John R Falck
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John Russell (Camille) Falck
Personal: Born Dec. 2, 1948 in the then U.S.A. territory of Alaska, he lived in Kobe, Japan from age 6 months to 5 years where he attended first grade; subsequent primary and secondary schooling in Albuquerque, New Mexico. Married Elaine Renee Fogel (deceased 9/2008), sons Benjamin (b. 7/1989) and Aaron (b. 6/1991). He earned a B.Sc. and Ph.D. in Organic Chemistry from Colorado State University in 1970 and 1973, respectively, and the Diploma of Imperial College (DIC), London, England, in 1974.
Education/Training: Following postdoctoral studies with Nobel laureates Sir Derek H. R. Barton (Imperial College, London) and Elias J. Corey (Harvard Univ., Cambridge) as well as Theodore Cohen (Univ. Pittsburgh), he joined the faculty at the Univ of Texas Health Science Center at Dallas (now University of Texas Southwestern Medical Center) in 1979 where he spent his entire independent career. In 1997, he was appointed the Robert A. Welch Distinguished Chair in Chemistry. As of this writing, he has >800 peer-reviewed publications and 40 patents.
Scientific Contributions
(i) Cytochrome P450 (CYP) Eicosanoids (Third Branch of the Arachidonate Cascade): Soon after the initial reports of arachidonic acid (AA) metabolism by microsomal cytochromes P450 (P450), Dr. Falck played a pivotal role in the identification, synthesis, and delineation of the physiological and pathophysiological roles of these enzymes and their metabolites.1,2 In collaboration with the laboratory of Dr. Jorge H. Capdevila, his group was instrumental in the initial structural characterization of 5,6-, 8,9-, 11,12- and 14,15-epoxyeicosatrienoic acids (EETs) and of 19-, and 20-hydroxyeicosatetraenoic acids (19- and 20-HETE) as products of the epoxygenase and ω/ω-1 hydroxylase branches, respectively, of the CYP AA Monooxygenase Pathway. Dr. Falck’s elucidation of the structures, relative and absolute stereochemistries,3-6 and synthesis of all primary7-12 and many secondary13-16 metabolites of the P450 monooxygenase were essential steps during the subsequent development of analytical methods17-22 for their characterization as products of the in vivo metabolism of AA,23-28 the identification of the P450 isozymes participating in their formation, and the definition of their product selectivity,29 and regulatory control.30-32 This accumulated knowledge and Dr. Falck’s early grasp of their potential biological relevance33 has been, and continues to be the motivation for the many functional studies that contributed to our present understanding of the physiological and/or pathophysiological significance of AA monooxygenase pathway.34-40 More recently, these studies have been greatly facilitated by Dr. Falck’s studies of metabolite structure-activity relationships (SARs)41 that resulted in the introduction of several stable EET and 20-HETE agonist and antagonist analogs,42-49 selective biosynthesis inhibitor,50,51 and ultimately delved into the mechanisms and sites of action of the metabolites.52-55
(ii) Total Syntheses: A hallmark of the Falck lab’s approach to natural product total synthesis was the integration of new methodology and/or novel strategies into the synthetic design, e.g., morphinanedienone alkaloids,56 hydrastine,57 (±)-14-epicorynoline and O-methylarnottianamide,58 (+)-dihydrocompactin,59 (+)-dihydromevinolin,60 (-)-warburganal,61 (-)-stypoldione,62 (+)-goniofufurone,63 chiral inositol polyphosphate diphosphates,64 (+)- and (-)-FR-900848,65 curacin A,66 (±)-halomon,67 (+)-fostriecin,68 perillene and dendrolasin,69 constanolactones A and B,70 vancomycin B2,71 and FR252921.72
(iii) Synthetic Methodology/Biochemical Reagents: Contributions range from organometallic reagents/procedures, amination methodology, and novel cycloadditions73-80 to medicinal methodology and reagents to address biological applications.81-85
References[edit]
1. Capdevila, J.; Yadagiri, P.; Manna, S.; Falck, J.R., Absolute Configuration of the
Hydroxyeicosatetraenoic Acids (HETEs) Formed During Catalytic Oxygenation of Arachidonic Acid by Microsomal Cytochrome P-450. Biochem. Biophys. Res. Comm. 141: 1007-1011, 1986.
2. Chacos, N; Falck, J.R.; Wixtrom, C.; Capdevila, J., Novel Epoxides Formed During the Liver Cytochrome P-450 Oxidation of Arachidonic Acid. Biochem. Biophys. Res. Comm. 104: 916-922, 1982. PMID: 6803794.
3. Falck, J.R.; Manna, S.; Capdevila, J., Enantiospecific Synthesis of Methyl 11,12- and 14,15-Epoxyeicosatrienoate. Tetrahedron Lett. 25: 2443-2446, 1984.
4. Falck, J.R.; Manna, S.; Jacobson, H.R.; Estabrook, R.W.; Chacos, N.; Capdevila, J., Absolute Configuration of Epoxyeicosatrienoic Acids (EETs) Formed During Catalytic Oxygenation of Arachidonic Acid By Purified Rat Liver Microsomal Cytochrome P- 450. J. Am. Chem. Soc. 106: 3334-3336, 1984.
5. Moustakis, C.A; Viala, J.; Capdevila, J.; Falck, J.R., Total Synthesis of the Cytochrome P-450 Epoxygenase Metabolites 5(R),6(S)-, 5(S),6(R)-, and 14(R),15(S)-Epoxyeicosatrienoic Acid (EET) and Hydration Products 5(R),6(R)- and 14(R),15(R)-Dihydroxyeicosatrienoic Acid (DHET). J. Am. Chem. Soc. 107: 5283-5285, 1985.
6. Mosset, P.; Yadagiri, P.; Lumin, S.; Capdevila, J.; Falck, J.R., Arachidonate Epoxygenase: Total Synthesis of Both Enantiomers of 8,9- and 11,12-Epoxyeicosatrienoic Acid. Tetrahedron Lett. 27: 6035-6038, 1986.
7. Falck, J.R.; Manna, S., 8,9-Epoxyarachidonic Acid: A Cytochrome P-450 Metabolite. Tetrahedron Lett. 23: 1755-1756, 1982.
8. Manna, S.; Falck, J.R.; Chacos, N.; Capdevila, J., Synthesis of Arachidonic Acid Metabolites Produced by Purified Kidney Cortex Microsomal Cytochrome P-450. Tetrahedron Lett. 24: 33-36, 1983.
9. Falck, J.R.; Lumin, S.; Blair, I.; Dishman, E.; Martin, M.V.; Waxman, D.J.; Guengerich, F.P.; Capdevila, J.H., Cytochrome P-450-Dependent Oxidation of Arachidonic Acid to 16-, 17-, and 18-Hydroxyeicosatetraenoic Acids. J. Biol. Chem. 265: 10244-10249, 1990.
10. Falck, J.R.; Lumin, S.; Lee, S.-G.; Heckmann, B.; Mioskowski, C.; Karara, A.; Capdevila, J., Enantiospecific Synthesis of 17- and 18-Hydroxyeicosatetraenoic Acids, Cytochrome P450 Arachidonate Metabolites. Tetrahedron Lett. 33: 4893-4896, 1992.
11. Bednar, M.M.; Gross, C.E.; Balazy, M.K.; Belosludtsev, Y.; Colella, D.T.; Falck, J.R.; Balazy, M., 16(R)-Hydroxy-5,8,11,14-eicosatetraenoic Acid, a New Arachidonate Metabolite in Human Polymorphonuclear Leukocytes. Biochem. Pharm. 60: 447-455, 2000.
12. Reddy, Y.K.; Reddy, L.M.; Capdevila, J.H.; Falck, J.R., Practical, Asymmetric Synthesis of 16-Hydroxyeicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic Acid (16-HETE), an Endogenous Inhibitor of Neutrophil Activity. Bioorg. Med. Chem. Lett. 13: 3719-3720, 2003.
13. Spearman, M.E.; Prough, R.A.; Estabrook, R.W.; Falck, J.R.; Manna, S.; Leibman, K.C.; Murphy, R.C.; Capdevila, J., Novel Glutathione Conjugates formed from Epoxyeicosatrienoic Acids (EETs). Arch. Biochem. Biophys. 242: 225-230, 1985.
14. Manna, S.; Viala, J.; Yadagiri, P.; Falck, J.R., Synthesis of 12(S),20- ,12(S),19(R)-, and 12(S),19(S)-Dihydroxyeicosa-cis-5,8,14-trans-10-tetraenoic Acids, Metabolites of 12(S)-HETE. Tetrahedron Lett. 27: 2679-2682, 1986.
15. Capdevila, J.H.; Mosset, P.; Yadagiri, P.; Lumin, S.; Falck, J.R., NADPH-Dependent Microsomal Metabolism of 14,15-Epoxyeicosatrienoic Acid to Diepoxides and Epoxyalcohols. Arch. Biochem. Biophys. 261: 122-133, 1988.
16. Falck, J.R.; Reddy, L.M.; Byun, K.; Campbell, W.B.; Yi, X.-Y., Epoxygenase Eicosanoids: Synthesis of Tetrahydrofuran-diol Metabolites and their Vasoactivity. Bioorg. Med. Chem. Lett. 17: 2634-2638, 2007.
17. Hammonds, T.D.; Blair, I.A.; Falck, J.R.; Capdevila, J.H., Resolution of Epoxyeicosatrienoate Enantiomers by Chiral Phase Chromatography. Anal. Biochem. 182: 300-303, 1989.
18. Schwartzman, M.L.; Omata, K.; Lin, F.; Bhatt, R.K.; Falck, J.R.; Abraham, N.G., Detection of 20-Hydroxyeicosatetrenoic Acid in Rat Urine. Biochem. Biophys. Res. Comm. 180: 445-449, 1991.
19. Capdevila, J.H.; Wei, S.; Kumar, A.; Kobayashi, J.; Snapper, J.R.; Zeldin, D.; Bhatt, R.K.; Falck, J., Resolution of Dihydroxyeicosanoates and of Dihydroxyeicosatrienoates by Chiral Phase Chromatography. Anal. Biochem. 207: 236-240, 1992.
20. Grates, H.E.; McGowen, R.M.; Gupta, S.V.; Falck, J.R.; Brown, T.R.; Callewaert, D.M.; Sasaki, D.M., Quantification of 20-Hydroxyeicosatetraenoic Acid by Colorimetric Competitive Enzyme Linked Immunosorbent Assay. J. Biosci. 28: 109-113, 2003.
21. Zghibeh, C.M.; Gopal, V.R.; Poff, C.D.; Falck, J.R.; Balazy, M., Determination of trans-Arachidonic Acid Isomers in Human Blood Plasma. Anal. Biochem. 332: 137-144, 2004.
22. Wei, S.; Brittin, J.J.; Falck, J.R.; Anjaiah, S.; Nithipatikom, K.; Cui, L.; Campbell, W.B.; Capdevila, J.H., Chiral Resolution of the Epoxyeicosatrienoic Acids, Arachidonic Acid Epoxygenase Metabolites. Anal. Biochem. 352: 129-134, 2006.
23. Capdevila, J.; Pramanik, B.; Napoli, J.L.; Manna, S.; Falck, J.R., Arachidonic Acid Epoxidation: Epoxyeicosatrienoic Acids are Endogenous Constituents of Rat Liver. Arch. Biochem. Biophys. 231: 511-517, 1984.
24. Toto, R.; Siddhanta, A.; Manna, S.; Pramanik, B.; Falck, J.R.; Capdevila, J., Arachidonic Acid Epoxygenase: Detection of Epoxyeicosatrienoic Acids (EETs) in Human Urine. Biochim. Biophys. Acta 919: 132-139, 1987.
25. Falck, J.R; Schueler, V.J.; Jacobson, H.R.; Siddhanta, A.K.; Pramanik, B.; Capdevila, J., Arachidonate Epoxygenase: Identification of Epoxyeicosatrienoic Acids (EETs) in Rabbit Kidney. J. Lipid Res. 28: 840-846, 1987.
26. Capdevila, J.H.; Kishore, V; Dishman, E.; Blair, I.A.; Falck, J.R., A Novel Pool of Rat Liver Inositol and Ethanolamine Phospholipids Contains Epoxyeicosatrienoic Acids (EETs). Biochem. Biophys. Res. Comm. 146: 638-644, 1987.
27. Karara, A.; Dishman, E.; Blair, I.; Falck, J.R.; Capdevila, J.H., Endogenous Epoxyeicosatrienoic Acids (EETs): Cytochrome P-450 Controlled Stereoselectivity of the Hepatic Arachidonic Acid Epoxygenase. J. Biol. Chem. 264: 19822-19827, 1989.
28. Karara, A.; Dishman, E.; Falck, J.R.; Capdevila, J.H., Endogenous Epoxyeicosatrienoyl-phospholipids. A Novel Class of Cellular Glycerolipids Containing Epoxidized Arachidonate Moieties. J. Biol. Chem. 266: 7561-7569, 1991.
29. Capdevila, J.H.; Karara, A; Waxman, D.J.; Martin, M.V.; Falck, J.R.; Guenguerich, F.P., Cytochrome P-450 Enzyme-specific Control of the Regio- and Enantiofacial Selectivity of the Microsomal Arachidonic Acid Epoxygenase. J. Biol. Chem. 265:10865-10871, 1990.
30. Chacos, N.; Capdevila, J.; Falck, J.R.; Manna, S.; Martin-Wixtrom, C.; Gill, S.S.; Hammock, B.D.; Estabrook, R.W., The Reaction of Arachidonic Acid Epoxides (Epoxyeicosatrienoic Acids) with a Cytosolic Epoxide Hydrolase. Arch. Biochem. Biophys. 223: 639-648, 1983.
31. Zeldin, D.C.; Kobayashi, J.; Falck, J.R.; Winder, B.S.; Hammock, B.D.; Snapper, J.R.; Capdevila, J.H., Regio- and Enantiofacial Selectivity of Epoxyeicosatrienoic Acid Hydration by Cytosolic Epoxide Hydrolase. J. Biol. Chem. 268: 6402-6407, 1993.
32. Zeldin, D.C.; Wei, S.; Falck, J.R.; Hammock, B.D.; Snapper, J.R; Capdevila, J.H., Metabolism of Epoxyeicosatrienoic Acids by Cytosolic Epoxide Hydrolase: Substrate Structural Determinants of Asymmetric Catalysis. Arch. Biochem. Biophys. 316: 443- 451, 1995.
33. Escalante, B.; Erlij, D.; Falck, J.R.; McGiff, J.C., Effect of Cytochrome P450 Arachidonate Metabolites on Ion Transport in Rabbit Kidney Loop of Henle. Science 251: 799-802, 1991.
34. Snyder, G.D.; Capdevila, J.; Chacos, N.; Manna, S.; Falck, J.R., Action of Luteinizing Hormone-Releasing Hormone: Involvement of Novel Arachidonic Acid Metabolites. Proc. Natl. Acad. Sci. USA 80: 3504-3507, 1983.
35. Capdevila, J.; Chacos, N.; Falck, J.R.; Manna, S.; Negro-Vilar, A.; Ojeda, S.R., Novel Hypothalamic Arachidonate Products Stimulate Somatostatin Release from the Median Eminence. Endocrinology 113: 421-423, 1983.
36. Capdevila, J.; Snyder, G.D.; Falck, J.R., Epoxygenation of Arachidonic Acid by Rat Anterior Pituitary Microsomal Fractions. FEBS Lett. 178: 319-322, 1984.
37. Negro-Vilar, A.; Snyder, G.D.; Falck, J.R.; Manna, S.; Chacos, N.; Capdevila, J., Involvement of Eicosanoids in Release of Oxytocin and Vasopressin from the Neural Lobe of the Rat Pituitary. Endocrinology 116: 2663-2668, 1985.
38. Escalante, B.; Falck, J.R.; Yadagiri, P.; Sun, L.; Laniado-Schwartzman, M., 19(S)-Hydroxyeicosatetraenoic Acid is a Potent Stimulator of Renal Na+-K+-ATPase. Biochem. Biophys. Res. Comm. 152: 1269-1274, 1988.
39. Snyder, G.D.; Yadagiri, P.; Falck, J.R., Effect of Epoxyeicosatrienoic Acids on Growth Hormone Release from Somatotrophs. Am. J. Physiol. 256: E221-E226, 1989.
40. Campbell, W.B.; Falck, J.R.; Gauthier, K., Role of Epoxyeicosatrienoic Acids as Endothelium-Derived Hyperpolarizing Factor in Bovine Coronary Arteries. Med. Sci. Monit. 7: 578-584, 2001.
41. Bernstrom, K.; Malcolm, K.; McGee, J.; Maclouf, J.; Levy-Toledano, S.; Falck, J.R.; Fitzpatrick, F.A., 14,15-cis-Episulfide-eicosatrienoic Acid, an 'Epoxygenase' Eicosanoid Analog, Inhibits Ionophore- But Not Thrombin-Induced Platelet Aggregation. Molecular Pharm. 39: 114-119, 1991.
42. Wang, M.H.; Brand-Schieber, E.; Zand, B.A.; Nguyen, X.; Falck, J.R.; Balu, N.; Schwartzman, M.L., Cytochrome P450-Derived Arachidonic Acid Metabolism in the Rat Kidney: Characterization of Selective Inhibitors. J. Pharm. Exp. Therap. 284: 966- 973, 1998.
43. Gauthier, K.M.; Deeter, C.; Krishna, U.M.; Reddy, Y.K.; Bondlela, M.; Falck, J.R.; Campbell, W.B., 14,15-Epoxyeicosa-5(Z)-Enoic Acid: A Selective Epoxyeicosatrienoic Acid Antagonist that Inhibits Endothelium-Dependent Hyperpolarization and Relaxation in Coronary Arteries. Circ. Res. 90: 1028-1036, 2002.
44. Falck, J.R.; Krishna, U.M.; Reddy, Y.K.; Kumar, P.S.; Reddy, K.M.; Hittner, S.B.; Deeter, C.; Sharma, K.K.; Gauthier, K.M.; Campbell, W.B., Comparison of Vasodilatory Properties of 14,15-EET Analogs: Structural Requirements for Dilation. Am. J. Physiol. 284: H337-H349, 2003.
45. Yu, M.; Alonso-Galicia, M.; Sun, C.-W.; Roman, R.J.; Ono, N.; Hirano, H.; Ishimoto, T.; Reddy, Y.K.; Katipally, K.R.; Reddy, K.M.; Gopal, V.R.; Yu, J.; Takhi, M.; Falck, J.R., 20-Hydroxyeicosatetraenoic Acid (20-HETE): Structural Determinants for Renal Vasoconstriction. Bioorg. Med. Chem. 11: 2803-2821, 2003.
46. Falck, J.R.; Reddy, L.M.; Reddy, Y.K.; Bondlela, M.; Krishna, U.M.; Ji, Y.; Sun, J.; Liao, J.K., 11,12-Epoxyeicosatrienoic Acid (11,12-EET): Structural Determinants for Inhibition of TNF-α-Induced VCAM-1 Expression. Bioorg. Med. Chem. Lett. 13: 4011-4014, 2003.
47. Liu, Y.; Wang, R.; Li, J.; Rao, J.; Li, W.; Falck, J.R.; Manthati, V.L.; Medhora, M.; Jacobs, E.R.; Zhu, Falck, J.R.; Wallukat, G.; Puli, N.; Goli, M.; Arnold, C.; Konkel, A.; Rothe, M.; Fischer, R.; Muller, D.N.; Schunck, W.-H., 17(R),18(S)- Epoxyeicosatetraenoic Acid, a Potent Eicosapentaenoic Acid (EPA) Derived Regulator of Cardiomyocyte Contraction: Structure-Activity Relationships and Stable Analogues. J. Med. Chem. 54: 4109-4118, 2011.
48. Falck, J.R.; Koduru, S.R.; Mohapatra, S.; Manne, R.; Atcha, K.R.; Manthati, V.L.; Capdevila, J.H.; Christian, S.; Imig, J.D.; Campbell, W.B., 14,15-Epoxyeicosa-5,8,11- trienoic Acid (14,15-EET) Surrogates: Carboxylate Modifications. J. Med. Chem. 57:6965–6972, 2014.
49. Adebesin, A.M.; Wesser, T.; Vijaykumar, J.; Konkel, A.; Paudyal, M.; Lossie, J.; Zhu, C.; Westphal, C.; Puli, N.; Fischer, R.; Schunck, W.-H.; Falck, J.R., Development of Robust 17(R),18(S)-Epoxyeicosatetraenoic Acid (17,18-EEQ) Analogs as Potential Clinical Antiarrhythmic Agents. J. Med. Chem. 62: 10124−10143, 2019.
50. Falck, J.R.; Manna, S.; Viala, J.; Siddhanta, A.K.; Moustakis, C.A.; Capdevila, J., Arachidonate Epoxygenase: Inhibitors and Metabolite Analogues. Tetrahedron Lett. 26: 2287-2290, 1985.
51. Brand-Schieber, E.; Falck, J.R.; Schwartzman, M., Selective Inhibition of Arachidonic Acid Epoxidation in vivo. J. Physiol. Pharm. 51: 655-672, 2000.
52. Takahashi, K.; Capdevila, J.; Karara, A.; Falck, J.R.; Jacobson, H.R.; Badr, K.F., Cytochrome P-450 Arachidonate Metabolites in Rat Kidney: Characterization and Hemodynamic Responses. Am. J. Physiol. 258: F781-F789, 1990.
53. Wong, P. Y.-K.; Lin, K.T.; Iles, J.; Falck, J.R.; Yan, Y.T.; Shen, S.Y.; Ahern, D.; Bhatt, R.K., 14(R),15(S)-Epoxyeicosatrienoic Acid (14(R),(15(S)-EET) Receptor in Guinea-Pig Mononuclear Cell-Membranes. J. Lipid Mediators 6: 199-208, 1993.
54. Chen, Y.; Falck, J.R.; Manthati, V.L.; Jat, J.L.; Campbell, W.B., 20-Iodo-14,15- Epoxyeicosa-8(Z)-enoyl-3-azidophenylsulfonamide: Photoaffinity Labeling of a 14,15- Epoxyeicosatrienoic Acid Receptor. Biochemistry 50: 3840-3848, 2011.
55. Garcia, V.; Gilani, A.; Shkolnik, B.; Pandey, V.; Zhang, F.F.; Dakarapu, R.; Gandham, S.K.; Reddy, N.R.; Graves, J.P.; Gruzdev, A.; Zeldin, D.C.; Capdevila, J.H.; Falck, J.R.; Schwartzman, M.L., 20-HETE Signals Through G Protein-Coupled Receptor GPR75 (Gq) to Affect Vascular Function and Trigger Hypertension. Cir. Res. 120: 1776-1788, 2017.
56. Miller, L.L.; Stermitz, F.R.; Falck, J.R., Electrooxidative Cyclization of l-Benzyltetrahydroisoquinolines. A novel Nonphenolic Coupling Reaction. J. Am.Chem. Soc. 95: 2651-2656, l973.
57. Falck, J.R.; Manna, S., An Intramolecular Passerini Reaction: Synthesis of Hydrastine. Tetrahedron Lett. 22: 619-620, 1981.
58. Falck, J.R.; Manna, S.; Mioskowski, C., Isoquinolinium Cycloadditions: Total Synthesis of (±)-14-Epicorynoline and O-Methylarnottianamide. J. Am. Chem. Soc. 105: 631-633, 1983.
59. Yang, Y.-L.; Manna, S.; Falck, J.R., Total Synthesis of (+)-Dihydrocompactin. J. Am. Chem. Soc. 106: 3811-3814, 1984.
60. Falck, J.R.; Yang, Y.-L., Total Synthesis of (+)-Dihydromevinolin. Tetrahedron Lett. 25: 3563-3566, 1984.
61. Manna, S.; Yadagiri, P.; Falck, J.R., Terpenoid Precursors via Steroid Degradation: Synthesis of (-)-Warburganal. J.C.S. Chem. Commun.: 1324-1325, 1987.
62. Falck, J.R.; Chandrasekhar, S.; Manna, S.; Chiu, C.-C.S.; Mioskowski, C.; Wetzel, I., Total Synthesis of the Spiro-o-Benzoquinonefuran (-)-Stypoldione. J. Am. Chem. Soc. 115: 11606-11607, 1993.
63. Ye, J.; Bhatt, R.K.; Falck, J.R., Stereospecific α-Alkoxystannane Couplings with Acyl Chlorides: Total Synthesis of (+)-Goniofufurone. Tetrahedron Lett. 34: 8007-8010, 1993.
64. Falck, J.; Reddy, K.K.; Ye, J.; Saady, M.; Mioskowski, C.; Shears, S.B.; Tan, Z.; Safrany, S., Synthesis and Structure of Cellular Mediators: Inositol Polyphosphate Diphosphates. J. Am. Chem. Soc. 117: 12172-12175, 1995.
65. Falck, J.R.; Mekonnen, B.; Yu, J.; Lai, J.-Y. Synthesis of the Polycyclopropane Antibiotic FR-900848 via the Horeau Gambit. J. Am. Chem. Soc. 118: 6096-6097, 1996.
66. Lai, J.-Y.; Yu, J.; Mekonnen, B.; Falck, J.R., Synthesis of Curacin A, An Antimitotic Cyclopropane-Thiazoline From the Marine Cyanobacterium Lyngbya majuscula. Tetrahedron Lett. 37: 7167-7170, 1996.
67. Schlama, T.; Baati, R.; Gouverneur, V.; Valleix, A.; Falck, J.R.; Mioskowski, C., Total Synthesis of (±)-Halomon by a Johnson-Claisen Rearrangement. Angew. Chem. Int. Ed. 37: 2085-2087, 1998.
68. Reddy, Y. K.; Falck, J.R., Asymmetric Synthesis of (+)-Fostriecin. Org. Lett. 4: 969-971, 2002.
69. Barma, D. K.; Kundu, A.; Baati, R.; Mioskowski, C.; Falck, J.R., A Convenient Preparation of 3-Substituted Furans: Synthesis of Perillene and Dendrolasin. Org. Lett. 4: 1387-1389, 2002.
70. Yu, J.; Lai, J.-Y.; Ye, J.; Balu, N.; Reddy, M.; Duan, D.; Fogel, E.R.; Capdevila, J.H.; Falck, J.R., Chiral Cyclopropanes: Asymmetric Synthesis of Constanolactones A and B. Tetrahedron Lett. 43: 3939-3941, 2002.
71. Bolitt, V.; Mioskowski, C.; Kollah, R.O.; Manna, S.; Rajapaksa, D.; Falck, J.R., Total Synthesis of Vineomycinone B2 Methyl Ester via Double Bradsher Cyclization. J. Am. Chem. Soc. 113: 6320-6321, 1991.
72. Falck, J.R.; He, A.; Fukui, H.; Tsutsui, H.; Radha, A., Synthesis and Stereochemical Assignment of FR252921, a Promising Immunosuppressant. Angew. Chem. Int. Ed. 46: 4527-4529, 2007.
73. Ye, J.; Bhatt, R.K.; Falck, J.R., Stereospecific Palladium/Copper Co-Catalyzed Cross-Coupling of α-Alkoxy- and α-Aminostannanes with Acyl Chlorides. J. Am. Chem. Soc. 116: 1-5, 1994.
74. Falck, J. R.; Yu, J.; Cho, H.-S., A Convenient Synthesis of Unsymmetric Polyfluoroethers. Tetrahedron Lett. 35: 5997-6000, 1994.
75. Zhu, C.; Wang, R.; Falck, J.R., Mild and Rapid Hydroxylation of Aryl/Heteroaryl Boronic Acids and Boronate Esters with N-Oxides. Org. Lett. 14: 3494-3497, 2012.
76. Jat, J.L.; Paudyal, M.P.; Gao, H.; Xu, Q.-L.; Yousufuddin, M.; Devarajan, D.; Ess, D.H.; Kürti, L.; Falck, J.R., Direct Stereospecific Synthesis of Unprotected N-H and N-Me Aziridines from Olefins. Science 343: 61-65, 2014.
77. Paudyal, M.P.; Adebesin, A.M.; Burt, S.R.; Ess, D.H.; Ma, Z.; Kürti, L.; Falck, J.R., Dirhodium Catalyzed C-H Arene Amination using Hydroxylamines. Science 353:1144-1147, 2016.
78. Munnuri, S.; Adebesin, A.M.; Paudyal, M.P.; Yousufuddin, M.; Dalipe, A.; Falck, J.R., Catalyst-Controlled Diastereoselective Synthesis of Cyclic Amines via C–H Functionalization. J. Am. Chem. Soc. 139: 18288-18294, 2017.
79. Dakarapu, R.; Falck, J.R., Stereospecific Stille Cross-Couplings using Mn(II)Cl2. J. Org. Chem. 83: 1241-1251, 2018.
80. Anugu, R.R.; Munnuri, S.; Falck, J.R., Picolinate Directed Arene meta-C−H Amination via FeCl3 Catalysis. J. Am. Chem. Soc. 142: 5266-5271, 2020.
81. Falck, J.R.; Krieger, M.; Goldstein, J.L.; Brown, M.S., Preparation and Spectral Properties of Lipophilic Fluorescein Derivatives: Application to Plasma Low-Density Lipoprotein. J. Am. Chem. Soc. 103: 7396-7398, 1981.
82. Anderson, R.G.W.; Falck, J.R.; Goldstein, J.L.; Brown, M.S., Visualization of Acidic Organelles in Intact Cells by Electron Microscopy. Proc. Natl. Acad. Sci. USA 81:4838-4842, 1984.
83. Mosley, S.T.; Yang, Y.-L.; Falck, J.R.; Anderson, R.G.W., Receptor-Mediated Delivery of Photoprotective Agents by Low-Density Lipoprotein. Exp. Cell Res. 155:389-396, 1984.
84. Kho, Y.; Kim, S.C.; Jiang, C.; Barma, D.; Kwon, S.W.; Cheng, J.; Jaunbergs, J.; Weinbaum, C.; Tamanoi, F.; Falck, J.; Zhao, Y., A Tagging-via-substrate Technology for Detection and Proteomics of Farnesylated Proteins. Proc. Natl. Acad. Sci. USA 101: 12479-12484, 2004.
85. Nandi, A.; Sprung, R.; Barma, D.K.; Zhao, Y.; Kim, S.C.; Falck, J.R.; Zhao, Y., Global Identification of O-GlcNAc-Modified Proteins. Anal. Chem. 78: 452-458, 2006.
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