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  1. 1.   alpha-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands
  2. Ann, Jihyae; Czikora, Agnes; Saini, Amandeep S.; Zhou, Xiaoling; Mitchell, Gary A.; Lewin, Nancy E.; Peach, Megan; Blumberg, Peter M.; Lee, Jeewoo
  3. Journal of Medicinal Chemistry. 2018, Jul 26; 61(14): 6261-6276.
  1. 2.   N-Methyl-Substituted Fluorescent DAG-Indololactone Isomers Exhibit Dramatic Differences in Membrane Interactions and Biological Activity
  2. Gal, N.; Kolusheva, S.; Kedei, N.; Telek, A.; Naeem, T. A.; Lewin, N. E.; Lim, L.; Mannan, P.; Garfield, S. H.; El Kazzouli, S.; Sigano, D. M.; Marquez, V. E.; Blumberg, P. M.; Jelinek, R.
  3. Chembiochem. 2011, Oct; 12(15): 2331-2340.
  1. 3.   Membrane anchoring of diacylglycerol lactones substituted with rigid hydrophobic acyl domains correlates with biological activities
  2. Raifman, O.; Kolusheva, S.; Comin, M. J.; Kedei, N.; Lewin, N. E.; Blumberg, P. M.; Marquez, V. E.; Jelinek, R.
  3. Febs Journal. 2010, Jan; 277(1): 233-243.
  1. 4.   Ceramides: Branched alkyl chains in the sphingolipid siblings of diacylglycerol improve biological potency
  2. Kang, J. H.; Garg, H.; Sigano, D. M.; Francella, N.; Blumenthal, R.; Marquez, V. E.
  3. Bioorganic & Medicinal Chemistry. 2009 17(4): 1498-1505.
  1. 5.   Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'
  2. Chen, J. Y.; Nikolovska-Coleska, Z.; Yang, C. Y.; Gomez, C.; Gao, W.; Krajewski, K.; Jiang, S.; Roller, P.; Wang, S. M.
  3. Bioorganic & Medicinal Chemistry Letters. 2007, Jul; 17(14): 3939-3942.
  1. 6.   Understanding how the herpes thymidine kinase orchestrates optimal sugar and nucleobase conformations to accommodate its substrate at the active site: A chemical approach
  2. Marquez, V. E.; Choi, Y.; Comin, M. J.; Russ, P.; George, C.; Huleihel, M.; Ben-Kasus, T.; Agbaria, R.
  3. Journal of the American Chemical Society. 2005, NOV 2; 127(43): 15145-15150.
  1. 7.   Examination of phosphoryl-mimicking functionalities within a macrocyclic Grb2 SH2 domain-binding platform
  2. Kang, S. U.; Shi, Z. D.; Worthy, K. M.; Bindu, L. K.; Dharmawardana, P. G.; Choyke, S. J.; Bottaro, D. P.; Fisher, R. J.; Burke, T. R.
  3. Journal of Medicinal Chemistry. 2005, JUN 16; 48(12): 3945-3948.
  1. 8.   Design and synthesis of conformationally constrained Grb2 SH2 domain binding peptides employing alpha-methylphenylalanyl based phosphotyrosyl mimetics
  2. Oishi, S.; Karki, R. G.; Kang, S. U.; Wang, X. Z.; Worthy, K. M.; Bindu, L. K.; Nicklaus, M. C.; Fisher, R. J.; Burke, T. R.
  3. Journal of Medicinal Chemistry. 2005, FEB 10; 48(3): 764-772.
  1. 9.   Structure-based design of potent, conformationally constrained Smac mimetics
  2. Sun, H. Y.; Nikolovska-Coleska, Z.; Yang, C. Y.; Xu, L.; Liu, M. L.; Tomita, Y.; Pan, H. G.; Yoshioka, Y.; Krajewski, K.; Roller, P. P.; Wang, S. M.
  3. Journal of the American Chemical Society. 2004, DEC 29; 126(51): 16686-16687.
  1. 10.   Conformationally constrained analogues of diacylglycerol (DAG). 23. Hydrophobic ligand-protein interactions versus ligand-lipid interactions of DAG-lactones with protein kinase C (PK-C)
  2. Tamamura, H.; Sigano, D. M.; Lewin, N. E.; Peach, M. L.; Nicklaus, M. C.; Blumberg, P. M.; Marquez, V. E.
  3. Journal of Medicinal Chemistry. 2004, SEP 23; 47(20): 4858-4864.
  1. 11.   Conformationally constrained diacylglycerol (DAG) analogs: 4-C-hydroxyethyl-5-O-acyl-2,3-dideoxy-D-glyceropentono-1,4-lactone analogs as protein kinase C (PKC) ligands
  2. Lee, J.; Kim, S. Y.; Kang, J. H.; Acs, G.; Acs, P.; Blumberg, P. M.; Marquez, V. E.
  3. European Journal of Medicinal Chemistry. 2004 39(1): 69-77.
  1. 12.   Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants
  2. Das, K.; Clark, A. D.; Lewi, P. J.; Heeres, J.; de Jonge, M. R.; Koymans, L. M. H.; Vinkers, H. M.; Daeyaert, F.; Ludovici, D. W.; Kukla, M. J.; De Corte, B.; Kavash, R. W.; Ho, C. Y.; Ye, H.; Lichtenstein, M. A.; Andries, K.; Pauwels, R.; de Bethune, M. P.; Boyer, P. L.; Clark, P.; Hughes, S. H.; Janssen, P. A. J.; Arnold, E.
  3. Journal of Medicinal Chemistry. 2004 47(10): 2550-2560.
  1. 13.   Conformationally constrained analogues of diacylglycerol. 20. The search for an elusive binding site on protein kinase C through relocation of the carbonyl pharmacophore along the sn-1 side chain of 1,2-diacylglycerol lactones
  2. Tamamura, H.; Sigano, D. M.; Lewin, N. E.; Blumberg, P. M.; Marquez, V. E.
  3. Journal of Medicinal Chemistry. 2004 47(3): 644-655.
  1. 14.   CD40 ligand dysregulation in HIV infection: HIV glycoprotein 120 inhibits signaling cascades upstream of CD40 ligand transcription
  2. Zhang, R.; Fichtenbaum, C. J.; Hildeman, D. A.; Lifson, J. D.; Chougnet, C.
  3. Journal of Immunology. 2004 172(4): 2678-2686.
  1. 15.   Conformationally constrained analogues of diacylglycerol. 21. A solid-phase method of synthesis of diacylglycerol lactones as a prelude to a combinatorial approach for the synthesis of protein kinase C isozyme-specific ligands
  2. Duan, D. H.; Lewin, N. E.; Sigano, D. M.; Blumberg, P. M.; Marquez, V. E.
  3. Journal of Medicinal Chemistry. 2004 47(12): 3248-3254.
  1. 16.   Synthesis and conformational analysis of a locked analogue of carbovir built on a bicyclo 3.1.0 hex-2-enyl template
  2. Choi, Y. S.; Sun, G. Y.; George, C.; Nicklaus, M. C.; Kelley, J. A.; Marquez, V. E.
  3. Nucleosides Nucleotides & Nucleic Acids. 2003 22(12): 2077-2091.
  1. 17.   Differential binding modes of diacylglycerol (DAG) and DAG lactones to protein kinase C (PK-C)
  2. Sigano, D. M.; Peach, M. L.; Nacro, K.; Choi, Y.; Lewin, N. E.; Nicklaus, M. C.; Blumberg, P. M.; Marquez, V. E.
  3. Journal of Medicinal Chemistry. 2003 46(9): 1571-1579.
  1. 18.   Rational design of drugs that induce human immunodeficiency virus replication
  2. Hamer, D. H.; Bocklandt, S.; McHugh, L.; Chun, T. W.; Blumberg, P. M.; Sigano, D. M.; Marquez, V. E.
  3. Journal of Virology. 2003 77(19): 10227-10236.
  1. 19.   Recent advances in the synthesis of confortnationally locked nucleosides and their success in probing the critical question of conformational preferences by their biological targets
  2. Choi, Y.; Moon, H. R.; Yoshimura, V.; Marquez, V. E.
  3. Nucleosides Nucleotides & Nucleic Acids. 2003 22(5-8): 547-557.
  1. 20.   Synthesis of conformationally locked carbocyclic nucleosides built on an oxabicyclo 3.1.0 hexane system
  2. Comin, M. J.; Rodriguez, J. B.; Russ, P.; Marquez, V. E.
  3. Tetrahedron. 2003 59(3): 295-301.
  1. 21.   Asymmetric synthesis of a conformationally locked carboxylic analog of L-3 '-deoxythymine that mimics the South conformation: Biological implications and enzyme recognition
  2. Choi, Y. S.; Comin, M. J.; Clifford, G.; Balzarini, J.; Marquez, V. E.
  3. Abstracts of Papers of the American Chemical Society. 2003 225(Part 2): U195-U195.
  1. 22.   Synthetic diacylglycerols (DAG) and DAG-lactones as activators of protein kinase C (PK-C)
  2. Marquez, V. E.; Blumberg, P. M.
  3. Accounts of Chemical Research. 2003 36(6): 434-443.
  1. 23.   Diacylglycerol (DAG)-lactones, a new class of protein kinase C (PKC) agonists, induce apoptosis in LNCaP prostate cancer cells by selective activation of PKC alpha
  2. Garcia-Bermejo, M. L.; Leskow, F. C.; Fujii, T.; Wang, Q. M.; Blumberg, P. M.; Ohba, M.; Kuroki, T.; Han, K. C.; Lee, J.; Marquez, V. E.; Kazanietz, M. G.
  3. Journal of Biological Chemistry. 2002 277(1): 645-655.
  1. 24.   Use of 3d Qsar Methodology For Data Mining the National Cancer Institute Repository of Small Molecules - Application to Hiv-1 Reverse Transcriptase Inhibition
  2. Gussio, R.; Pattabiraman, N.; Kellogg, G. E.; Zaharevitz, D. W.
  3. Methods (Duluth). 1998 14(3): 255-263.
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