1 Pichereau, C, Allary, C. Therapeutic peptides under the spotlight. Eur BioPharma Rev 2005, Winter 05.
2 Dimond, PF. Could stapling revive peptide therapeutics? Genetic Eng Biotechnol News 2010, September 20.
3 Glaser, V. Competition mounting in peptide market. Gen Eng Biotechnol News 2009, July 1, 29.
4 Torchilin, VP, Lukyanov, AN. Peptide and protein drug delivery to and into tumors: challenges and solutions. Drug Discov Today 2003, 8:259–266.
5 Bioseeker Group AB. Peptides in oncology drug pipeline update. Market research report. Report nr 171783, 2011.
6 Hamman, JH, Enslin, GM, Kotze, AF. Oral delivery of peptide drugs: barriers and developments. BioDrugs 2005, 19:165–177.
7 Langguth, P, Bohner, V, Heizmann, J, Merkle, HP, Wolffram, S, Amidon, GL, Yamashita, S. The challenge of proteolytic enzymes in intestinal peptide delivery. J Contr Release 1997, 46:39–57.
8 Yang, M, Frokjaer, S. Novel formulation approaches for peptide and protein injectables. Delivery Technologies for Biopharmaceuticals. John Wiley %26 Sons, Ltd
; 2009, 9–28.
9 Brown, LR. Commercial challenges of protein drug delivery. Expert Opin Drug Deliv 2005, 2:29–42.
10 Torchilin, VP. Intracellular delivery of protein and peptide therapeutics. Drug Disc Today: Technol 2008, 5:e95–e103.
11 Kelley, WS. Therapeutic peptides: the devil is in the detail. Nat Biotechnol 1996, 14:28–31.
12 Zega, A. Azapeptides as pharmacological agents. Curr Med Chem 2005, 12:589–597.
13 Ekici, OD, Gotz, MG, James, KE, Li, ZZ, Rukamp, BJ, Asgian, JL, Caffrey, CR, Hansell, E, Dvorak, J, McKerrow, JH, et al. Aza‐peptide michael acceptors: a new class of inhibitors specific for caspases and other clan CD cysteine proteases. J Med Chem 2004, 47:1889–1892.
14 Piliero, PJ. Atazanavir: a novel HIV‐1 protease inhibitor. Expert Opin Investig Drugs 2002, 11:1295–1301.
15 Tzefos, M, Harris, K, Brackett, A. Clinical efficacy and safety of once‐weekly glucagon‐like peptide‐1 agonists in development for treatment of type 2 diabetes mellitus in adults. Ann Pharmacother 2012, 46:68–78.
16 Deacon, CF. Circulation and degradation of GIP and GLP‐1. Horm Metab Res 2004, 36:761–765.
17 Tan, TM, Field, BC, Minnion, JS, Cuenco‐Shillito, J, Chambers, ES, Zac‐Varghese, S, Brindley, CJ, Mt‐Isa, S, Fiorentino, F, Ashby, D, et al. Pharmacokinetics, adverse effects and tolerability of a novel analogue of human pancreatic polypeptide, PP 1420. Br J Clin Pharmacol 2012, 73:232–239
18 Hostrup, S, Huus, K, Parshad, H. %22Modification of peptides and proteins.%22 Delivery Technologies for Biopharmaceuticals. John Wiley %26 Sons, Ltd
; 2009, 169–191.
19 Francesco, MV. Peptide and protein PEGylation: a review of problems and solutions. Biomaterials 2001, 22:405–417.
20 Kellam, B, Drouillat, B, Dekany, G, Starr, MS, Toth, I. Synthesis and in vitro evaluation of lipoamino acid and carbohydrate‐modified enkephalins as potential antinociceptive agents. Int J Pharm 1998, 161:55–64.
21 Toth, I, Flinn, N, Hillery, A, Gibbons, WA, Artursson, P. Lipidic conjugates of luteinizing hormone releasing hormone (LHRH)+ and thyrotropin releasing hormone (TRH)+ that release and protect the native hormones in homogenates of human intestinal epithelial (caco‐2) cells. Int J Pharm 1994, 105:241–247.
22 Toth, I, Malkinson, JP, Flinn, NS, Drouillat, B, Horvath, A, Erchegyi, J, Idei, M, Venetianer, A, Artursson, P, Lazorova, L, et al. Novel lipoamino acid‐ and liposaccharide‐based system for peptide delivery: application for oral administration of tumor‐selective somatostatin analogues. J Med Chem 1999, 42:4010–4013.
23 Bellmann‐Sickert, K, Elling, CE, Madsen, AN, Little, PB, Lundgren, K, Gerlach, LO, Bergmann, R, Holst, B, Schwartz, TW, Beck‐Sickinger, AG. Long‐acting lipidated analogue of human pancreatic polypeptide is slowly released into circulation. J Med Chem 2011, 54:2658–2667.
24 Yuan, L, Wang, J, Shen, WC. Reversible lipidization prolongs the pharmacological effect, plasma duration, and liver retention of octreotide. Pharm Res 2005, 22:220–227.
25 Cui, H, Webber, MJ, Stupp, SI. Self‐assembly of peptide amphiphiles: from molecules to nanostructures to biomaterials. Biopolymers 2010, 94:1–18.
26 Black, M, Trent, A, Kostenko, Y, Lee, JS, Olive, C, Tirrell, M. Self‐assembled peptide amphiphile micelles containing a cytotoxic T‐cell epitope promote a protective immune response in vivo. Adv Mater 2012. In press.
27 Kokkoli, E, Mardilovich, A, Wedekind, A, Rexeisen, E, Garg, A, Craig, J. Self‐assembly and applications of biomimetic and bioactive peptide‐amphiphiles. Soft Matter 2006, 2:1015–1024.
28 Nielsen, PE. Peptide nucleic acid: a versatile tool in genetic diagnostics and molecular biology. Curr Opin Biotechnol 2001, 12:16–20.
29 Del Pozo‐Rodriguez, A, Delgado, D, Solinis, MA, Gascon, AR. Lipid nanoparticles as vehicles for macromolecules: nucleic acids and peptides. Recent Pat Drug Deliv Formula 2011, 5:214–226.
30 Corradini, R, Sforza, S, Tedeschi, T, Totsingan, F, Manicardi, A, Marchelli, R. Peptide nucleic acids with a structurally biased backbone. updated review and emerging challenges. Curr Top Med Chem 2011, 11:1535–1554.
31 Shen, G, Fang, H, Song, Y, Bielska, AA, Wang, Z, Taylor, JS. Phospholipid conjugate for intracellular delivery of peptide nucleic acids. Bioconjug Chem 2009, 20:1729–1736.
32 Ali, M, Manolios, N. Peptide delivery systems. Lett Peptide Sci 2002, 8:289–294.
33 Lundstrom, K. %22Nanocarriers for the delivery of peptides and proteins.%22 Delivery Technologies for Biopharmaceuticals. John Wiley %26 Sons, Ltd
; 2009, 193–205.
34 Mao, S, Cun, D, Kawashima, Y. %22Novel non‐injectable formulation approaches of peptides and proteins.%22 Delivery Technologies for Biopharmaceuticals. John Wiley %26 Sons, Ltd
; 2009, 29–67.
35 Chen, MC, Wang, JL, Tzen, JT. Elevating bioavailability of cyclosporine a via encapsulation in artificial oil bodies stabilized by caleosin. Biotechnol Prog 2005, 21:1297–1301.
36 Soman, NR, Baldwin, SL, Hu, G, Marsh, JN, Lanza, GM, Heuser, JE, Arbeit, JM, Wickline, SA, Schlesinger, PH. Molecularly targeted nanocarriers deliver the cytolytic peptide melittin specifically to tumor cells in mice, reducing tumor growth. J Clin Invest 2009, 119:2830–2842.
37 Soman, NR, Lanza, GM, Heuser, JM, Schlesinger, PH, Wickline, SA. Synthesis and characterization of stable fluorocarbon nanostructures as drug delivery vehicles for cytolytic peptides. Nano Lett 2008, 8:1131–1136.
38 Pan, H, Soman, NR, Schlesinger, PH, Lanza, GM, Wickline, SA. Cytolytic peptide nanoparticles (‘NanoBees’) for cancer therapy. WIREs Nanomed Nanobiotechnol 2011, 3:318–327.
39 Wang, T, Wang, N, Hao, A, He, X, Li, T, Deng, Y. Lyophilization of water‐in‐oil emulsions to prepare phospholipid‐based anhydrous reverse micelles for oral peptide delivery. Eur J Pharma Sci 2010, 39:373–379.
40 Li, CL, Deng, YJ. Oil‐based formulations for oral delivery of insulin. J Pharm Pharmacol 2004, 56:1101–1107.
41 Walde, P, Giuliani, AM, Boicelli, CA, Luisi, PL. Phospholipid‐based reverse micelles. Chem Phys Lipids 1990, 53:265–288.
42 Melo, EP, Aires‐Barros, MR, Cabral, JM. Reverse micelles and protein biotechnology. Biotechnol Annu Rev 2001, 7:87–129.
43 Vlieghe, P, Lisowski, V, Martinez, J, Khrestchatisky, M. Synthetic therapeutic peptides: science and market. Drug Discov Today 2010, 15:40–56.
44 Ashok, B, Arleth, L, Hjelm, RP, Rubinstein, I, Onyuksel, H. In vitro characterization of PEGylated phospholipid micelles for improved drug solubilization: effects of PEG chain length and PC incorporation. J Pharm Sci 2004, 93:2476–2487.
45 Vukovic, L, Khatib, FA, Drake, SP, Madriaga, A, Brandenburg, KS, Kral, P, Onyuksel, H. Structure and dynamics of highly PEG‐ylated sterically stabilized micelles in aqueous media. J Am Chem Soc 2011, 133:13481–13488.
46 Onyuksel, H, Jeon, E, Rubinstein, I. Nanomicellar paclitaxel increases cytotoxicity of multidrug resistant breast cancer cells. Cancer Lett 2009, 274:327–330.
47 Lim, SB, Rubinstein, I, Sadikot, RT, Artwohl, JE, Onyuksel, H. A novel peptide nanomedicine against acute lung injury: GLP‐1 in phospholipid micelles. Pharm Res 2011, 28:662–672.
48 Onyuksel, H, Banerjee, A. Phospholipid based nanomicelle in cancer nanomedicine. In: Preedy, V, Hunter, R, eds. Nanomedicine in Health and Disease, 1st ed. London: Science Publishers
; 2011, 314–335.
49 Krishnadas, A, Rubinstein, I, Sekosan, M, Onyuksel, H. Targeted delivery of paclitaxel to breast cancer by vasoactive intestinal peptide conjugated sterically stabilized phospholipid mixed micelles. AAPS J 2004, 6:M1191.
50 Cesur, H, Rubinstein, I, Pai, A, Onyuksel, H. Self‐associated indisulam in phospholipid‐based nanomicelles: a potential nanomedicine for cancer. Nanomedicine 2009, 5:178–183.
51 Onyuksel, H, Mohanty, PS, Rubinstein, I. VIP‐grafted sterically stabilized phospholipid nanomicellar 17‐allylamino‐17‐demethoxy geldanamycin: a novel targeted nanomedicine for breast cancer. Int J Pharm 2009, 365:157–161.
52 Koo, OM, Rubinstein, I, Onyuksel, H. Actively targeted low‐dose camptothecin as a safe, long‐acting, disease‐modifying nanomedicine for rheumatoid arthritis. Pharm Res 2011, 28:776–787.
53 Kuzmis, A, Lim, SB, Desai, E, Jeon, E, Lee, B, Rubinstein, I, Onyuksel, H. Micellar nanomedicine of human neuropeptide Y. Nanomed: Nanotechnol Biol Med 2011, 7:464–471.
54 Lim, SB, Rubinstein, I, Onyuksel, H. Freeze drying of peptide drugs self‐associated with long‐circulating, biocompatible and biodegradable sterically stabilized phospholipid nanomicelles. Int J Pharm 2008, 356:345–350.
55 Guo, J, Wu, T, Ping, Q, Chen, Y, Shen, J, Jiang, G. Solubilization and pharmacokinetic behaviors of sodium cholate/lecithin‐mixed micelles containing cyclosporine A. Drug Deliv 2005, 12:35–39.
56 Dagar, S, Onyuksel, H, Akhter, S, Krishnadas, A, Rubinstein, I. Human galanin expresses amphipathic properties that modulate its vasoreactivity in vivo. Peptides 2003, 24:1373–1380.
57 Banerjee, A, Onyuksel, H. Human pancreatic polypeptide in a phospholipid based micellar formulation. Pharma Res 2012, 29:1698–1711.
58 Krishnadas, A, Onyuksel, H, Rubinstein, I. Interactions of VIP, secretin and PACAP(1‐38) with phospholipids: a biological paradox revisited. Curr Pharm Des 2003, 9:1005–1012.
59 Sadikot, RT, Rubinstein, I. Long‐acting, multi‐targeted nanomedicine: addressing unmet medical need in acute lung injury. J Biomed Nanotechnol 2009, 5:614–619.
60 Onyuksel, H, Sejourne, F, Suzuki, H, Rubinstein, I. Human VIP‐α
: a long‐acting, biocompatible and biodegradable peptide nanomedicine for essential hypertension. Peptides 2006, 27:2271–2275.
61 Onyuksel, H, Ikezaki, H, Patel, M, Gao, XP, Rubinstein, I. A novel formulation of VIP in sterically stabilized micelles amplifies vasodilation in vivo. Pharm Res 1999, 16:155–160.
62 Lim, SB, Rubinstein, I, Onyuksel, H. %22Study of Sterically Stabilized Phospholipid Simple and Mixed Micelles as Nanocarriers for Peptide Drugs.%22 Society for Biomaterials Annual Meeting, Chicago, IL; 2007.
63 Brandenburg, KS, Rubinstein, I, Sadikot, RT, Onyuksel, H. Polymyxin B self‐associated with phospholipid nanomicelles. Pharm Dev Technol 2011. In press.
64 Gandhi, S, Rubinstein, I, Tsueshita, T, Onyuksel, H. Secretin self‐assembles and interacts spontaneously with phospholipids in vitro. Peptides 2002, 23:201–204.
65 Koo, OM, Rubinstein, I, Onyuksel, H. Role of nanotechnology in targeted drug delivery and imaging: A concise review. Nanomed: Nanotechnol Biol Med 2005, 1:193–212.
66 Ashok, B, Rubinstein, I, Tsueshita, T, Onyuksel, H. Effects of peptide molecular mass and PEG chain length on the vasoreactivity of VIP and PACAP1–38 in pegylated phospholipid micelles. Peptides 2004, 25:1253–1258.
67 Reubi, JC. Peptide receptors as molecular targets for cancer diagnosis and therapy. Endocr Rev 2003, 24: 389–427.
68 Delgado, M, Abad, C, Martinez, C, Leceta, J, Gomariz, RP. Vasoactive intestinal peptide prevents experimental arthritis by downregulating both autoimmune and inflammatory components of the disease. Nat Med 2001, 7:563–568.