LDC and HZI enter partnership for the discovery of new drugs against multi-resistant bacteria

02-Apr-2015 - Germany

The Lead Discovery Center GmbH (LDC) and the Helmholtz Centre for Infection Research (HZI) will be working in close cooperation to identify and optimize new drug candidates against Methicillin-resistant Staphylococcus aureus (MRSA).

©HZI/Rohde

Methicillin-resistant Staphylococcus aureus is one of the most common and most dangerous hospital-acquired infections.

MRSA are resistant to several traditional broad-spectrum antibiotics and therefore constitute a serious threat worldwide, particularly in hospitals and care homes for the elderly. They can cause serious illnesses, especially in patients with weakened immune systems, resulting in long periods of hospitalization, and in some cases, death. Based on data gathered by the German national hospital infection surveillance system (KISS), experts estimate the number of MRSA hospital infections to be approximately 14,000 per annum in Germany alone. Up to 2,000 patients die as a result of these infections each year.

The LDC and the HZI are pooling their expertise to advance a new approach to combating MRSA developed at the HZI.  Their goal is to develop a drug that effectively blocks the establishment of an infection without actually killing the bacteria. ‘This strategy has two important advantages over traditional antibiotics,’ explains Prof. Mark Brönstrup, Head of Chemical Biology at the HZI. ‘First, we avoid further selective pressure that would inevitably lead to the development of new drug resistance.  Secondly, the drug would be better tolerated, as it wouldn’t affect the patient’s normal bacterial flora.’

The addressed therapeutic target has already been validated at the HZI in previous studies.  A drug aimed at this protein has the potential to inhibit a central infection mechanism of S. aureus.  In the first phase of the project, the LDC will screen their own substance library, together with the library supplied by the HZI, for compounds that selectively block the target structure. These hit compounds will be characterized in terms of their potency, selectivity and pharmacological properties, and then further optimized by the LDC in the second stage of the project. In parallel, the HZI will test the efficacy of optimized compounds against MRSA in a battery of biological model systems.

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