core of Batzelladine A. Durón, S. G.; Gin, D. Y. Org. Lett. 2001, 3, 1551-1554.
Total Synthesis of (+)-Pyrenolide D. Engstrom, K. E.; Mendoza, M. R.; Navarro-Villalobos, M.; Gin, D. Y. Angew. Chem. Int. Ed. 2001, 40, 1128-1130.
Stereoselective Synthesis of 2-Hydroxy-alpha-Mannopyranosides from Glucal Donors. Kim, J.-Y.; Di Bussolo, V.; Gin, D. Y. Org. Lett. 2001, 3, 303-306.
Chemoselective Iterative Dehydrative Glycosylation. Nguyen, H. M.; Poole, J. L.; Gin, D. Y. Angew. Chem, Int. Ed. 2001, 40, 414-417.
Gin, D. Y. Dehydrative Glycosylation with 1-Hydroxy Donors. in: Glycochemistry: Principles, Synthesis and Applications; Wang, P. and Bertozzi, C.R., Ed.; Marcel Dekker, Inc.: New York, NY, 2001.
Synthesis of Glycosyl-1-Phosphates via Dehydrative Glycosylation. Garcia, B. A.; Gin, D. Y. Org. Lett. 2000, 2, 2135-2138.
Dehydrative Glycosylation with Activated Diphenyl Sulfonium Reagents. Scope, Mode of C(1)-Hemiacetal Activation, and Detection of Reactive Glycosyl Intermediates. Garcia, B. A.; Gin, D. Y. J. Am. Chem. Soc. 2000, 122, 4269-4279.
Acetamidoglycosylation with Glycal Donors. A One-Pot Glycosidic Coupling with Direct Stereoselective Installation of the C(2)-N-Acetylamino Functionality. Di Bussolo, V.; Liu, J.; Huffman, Jr., L. G.; Gin, D. Y. Angew. Chem. Int. Ed. 2000, 39, 204-207. “News of the Week” Chem. & Eng. News 2000, 78, 7-8.
Direct Oxidative Glycosylations with Glycal Donors. Di Bussolo, V.; Kim, Y.-J.; Gin, D. Y. J. Am. Chem. Soc. 1998, 120, 13515-13516.
Direct Glycosylations with 1-Hydroxy Glycosyl Donors Using Trifluoromethanesulfonic Anhydride and Diphenyl Sulfoxide. Garcia, B. A.; Poole, J. L.; Gin, D. Y. J. Am. Chem. Soc. 1997, 119, 7597-7598.
