Bioaktív okta- és hexadeka-merek szintézise és vizsgálata
Title in English
Synthesis and investigations of bioactive octa- and hexadeca-meric compounds
Panel
Physiology, Pathophysiology, Pharmacology and Endocrinology
Department or equivalent
Pathobiochemistry Research Group of Hungarian Academy of Scienses in Semmelweis (Office for Research Groups Attached to Universities and Other Institutions)
Participants
Kéri, György
Starting date
2003-01-01
Closing date
2006-12-31
Funding (in million HUF)
4.076
FTE (full time equivalent)
0.00
state
closed project
Final report
Results in Hungarian
Új, biológiailag aktív oligomer hordozó molekulákat terveztünk, szintetizáltunk és teszteltünk. A kismolekulasúlyú oligomer molekulák alkalmasaknak bizonyultak arra, hogy hozzájuk 3-8 darab egy szabad karbonsavval rendelkező aminosav-, peptid- vagy peptidmimetikus származékot lehessen kapcsolni. Az oligofunkciós hordozó molekula 1-4 tercier amino csoportja elősegíti poláros oldószerekben való oldékonyságot. A gonadotrop hormon releasing hormon, a szomatosztatin és a multi drog rezisztenciát gátló peptideket illetve származékaikat szintetizáltuk és in vitro sejkultúrákon teszteltük. Különösen aktívak voltak anyagaink az angiogenezis stimulálásában valamint a neurogén-gyulladás gátlásában. Egy szabadalmi bejelentést tettünk, egy pedig készülőben van.
Results in English
New biologically active oligomeric carrier molecules having exact chemical structures and homogen molecular weight were designed, synthesized, tested and patented. The compounds are suitable to conjugate 3-8 biologically active peptide derivatives or peptidmimetics having a free carboxyl group. The carrier molecules are more soluble in polar solvents because of the 1-4 tertier nitrogen groups. The gonadotrop hormone releasing hormone agonists and inhibitors, somatostatin inhibitors and multi drug resistance inhibitors were especially active on stimulation of angiogenesis and against neurogenic inflammation. The new compounds were tested on cell cultures in vitro. It has been shown that the oligomeric conjugates i.e. the biologically active analogs coupled to the oligo-cation carrier resulted in non-toxic conjugates. We have prepared two patent applications.
Horváth Aniko et al: A synthetic group A streptococcal vaccine of high purity and broad protective range,-3rd International and 28th European Peptide symposium, in the proceeding of the 28th Eeuropean Peptide Symposium, 2005
Klebl Bert (De); Baumann Matthias (De); Hoppe Edmund (De); Brehmer Dirk (De); Daub Henrik (De); Kéri György (Hu); Varga Zoltán (Hu); Marosfalvi Jenő (Hu); Őrfi László: Pyrimidine Derivatives, WO2006021458, 2006, 2006
Kéri Gy, Őrfi L, Erős D, Hegymegi-Barakonyi B, Szántai-Kis Cs, Horváth Z, Wáczek F, Marosfalvy J, Szabadkai I, Pató J, Greff Z, Hafenbradl D, Daub H, Müller G, Klebl B, Ullrich A.: Signal Transduction Therapy with Rationally Designed Kinase Inhibitors., Current Signal Transduction Therapy 1 : 67-95, 2006, 2006
Keri Gyorgy Dr (Hu); Szolcsanyi Janos Dr (Hu); Pinter Erika Dr (Hu); Helyes Zsuzsanna Dr (Hu); Ercheg: Signal Transduction Therapy with Rationally Designed Kinase Inhibitors., Use Of Phenylhydrazone Derivatives As Antiinflammatory Or Analgetic Agents, 2006
Magdolna Kovács, Borbála Vincze, Judit E. Horváth, János Seprődi.: Structure-activity study on the LH- and FSH-releasing and anticancer effects of gonadotropin-releasing hormone-III analogs., Peptides (accepted for publication) 2006, 2007
Tejeda M, Gaál D, Hullán L, Hegymegi-Barakonyi B and Kéri Gy.: Evaluation of the Antitumor Efficacy of the Somatostatin Structural Derivative TT-232 on Different Tumor Models., Anticancer Research 26 : 3477-3484 2006., 2006
Anikó Horváth, János Seprődi, Tibor Vántus, Miklós Idei, Gyöngyi Bökönyi, József Tóvári, György Kéri: Effect of new synthetic peptides and peptidomimetics on angiogenesis., International Conference of the 43rd Japanase Peptide Symposium and 4th Peptide Engineering Meeting. 43JPS/PEM4, Yokohama, November 5-8, 2006. P124 . (abstract), 2006
Anikó Horváth, János Seprődi, Tibor Vántus, Miklós Idei, Gyöngyi Bökönyi, József Tóvári, István Kenessey, György Kéri: Effect of new synthetic peptides and peptidomimetics on angiogenesis., Peptide Science 2006. Eds. Hitoshi Isida and Hisakazu Mihara, JaSymposium and 4th Peptide Engineering Meeting. 43JPS/PEM4, Yokohama, 249-250, 2006
Anikó Horváth, György Kéri, József Tóvári, János Seprődi, Tibor Vántus, István Kenessey, Miklós Idei, Tanai Henrietta.: Peptides for activation of angiogenesis, pharmaceutical compounds containing same and use of these compounds, Magyar szabadalmi bejelentés, 2006.10. 27. (aktaszám:102369-9535 PT/TM), 2006
