Targets, Structures, and Recent Approaches in Malignant Melanoma Chemotherapy
Ana Marta Matos
Research Institute for Medicines and Pharmaceutical Sciences (i Med. UL), Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisbon (Portugal)
Search for more papers by this authorCorresponding Author
Dr. Ana Paula Francisco
Research Institute for Medicines and Pharmaceutical Sciences (i Med. UL), Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisbon (Portugal)
Research Institute for Medicines and Pharmaceutical Sciences (i Med. UL), Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisbon (Portugal)Search for more papers by this authorAna Marta Matos
Research Institute for Medicines and Pharmaceutical Sciences (i Med. UL), Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisbon (Portugal)
Search for more papers by this authorCorresponding Author
Dr. Ana Paula Francisco
Research Institute for Medicines and Pharmaceutical Sciences (i Med. UL), Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisbon (Portugal)
Research Institute for Medicines and Pharmaceutical Sciences (i Med. UL), Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisbon (Portugal)Search for more papers by this authorGraphical Abstract
Targeting malignancies: Discovery of the pathophysiological processes behind malignant metastatic melanoma has allowed the development of novel drugs that are selective for several molecular targets. Such drugs may lead to increased survival rates and improved quality of life for cancer patients. Identifying the best molecular targets should lay the groundwork for developing new effective chemotherapies.
Abstract
Malignant metastatic melanoma is one of the oncologic diseases with the worst clinical prognosis, due primarily to resistance phenomena against chemotherapeutic agents in current use. However, over the last few years, characterization of the molecular mechanisms involved in the development and progression of the disease has contributed to elucidation of the main pathways by which tissue invasion and metastasis can occur. More importantly, the identification of abnormalities in signaling cascades in melanoma cells has facilitated new therapeutic approaches against malignant melanoma through the design of highly potent and selective drugs with low associated toxicity. Ultimately, recognition of the restricted applicability of new chemotherapies in certain genetic contexts has led to significant improvements in the results of clinical trials, anticipating the existing need for investment in personalized therapies, and taking into account the molecular alterations observed in tumors. Although significant advances have been made in terms of extending the median overall survival rate and improving the quality of life for patients, the mechanisms that compromise in vivo drug efficacy remain poorly understood, particularly those concerning therapeutic resistance phenomena. This review summarizes recently validated targets from the perspective of the medicinal chemistry carried out in the design of the most promising structures.
References
- 1R. Siegel, D. Naishadham, A. Jemal, CA Cancer J. Clin. 2012, 62, 10–29.
- 2R. Bestak, G. M. Halliday, Photochem. Photobiol. 1996, 64, 969–974.
- 3F. G. Haluska, F. S. Hodi, J. Clin. Oncol. 1998, 16, 670–682.
- 4J. A. Curtin, J. Fridlyand, T. Kageshita, H. N. Patel, K. J. Busam, H. Kutzner, K. H. Cho, S. Aiba, E. B. Brocker, P. E. LeBoit, D. Pinkel, B. C. Bastian, N. Engl. J. Med. 2005, 353, 2135–2147.
- 5I. J. Fiddler, Cancer Control 1995, 5, 398–404.
- 6M. C. J. Hendrix, E. A. Seftor, A. R. Hess, R. E. B. Seftor, Oncogene 2003, 22, 3070–3075.
- 7R. Mouawad, M. Sebert, J. Michels, J. Bloch, J. Spano, D. Khayat, Crit. Rev. Oncol. Hematol. 2010, 74, 27–39.
- 8
- 8aP. B. Chapman, A. Hauschild, C. Robert, J. B. Haanen, P. Ascierto, J. Larkin, R. Dummer, C. Garbe, A. Testori, M. Maio, D. Hogg, P. Lorigan, C. Lebbe, T. Jouary, D. Schadendorf, A. Ribas, S. J. O’Day, J. A. Sosman, J. M. Kirkwood, A. M. Eggermont, B. Dreno, K. Nolop, J. Li, B. Nelson, J. Hou, R. J. Lee, K. T. Flaherty, G. A. McArthur, New Engl. J. Med. 2011, 364, 2507–2516;
- 8bR. Nazarian, H. Shi, Q. Wang, X. Kong, R. C. Koya, H. Lee, Z. Chen, M. Lee, H. Sazegar, T. Chodon, S. F. Nelson, G. McArthur, J. A. Sosman, A. Ribas, R. S. Lo, Nature 2010, 468, 973–977.
- 9
- 9aG. Hill, E. Krementz, H. Hill, Cancer 1984, 53, 1299–1305;
10.1002/1097-0142(19840315)53:6<1299::AID-CNCR2820530613>3.0.CO;2-4 PubMedWeb of Science®Google Scholar
- 9bG. Q. Phan, P. Attia, S. M. Steinberg, D. E. White, S. A. Rosenberg, J. Clin. Oncol. 2001, 19, 3477–3482;
- 9cM. B. Atkins, M. T. Lotze, J. P. Dutcher, R. I. Fisher, G. Weiss, K. Margolin, J. Abrams, M. Sznol, D. Parkinson, M. Hawkins, C. Paradise, L. Kunkel, S. A. Rosenberg, J. Clin. Oncol. 1999, 17, 2105–2116.
- 10G. Palmieri, M. Capone, M. Ascierto, G. Gentilcore, D. Stroncek, M. Casula, M. Sini, M. Palla, N. Mozzillo, P. Ascierto, J. Transl. Med. 2009, 7, 86.
- 11M. Raman, W. Chen, M. H. Cobb, Oncogene 2007, 26, 3100–3112.
- 12M. S. Soengas, S. W. Lowe, Oncogene 2003, 22, 28–51.
- 13T. L. Hocker, M. K. Singh, H. Tsao, J. Invest. Dermatol. 2008, 128, 2575–2595.
- 14C. A. Lange-Carter, G. L. Johnson, Science 1994, 265, 1458–1461.
- 15B. Wehrle-Haller, Pigment Cell Res. 2003, 16, 287–296.
- 16V. A. Nikolaou, A. J. Stratigos, K. T. Flaherty, H. Tsao, J. Invest. Dermatol. 2012, 132, 854–863.
- 17C. Andre, A. Hampe, P. Lachaume, E. Martin, X. P. Wang, V. Manus, W. X. Hu, F. Galibert, Genomics 1997, 39, 216–226.
- 18M. S. Brose, P. Volpe, M. Feldman, M. Kumar, I. Rishi, R. Gerrero, E. Einhorn, M. Herlyn, J. Minna, A. Nicholson, J. Roth, S. Albelda, H. Davies, C. Cox, G. Brignell, P. Stephens, P. Futreal, R. Wooster, M. Stratton, B. Weber, Cancer Res. 2002, 62, 6997–7000.
- 19T. Whitwam, M. W. Vanbrocklin, M. E. Russo, P. T. Haak, D. Bilgili, J. H. Resau, H. M. Koo, S. L. Holmen, Oncogene 2007, 26, 4563–4570.
- 20A. Zebisch, J. Troppmair, Cell. Mol. Life Sci. 2006, 63, 1314–1330.
- 21H. Davies, G. R. Bignell, C. Cox, P. Stephens, S. Edkins, S. Clegg, J. Teague, H. Woffendin, M. J. Garnett, W. Bottomley, N. Davis, E. Dicks, R. Ewing, Y. Floyd, K. Gray, S. Hall, R. Hawes, J. Hughes, V. Kosmidou, A. Menzies, C. Mould, A. Parker, C. Stevens, S. Watt, S. Hooper, R. Wilson, H. Jayatilake, B. A. Gusterson, C. Cooper, J. Shipley, D. Hargrave, K. Pritchard-Jones, N. Maitland, G. Chenevix-Trench, G. J. Riggins, D. D. Bigner, G. Palmieri, A. Cossu, A. Flanagan, A. Nicholson, J. W. Ho, S. Y. Leung, S. T. Yuen, B. L. Weber, H. F. Seigler, T. L. Darrow, H. Paterson, R. Marais, C. J. Marshall, R. Wooster, M. R. Stratton, P. A. Futreal, Nature 2002, 417, 949–954.
- 22C. Hagemann, J. L. Blank, Cell Signalling 2001, 13, 863–875.
- 23Y. F. Wang, C. C. Jiang, K. A. Keijda, S. Gillespie, X. D. Zhang, P. Hersey, Clin. Cancer Res. 2007, 13, 4934–4942.
- 24E. Steingrímsson, N. G. Copeland, N. A. Jenkins, Annu. Rev. Genet. 2004, 38, 365–411.
- 25C. Levy, M. Khaled, D. E. Fischer, Trends Mol. Med. 2006, 12, 406–414.
- 26
- 26aS. Dalton, R. Treisman, Cell 1992, 68, 597–612;
- 26bT. Tanos, M. J. Marinissen, F. C. Leskow, D. Hochbaum, H. Martinetto, J. S. Gutkind, O. A. Coso, J. Biol. Chem. 2005, 280, 18842–18852.
- 27J. M. Stahl, A. Sharma, M. Cheung, M. Zimmerman, J. Q. Cheng, M. W. Bosenberg, M. Kester, L. Sandirasegarane, G. P. Robertson, Cancer Res. 2004, 64, 7002–7010.
- 28F. Meier, B. Schittek, S. Busch, C. Garbe, K. Smalley, K. Satyamoorthy, G. Li, M. Herlyn, Front. Biosci. 2005, 10, 2986–3001.
- 29
- 29aS. P. Staal, Proc. Natl. Acad. Sci. USA 1987, 84, 5034–5037;
- 29bM. Cheung, A. Sharma, S. V. Madhunapantula, G. P. Robertson, Cancer Res. 2008, 68, 3429–3439.
- 30
- 30aS. R. Datta, H. Dudek, X. Tao, S. Masters, H. Fu, Y. Gotoh, M. E. Greenberg, Cell 1997, 91, 231–241;
- 30bM. H. Cardone, N. Roy, H. R. Stennicke, G. S. Salvesen, T. F. Franke, E. Stanbridge, S. Frisch, J. C. Reed, Science 1998, 282, 1318–1321.
- 31A. Faissner, N. Heck, A. Dobbertin, J. Garwood, Adv. Exp. Med. Biol. 2006, 557, 25–53.
- 32J. E. Damen, L. Liu, P. Rosten, R. K. Humphries, A. B. Jefferson, P. W. Majerus, G. Krystal, Proc. Natl. Acad. Sci. USA 1996, 93, 1689–1693.
- 33H. B. Salvesen, N. MacDonald, A. Ryan, I. J. Jacobs, E. D. Lynch, L. A. Akslen, S. Das, Int. J. Cancer 2001, 91, 22–26.
- 34K. T. Flaherty, I. Puzanov, K. B. Kim, A. Ribas, J. A. McArthur, J. A. Sosman, P. J. O’Dwyer, R. J. Lee, J. F. Grippo, K. Nolop, P. B. Chapman, New Eng. J. Med. 2010, 363, 809–819.
- 35
- 35aS. J. Heidorn, C. Milagre, S. Whittaker, A. Nourry, I. Niculescu-Duvas, N. Dhomen, J. Hussain, J. S. Reis-Filho, C. J. Springer, C. Pritchard, R. Marais, Cell 2010, 140, 209–221;
- 35bG. Hatzivassiliou, K. Song, I. Yen, B. J. Brandhuber, D. J. Anderson, R. Alvarado, M. J. C. Ludlam, D. Stokoe, S. L. Gloor, G. Vigers, T. Morales, I. Aliagas, B. Liu, S. Sideris, K. P. Hoeflich, B. S. Jaiswal, S. Seshagiri, H. Koeppen, M. Belvin, L. S. Friedman, S. Malek, Nature 2010, 464, 431–435.
- 36A. Hauschild, S. S. Agarwala, U. Trefzer, D. Hogg, C. Robert, P. Hersey, A. Eggermont, S. Grabbe, R. Gonzalez, J. Gille, C. Peschel, D. Schadendorf, C. Garbe, S. O’Day, A. Daud, J. M. White, C. Xia, K. Patel, J. M. Kirkwood, U. Keilholz, J. Clin. Oncol. 2009, 27, 2823–2830.
- 37S. Wenglowsky, K. A. Ahrendt, A. J. Buckmelter, B. Feng, S. L. Gloor, S. Gradl, J. Grina, J. D. Hansen, E. R. Laird, P. Lunghofer, S. Mathieu, D. Moreno, B. Newhouse, L. Ren, T. Risom, J. Rudolph, J. Seo, H. L. Sturgis, W. C. Voegtli, Z. Wen, Bioorg. Med. Chem. Lett. 2011, 21, 5533–5537.
- 38S. Wenglowsky, D. Moreno, J. Rudolph, Y. Ran, K. A. Ahrendt, A. Arrigo, B. Colson, S. L. Gloor, G. Hastings, Bioorg. Med. Chem. Lett. 2012, 22, 912–915.
- 39M. Mathieu, S. N. Gradl, L. Ren, Z. Wen, I. Aliagas, J. Gunzner-Toste, W. Lee, R. Pulk, G. Zhao, B. Alicke, J. W. Boggs, A. J. Buckmelter, E. F. Choo, V. Dinkel, S. L. Gloor, S. E. Gould, J. D. Hansen, G. Hastings, G. Hatzivassiliou, E. R. Laird, D. Moreno, Y. Ran, W. C. Voegtli, S. Wenglowsky, J. Grina, J. Rudolph, J. Med. Chem. 2012, 55, 2869–2881.
- 40M. W. Rowbottom, R. Faraoni, Q. Chao, B. T. Campbell, A. G. Lai, E. Setti, M. Ezawa, K. G. Sprankle, S. Abraham, L. Tran, B. Struss, M. Gibney, R. C. Armstrong, R. N. Gunawardane, R. R. Nepomuceno, I. Valenta, H. Hua, M. F. Gardner, M. D. Cramer, D. Gitnick, D. E. Insko, J. L. Apuy, S. Jones-Bolin, A. K. Ghose, T. Herbertz, M. A. Ator, B. D. Dorsey, B. Ruggeri, M. Williams, S. Bhagwat, J. James, M. W. Holladay, J. Med. Chem. 2012, 55, 1082–1105.
- 41J. James, B. Ruggeri, R. C. Armstrong, M. W. Rowbottom, S. Jones-Bolin, R. N. Gunawardane, P. Dobrzanski, M. F. Gardner, H. Zhao, M. D. Cramer, K. Hunter, R. R. Nepomuceno, M. Cheng, D. Gitnick, M. Yazdanian, D. E. Insko, M. A. Ator, J. L. Apuy, R. Faraoni, B. D. Dorsey, M. Williams, S. S. Bhagwat, M. W. Holladay, Mol. Cancer Ther. 2012, 11, 930–941.
- 42D. B. Solit, L. A. Garraway, C. A. Pratilas, A. Sawai, G. Getz, A. Basso, Q. Ye, J. M. Lobo, Y. She, I. Osman, T. R. Golub, J. Sebolt-Leopold, W. R. Sellers, N. Rosen, Nature 2006, 439, 358–362.
- 43S. D. Barrett, A. J. Bridges, D. T. Dudley, A. R. Saltiel, J. H. Fergus, C. M. Flamme, A. M. Delaney, M. Kaufman, S. LePage, W. R. Leopold, S. A. Przybranowski, J. Sebolt-Leopold, K. Van Becelaere, A. M. Doherty, R. M. Kennedy, D. Marston, W. A. Howard, Y. Smith, Jr., J. S. Warmus, H. Tecle, Bioorg. Med. Chem. Lett. 2008, 18, 6501–6504.
- 44P. M. LoRusso, S. S. Krishnamurthi, J. J. Rinehart, L. M. Nabell, L. Malburg, P. B. Chapman, S. E. DePrimo, S. Bentivegna, K. D. Wilner, W. Tan, A. D. Ricart, Clin. Cancer Res. 2010, 16, 1924–1937.
- 45H. Abe, S. Kikuchi, K. Hayakawa, T. Iida, N. Nagahashi, K. Maeda, J. Sakamoto, N. Matsumoto, T. Miura, K. Matsumura, N. Seki, T. Inaba, H. Kawasaki, T. Yamaguchi, R. Kakefuda, T. Nanayama, H. Kurachi, Y. Hori, T. Yoshida, J. Kakegawa, Y. Watanabe, A. G. Gilmartin, M. C. Richter, K. G. Moss, S. G. Laquerre, ACS Med. Chem. Lett. 2011, 2, 320–324.
- 46J. R. Infante, L. A. Fecher, S. Nallapareddy, M. S. Gordon, K. T. Flaherty, D. S. Cox, D. J. DeMarini, S. R. Morris, H. A. Burris, W. A. Messersmith, J. Clin. Oncol. 2010, 28, 2503.
- 47J. G. Monzon, J. Dancey, OncoTargets Ther. 2012, 2, 31–46.
- 48G. P. Robertson, Cancer Metastasis Rev. 2005, 24, 273–285.
- 49
- 49aD. S. Ernst, E. Eisenhauer, N. Wainman, M. Davis, R. Lohmann, T. Baetz, K. Belanger, M. Smylie, Invest. New Drugs 2005, 23, 569–575;
- 49bS. K. Pal, K. Reckamp, H. Yu, R. A. Figlin, Expert Opin. Invest. Drugs 2010, 19, 1355–1366.
- 50A. W. Tolcher, T. A. Yap, I. Fearen, A. Taylor, C. Carpenter, A. T. Brunetto, M. Beeram, K. Papadopoulos, L. Yan, J. Bono, J. Clin. Oncol. 2009, 27, 3503.
- 51S. Chang, Z. Zhang, X. Zhuang, J. Luo, X. Cao, H. Li, Z. Tu, X. Lu, X. Ren, K. Ding, Bioorg. Med. Chem. Lett. 2012, 22, 1208–1212.
- 52Z. Xiao, Y. Hao, B. Liu, L. Qian, Leukemia Lymphoma 2002, 43, 1763–1768.
- 53G. Karapetyan, K. Chakrabarty, M. Hein, L. Langer, ChemMedChem 2011, 6, 25–37.
- 54M. Kunz, K. M. Driller, M. Hein, S. Libnow, I. Hohense, R. Ramer, B. Hinz, A. Berger, J. Eberle, P. Langer, ChemMedChem 2010, 5, 534–539.
- 55L. Liu, M. Kritsanida, P. Magiatis, N. Gaboriaud, Y. Wang, J. Wu, R. Buettner, F. Yang, S. Nam, L. Skaltsounis, R. Jove, Cancer Biol. Ther. 2012, 13, 1255–1261.
- 56
- 56aL. Liu, S. Nam, Y. Tian, F. Yang, J. Wu, Y. Wang, A. Scuto, P. Polychronopoulos, P. Magiatis, L. Skaltounis, R. Jove, Cancer Res. 2011, 71, 3972–3979;
- 56bF. Erben, D. Kleeblatt, M. Sonneck, M. Hein, H. Feist, T. Fahrenwaldt, C. Fischer, A. Matin, J. Iqbal, M. Plötz, J. Eberle, P. Langer, Org. Biomol. Chem. 2013, 11, 3963–3978.
- 57K. Vougogiannopoulou, A.-L. Skaltsounis, Planta Med. 2012, 78, 1515–1528.
- 58A. Berger, S.-A. Quast, M. Plötz, M. Hein, M. Kunz, P. Langer, J. Eberle, Biochem. Pharmacol. 2011, 81, 71–81.
- 59M. S. Neshat, I. K. Mellinghoff, C. Tran, B. Stiles, G. Thomas, R. Petersen, P. Frost, J. J. Gibbons, H. Wu, C. L. Sawyers, Proc. Natl. Acad. Sci. USA 2001, 98, 10314–10319.
- 60
- 60aK. Margolin, J. Longmate, T. Baratta, T. Synold, S. Christensen, J. Weber, T. Gajewski, I. Quirt, J. H. Doroshow, Cancer 2005, 104, 1045–1048;
- 60bR. D. Rao, H. E. Windschitl, J. B. Allred, V. J. Lowe, W. J. Maples, M. K. Gornet, V. J. Suman, E. T. Creagan, E. C. Pitot, S. N. Markovic, J. Clin. Oncol. 2006, 24, 8043.
- 61D. P. Sutherlin, L. Bao, M. Berry, G. Castanedo, I. Chuckowree, J. Dotson, A. Folks, L. Friedman, R. Goldsmith, J. Gunzner, T. Heffron, J. Lesnick, C. Lewis, S. Mathieu, J. Murray, J. Nonomiya, J. Pang, N. Pegg, W. W. Prior, L. Rouge, L. Salphati, D. Sampath, Q. Tian, V. Tsui, N. C. Wan, S. Wang, B. Wei, C. Wiesmann, P. Wu, B. Y. Zhu, A. Olivero, J. Med. Chem. 2011, 54, 7579–7587.
- 62A. J. Wagner, J. C. Bendell, S. Dolly, J. A. Morgan, J. A. Ware, J. Fredrickson, K. E. Mazina, J. E. Lauchle, H. A. Burris, J. S. De Bono, J. Clin. Oncol. 2011, 29, 3020.
- 63J. A. Curtin, K. Busam, D. Pinkel, B. C. Bastian, J. Clin. Oncol. 2006, 24, 4340–4346.
- 64E. Romano, G. K. Schwartz, P. B. Chapman, J. D. Wolchock, R. D. Carvajal, Lancet Oncol. 2011, 12, 913–922.
- 65S. Ugurel, R. Hildenbrand, A. Zimpfer, P. La Rosée, P. Paschka, A. Sucker, P. Keikavoussi, J. C. Becker, W. Rittgen, A. Hochhaus, D. Schadendorf, Br. J. Cancer 2005, 92, 1398–1405.
- 66R. D. Carvajal, C. R. Antonescu, J. D. Wolchok, P. B. Chapman, R. A. Roman, J. Teitcher, K. S. Panageas, K. J. Busam, B. Chmielowski, J. Lutzky, A. C. Pavlick, A. Fusco, L. Cane, N. Takebe, S. Vemula, N. Bouvier, B. C. Bastian, G. K. Schwartz, J. Am. Chem. Soc. 2011, 305, 2327–2334.
- 67H. M. Kluger, A. Z. Dudek, C. McCann, J. Ritacco, N. Southard, L. B. Jilaveanu, A. Molinaro, M. Sznol, Cancer 2011, 117, 2202–2208.
- 68S. E. Woodman, J. C. Trent, K. Stemke-Hale, A. J. Lazar, S. Pricl, G. M. Pavan, M. Fermeglia, Y. N. Gopal, D. Yang, D. A. Podoloff, D. Ivan, K. B. Kim, N. Papadopoulos, P. Hwu, G. B. Mills, M. A. Davies, Mol. Cancer Ther. 2009, 8, 2079–2085.
- 69D. Hananah, R. A. Weinberg, Cell 2011, 144, 646–674.
- 70E. K. Rofstad, E. F. Halsor, Cancer Res. 2000, 60, 4932–4938.
- 71S. Ugurel, G. Rappl, W. Tilgen, U. Reinhold, J. Clin. Oncol. 2001, 19, 577–583.
- 72D. G. Perez, V. J. Suman, T. R. Fitch, T. Amatruda, R. F. Morton, S. Z. Jilani, C. L. Constantinou, J. R. Egner, L. A. Kottschade, S. N. Markovic, Cancer 2009, 115, 119–127.
- 73M. González-Cao, S. Viteri, A. Díaz-Lagares, A. González, P. Redondo, Y. Nieto, J. Espinós, A. Chopitea, M. Ponz, S. Martín-Algarra, Oncology 2008, 74, 12–16.
- 74J. M. L. Ebos, R. S. Kerbel, Nat. Rev. Clin. Oncol. 2011, 8, 210–221.
- 75
- 75aR. L. Hudkins, N. C. Becknell, A. L. Zulli, T. L. Underiner, T. S. Angeles, L. D. Aimone, M. S. Albom, H. Chang, S. J. Miknyoczki, K. Hunter, S. Jones-Bolin, H. Zhao, E. R. Bacon, J. P. Mallamo, M. A. Ator, B. A. Ruggeri, J. Med. Chem. 2012, 55, 903–913;
- 75bM. Li, S. Wu, Z. Liu, W. Zhang, J. Xu, Y. Wang, J. Liu, D. Zhang, H. Tian, Y. Li, W. Ye, Biochem. Pharmacol. 2012, 83, 1251–1260;
- 75cV. Ferro, L. Liu, K. D. Johnstone, N. Wimmer, T. Karoli, P. Handley, J. Rowley, K. Dredge, C. P. Li, E. Hammond, K. Davis, L. Sarimaa, J. Harenberg, I. Bytheway, J. Med. Chem. 2012, 55, 3804–3813.