The designer leptin antagonist peptide Allo-aca compensates for short serum half-life with very tight binding to the receptor

Amino Acids

Volumn 46, Issue 4, 2014, Pages 873-882

  Otvos, Laszlo ^a   Vetter, Stefan W ^b   Koladia, Mohit ^b   Knappe, Daniel ^c   Schmidt, Rico ^c   Ostorhazi, Eszter ^d   Kovalszky, Ilona ^d   Bionda, Nina ^e   Cudic, Predrag ^e   Surmacz, Eva ^f   Wade, John D ^g   Hoffmann, Ralf ^c  

^a Temple University   (United States)

^b NORTH DAKOTA STATE UNIVERSITY   (United States)

^c UNIVERSITY OF LEIPZIG   (Germany)

^d SEMMELWEIS UNIVERSITY OF MEDICINE   (Hungary)

^e TORREY PINES INSTITUTE FOR MOLECULAR STUDIES   (United States)

^f TEMPLE UNIVERSITY   (United States)

^g FLOREY INSTITUTE OF NEUROSCIENCE AND MENTAL HEALTH   (Australia)

Author keywords

Anti proliferation; Dissociation constant; Metabolic stability; Peptide therapeutics; Receptor activation

Indexed keywords

ALLO ACA; LEPTIN RECEPTOR; PEPTIDE HORMONE RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; LEPTIN; PEPTIDE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTIPROLIFERATIVE ACTIVITY; ARTICLE; BINDING AFFINITY; BREAST CANCER; CELL GROWTH; CELL STRAIN K 562; CELL STRAIN MCF 7; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG DEGRADATION; DRUG HALF LIFE; DRUG RECEPTOR BINDING; FEMALE; GROWTH INHIBITION; IC 50; MAXIMUM PLASMA CONCENTRATION; MOUSE; MYELOID LEUKEMIA; NONHUMAN; PRIORITY JOURNAL; RAT; SURFACE PLASMON RESONANCE; ANIMAL; ANTAGONISTS AND INHIBITORS; BLOOD; BOVINE; CHEMISTRY; DRUG DESIGN; HALF LIFE TIME; HUMAN; KINETICS; METABOLISM; TUMOR CELL LINE;

ANIMALIA; BOVINAE;

ANIMALS; CATTLE; CELL LINE, TUMOR; DRUG DESIGN; FEMALE; HALF-LIFE; HUMANS; KINETICS; LEPTIN; MICE; PEPTIDES; RECEPTORS, LEPTIN;

EID: 84898927167     PISSN: 09394451     EISSN: 14382199     Source Type: Journal    
DOI: 10.1007/s00726-013-1650-6     Document Type: Article

References (43)

1. Albericio F, Kruger HG (2012) Therapeutic peptides. Future Med Chem 4:1527-1531
2. Beccari S, Kovalszky I, Wade JD, Otvos L Jr, Surmacz E (2013) Designer peptide antagonist of the leptin receptor with peripheral antineoplastic activity. Peptides 44:127-134
3. Carpenter B, Hemsworth GR, Wu Z, Maamra M, Strasburger CJ, Ross RJ, Artymiuk PJ (2012) Structure of the human obesity receptor leptin-binding domain reveals the mechanism of leptin antagonism by a monoclonal antibody. Structure 20:487-497
4. Fields GB, Noble RL (1990) Solid-phase peptide synthesis using 9-fluorenylmethoxycarbonyl amino acids. Int J Pept Protein Res 35:161-214
5. Frey WH 2nd, DeSota Johnson D, Hoffmann C, McCall JT (1981) Effect of stimulus on the chemical composition of human tears. Am J Ophthalmol 92:559-567
6. Gonzalez RR, Cherfils S, Escobar M, Yoo JH, Carino C, Styer AK, Sullivan BT, Sakamoto H, Olawaiye A, Serikawa T, Lynch MP, Rueda RR (2006) Leptin signaling promotes the growth of mammary tumors and increases the expression of vascular endothelial growth factor (VEGF) and its receptor type two (VEGF-R2). J Biol Chem 281:26320-26328
7. Gonzalez RR, Watters A, Xu Y, Singh UP, Mann DR, Rueda BR, Penichet ML (2009) Leptin-signaling inhibition results in efficient anti-tumor activity in estrogen receptor positive or negative breast cancer. Breast Cancer Res 11:R36
8. Han KY, Azar DT, Sabri A, Lee H, Jain J, Lee BS, Chang JH (2010) Characterization of the interaction between endostatin short peptide and VEGF receptor 3. Protein Pept Lett 19:969-974
9. Hoffmann R, Bulet P, Urge L, Otvos L Jr (1999) Range of activity and metabolic stability of synthetic antibacterial glycopeptides from insects. Biochim Biophys Acta 1426:459-467
10. Inui A, Meguid MM (2003) Cachexia and obesity: two sides of one coin? Curr Opin Clin Nutr Metab Care 6:395-399
11. Janssen S, Rosen DM, Ricklis RM, Dionne CA, Lilja H, Christensen SB, Isaacs JT, Denmeade SR (2006) Pharmacokinetics, biodistribution, and antitumor efficacy of a human glandural kallikrenin 2 (hK2)-activated thapsigargin prodrug. Prostate 66:358-368
12. Joslin JO (2009) Blood collection techniques in exotic small mammals. J Exotic Pet Med 18:117-139
13. Kalra SP (2008) Central leptin insufficiency syndrome: an interactive etiology for obesity, metabolic and neural diseases and for designing new therapeutic interventions. Peptides 29:127-138
14. Kilko SN, Corr M, Boyd LF, Lees A, Inman JK, Margulies DH (1993) Direct detection of major histocompatibility complex class I binding to antigenic peptides using surface plasmon resonance. Peptide immobilization and characterization of binding specificity. J Biol Chem 268:15425-15434
15. Knappe D, Henklein P, Hoffmann R, Hilpert K (2010) Easy strategy to protect antimicrobial peptides from fast degradation in serum. Antimicrob Agents Chemother 54:4003-4005
16. Kovalszky I, Surmacz E, Scolaro L, Cassone M, Sztodola A, Olah J, Hatfield MP, Lovas S, Otvos L Jr (2010) Leptin-based glycopeptide induces weight loss and simultaneously restores fertility in animal models. Diabetes Obes Metab 12:393-402
17. Landt M (2000) Leptin binding and binding capacity in serum. Clin Chem 46:379-384
18. Liao S, Qie JK, Xue M, Zhang ZQ, Liu KL, Ruan JX (2010) Metabolic stability of human parathyroid hormone peptide hPTH (1-34) in rat tissue homogenates: kinetics and products of proteolytic degradation. Amino Acids 38:1595-1605
19. Lister-James J, Moyer BR, Dean T (1996) Small peptides radiolabeled with 99mTc. Q J Nucl Med 40:221-233
20. Martins I, Gomez S, Costa RO, Otvos L, Oliveira CR, Resende R, Pereira CMF (2013) Leptin and ghrelin prevent hippocampal dysfunction induced by Aβ oligomers. Neurosci 241:41-51
21. McDermott JR, Smith AI, Biggins JA, Hardy JA, Dodd PR, Edwardson JA (1981) Degradation of luteinizing hormone-releasing hormone by serum and plasma in vitro. Regul Pept 2:69-79
22. Mistrik P, Moreau F, Allen JM (2004) BiaCore analysis of leptin-leptin receptor interaction: evidence for 1:1 stoichiometry. Anal Biochem 327:271-277
23. Miyake T, Sawada O, Kakinoki M, Sawada T, Kawamura H, Ogasawara K, Ohji M (2010) Pharmacokinetics of bevacizumab and its effect on vascular endothelial growth factor after intravitreal injection ofbevacizumab in macaque eyes. Invest Ophthalmol Vis Sci 51:1606-1608
24. Moulin A, Brunel L, Boeglin D, Demange L, Ryan J, M'Kadmi C, Denoyelle S, Martinez J, Fehrentz JA (2013) The 1,2,4-triazole as a scaffold for the design of ghrelin receptor ligands: development of JMV 2959, a potent antagonist. Amino Acids 44:301-314
25. Ottiger M, Thiel MA, Feige U, Lichtlen P, Urech DM (2009) Efficient intraocular penetration of topical anti-TNF-alpha single-chain antibody (ESBA105) to anterior and posterior segment without penetration enhancer. Invest Ophthalmol Vis Sci 50:586-779
26. Otvos L Jr, Surmacz E (2011) Targeting the leptin receptor: a potential new mode of treatment for breast cancer. Expert Rev Anticancer Ther 11:1147-1150
27. Otvos L Jr, Terrasi M, Cascio S, Cassone M, Abbadessa G, di Pascali F, Scolaro L, Knappe D, Stawikowski M, Cudic P, Wade JD, Hoffmann R, Surmacz E (2008) Development of a pharmacologically improved peptide agonist of the leptin receptor. Biochim Biophys Acta 1783:1745-1754
28. Otvos L Jr, Kovalszky I, Scolaro L, Sztodola A, Olah J, Cassone M, Knappe D, Hoffmann R, Lovas S, Hatfield MP, Beko G, Zhang S, Wade JD, Surmacz E (2011a) Peptide-based receptor antagonists for cancer treatment and appetite regulation. Biopolymers 96:117-125
29. Otvos L Jr, Kovalszky I, Riolfi M, Ferla R, Olah J, Sztodola A, Nama K, Molino A, Piubello Q, Wade JD, Surmacz E (2011b) Efficacy of a leptin receptor antagonist peptide in a mouse model of triple-negative breast cancer. Eur J Cancer 47:1578-1584
30. Otvos L Jr, Shao W-H, Vanniasinghe A, Amon MA, Holub MC, Kovalszky I, Wade JD, Doll M, Cohen PL, Manolios N, Surmacz E (2011c) Toward understanding the role of leptin and leptin receptor antagonism in preclinical models of rheumatoid arthritis. Peptides 32:1567
31. Ozturk K, Avcu F, Ural AU (2012) Aberrant expressions of leptin and adiponectin receptor isoforms in chronic myeloid leukemia patients. Cytokine 57:61-67
32. Peelman F, Van Beneden L, Zabeau H, Iserentant H, Ulrichts P, Defeau D, Verhee A, Catteeuw D, Elewaut D, Tavernier JF (2004) Mapping of the leptin binding sites and design of a leptin antagonist. J Biol Chem 279:41038-41046
33. Powell MF, Grey H, Gaeta F, Sette A, Colon SM (1992) Peptide stability in drug development: a comparison of peptide reactivity in different biological media. J Pharm Sci 81:731-735
34. Powell MF, Stewart T, Otvos L Jr, Urge L, Gaeta F, Sette A, Arrhenius T, Thomson D, Soda K, Colon SM (1993) Peptide stability in drug development. II. Effect of single amino acid substitution and glycosylation peptide reactivity in human serum. Pharmacol Res 10:1268-1273
35. Reagan-Shaw S, Nihal M, Ahmad N (2008) Dose translation from animal to human studies revisited. FASEB J 22:569-661
36. Romero E, Velez de Mendizabal N, Cendros JM, Peraire C, Bascompta E, Obach R, Troconiz IF (2012) Pharmacokinetic/pharmacodynamic model of the testosterone effects of triptorelin administered in sustained release formulations in patients with prostate cancer. J Pharmacol Exp Ther 342:788-798
37. Sandowski Y, Raver N, Gussakovski EE, Shochat S, Dym O, Livnah O, Rubinstein M, Krishna R, Gertler A (2002) Subcloning, expression, purification, and characterization of recombinant human leptin-binding domain. J Biol Chem 277:46304-46309
38. Scolaro L, Parrino C, Coroniti R, Otvos L Jr, Surmacz E (2013) Exproling leptin antagonism in ophthalmic cell models. PLoS One 8:e76437
39. Shpilman M, Niv-Spector L, Katz M, Varol C, Solomon G, Ayalon-Soffer M, Boder E, Halpern Z, Elinav E, Gertler AM (2011) Development and characterization of high affinity leptins and leptin antagonists. J Biol Chem 286:4429-4442
40. Sorbara L, Simpson T, Vaccari S, Jones L, Fonn D (2004) Tear turnover rate is reduced in patients with symptomatic dry eye. Cont Lens Anterior Eye 27:15-20
41. Wauters M, Considine RV, Van Gaal LF (2000) Human leptin: from an adipocyte hormone to an endocrine mediator. Eur J Endocrinol 143:293-311
42. Werle M, Bernkop-Schnurch A (2006) Strategies to improve plasma half life time of peptide and protein drugs. Amino Acids 30:351-367
43. Zannikos PN, Rohatagi S, Jensen BK, DePhillips SL, Rhodes GR (2000) Pharmacokinetics and concentration-effect analysis of intravenous RGD891, a platelet GPIIb/IIIa antagonist, using mixed-effects modeling (NONMEM). J Clin Pharmacol 40:1129-1140