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posted 09-03-2009 11:45 AM     Click Here to See the Profile for grischenko   Click Here to Email grischenko     Edit/Delete Message Reply w/Quote
OTAVA has revealed that it has designed selective CK2 inhibitors.
Design of specific small molecules that are able to block (inhibit) function of macromolecular targets responsible for the development of certain disorder is the classic and most widely used approach in modern drug therapeutics, for example, in cancer treatment To what criteria the cancer drug target must correspond before it could be accepted as a promising object for searching of an appropriate anti-cancer drug? Ideally it must be:

• disfunctioned in cancer cells;
• essential for cell surviving (target 'switching-off' must lead to cell death);
• the target's activity must not be compensated by other macromolecules; and
• the target must be presented only in tumour cells

Surprisingly, protein kinase CK2 corresponds to three out of four criteria indicated above.

Since 2005 this kinase was generally accepted as pharmacological tool of proven high therapeutic value.

The oncogenic potential of protein kinase CK2 and its involvement in virally mediated pathologies and inflammatory disorders has led to an increasing number of studies aimed at the discovery of selective CK2 inhibitors.

Efficient at low micromolar concentrations and selective CK2 inhibitors have been designed by OTAVA.

To discover new inhibitors, the company's researchers spanned computer-based molecular modelling with chemical synthesis of compounds, which were further tested in vitro to investigate their ability to bind to and affect the activity of CK2.

The binding modes of inhibitors that target the ATP-binding site of CK2 were also studied.

Some recently discovered novel patent-free inhibitors were organised in clusters of similar compounds: ProHit compound sets.

OTAVA offers ProHit Sets of CK2 inhibitors to academic and commercial laboratories worldwide to use in drug discovery programmes targeting protein kinases.

The company also plans to extend ProHit sets to other protein kinase targets.

List of selected publications by OTAVA’s scientists:

[1] Evaluation of 4,5,6,7-tetrahalogeno-1H-isoindole-1,3(2H)-diones as inhibitors of human protein kinase CK2. Golub AG, Yakovenko OY, Prykhod'ko AO, Lukashov SS, Bdzhola VG, Yarmoluk SM. Biochim. Biophys. Acta. 2008, 1784, 143.
[2] Kirchhoff atomic charges fitted to multipole moments: implementation for a virtual screening system O.Ya. Yakovenko, A.A. Oliferenko, V.G. Bdzhola, V.A. Palyulin, N.S. Zefirov. J. Comput. Chem. 2008, 29, 1332.
[3] Evaluation of 3-Carboxy-4(1H)-quinolones as Inhibitors of Human Protein Kinase CK2. Golub AG, Yakovenko OY, Bdzhola VG, Sapelkin VM, Zien P, Yarmoluk SM. J. Med. Chem. 2006, 49, 6443.
[4] Evaluation of 4H-4-chromenone derivatives as inhibitors of protein kinase CK2. A.O. Prykhod’ko, O.Ya. Yakovenko, A.G. Golub, A.G. Bdzhola, S.M. Yarmoluk, Biopolymers and cell 2005, 21, 287.
[5] Search for protein kinase CK2 inhibitors among 3-carboxy-4-aminoquinoline derivatives. V.M. Sapelkin, A.G. Golub, O.Ya. Yakovenko, V.G. Bdzhola, S.M. Yarmoluk, Ukrainica Bioorganica Acta 2005, 2, 28.
[6] Search for kasein kinase 2 inhibitors among 4 aminoquinazoline derivatives. V.M. Sapelkin, A.G. Golub, O.Ya. Yakovenko, V.G. Bdzhola, S.M. Yarmoluk, Ukrainica Bioorganica Acta 2004, 1, 74.
[7] Inhibitors of protein kinase CK2. A.O. Prykhod'ko, G.G. Dubinina, S.M. Golovach, S.M. Yarmoluk, Ukrainica Bioorganica Acta 2004, 1, 39.

Contact details:

150 Zabolotnogo St.
Kyiv 143, 03143
Tel./Fax: +380 44 5222458

OTAVA – North American Division
55 Ellerslie Ave., Suite 524
Toronto, Ontario, M2N 1X9
Tel.: 1-416-305-9979
Fax: 1-866-881-9921 (Toll-free in US & Canada)
Web-site: http://www.otavachemicals.com


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