Advanced Materials

The Advanced Materials Division (AMD) is a dynamic and multi-disciplinary division that addresses the need for specific research into the end-use of metals in the manufacturing, fabrication and mining industries.

Biomed

The Biomed group at Mintek undertakes early stage drug discovery with the primary objective of identifying novel inhibitors of HIV-1 replication. The group comprises both chemists and biochemists and utilizes a structure-based approach to design and discover useful, small-molecule, inhibitors.

 

 

HIV-1 integrase inhibitors

The HIV-1 integrase enzyme is the third virally-encoded enzyme and catalyses the insertion of viral DNA into the human genome. Fundamental to the life-cycle of the virus, the enzyme has been validated as a target for drug intervention. In particular, inhibitors of the strand transfer process of HIV -1 integrase have shown clinical relevance and led to the discovery and FDA-approval of Raltegravir (Merck and Co).  The Biomed group undertakes the rational design and synthesis of small molecules targeting the strand-transfer complex. Compounds are investigated for biological activity in direct integrase-inhibition assays and evaluated for drug-like characteristics.

 

 

Integrase-LEDGF inhibitors

The host protein lens epithelium-derived growth factor (LEDGF) directly interacts with HIV-1 integrase in the pre-integration complex (PIC) and has been shown to enhance integrase activity in vitro.  Targeting the LEDGF-IN interaction, the recently discovered LEDGINS (KULeuven, Belgium) represent a novel class of anti-HIV inhibitors with clinical potential. The Biomed group seeks novel modulators of this host protein- viral protein interaction through both a rational drug design approach and a library screening approach.

 

 

Recent publications

1.  Mphahlele M, Papathanasopoulos M, Cinellu MA, Coyanis M, Mosebi S, Traut T, Coates J, Hewer R. Bioorg Med Chem. 2012, 20(1), 401-407.
2.  Hewer R, Kriel FH, Coates J. Random and Rational approaches to HIV-1 drug discovery in Africa. In Drug Discovery in Africa. Eds Chibale, Davies-Coleman. Springer. In Press
3. Peacock AFA, Bullen GA, Gethings L, Williams JP, Kriel FH, Coates J. Journal of Inorganic Biochemistry. In Press.

 

 

For more information on the Biomed group please contact:

Raymond Hewer, PhD
Head: Biomed
Tel: +27 11 709 4478
Fax: +27 11 709 4480
raymondh@mintek.co.za