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Boronic Acids as a New Strategy to Boost beta-Lactam Antibiotics for the Treatment of Tubercolosis

Project description

New strategies to combat tuberculosis with antibiotics

Tuberculosis (TB), caused by Mycobacterium tuberculosis (Mtb), remains a significant health threat due to its infectious nature, drug resistance, and the need for prolonged treatments. While beta-lactam antibiotics (BLAs) are commonly used for other bacterial infections, they have not been effective against TB due to Mtb's resistance mechanisms. With the support of the Marie Skłodowska-Curie Actions programme, the BAN-BOOT project aims to inhibit the enzyme beta-lactamase which is present in Mtb and responsible for the ineffectiveness of BLAs. The team will develop and test specific enzyme inhibitors to enhance drug penetration through the bacterium and reduce the Mtb load in patients.

Objective

Tuberculosis (TB) is a highly infectious disease caused by Mycobacterium tuberculosis (Mtb), one of the most dangerous aerobic bacteria. The need for long-term treatments and the increase in drug resistance mechanisms make it necessary to urgently develop new strategies to combat this potentially lethal pathogen.
beta-Lactam Antibiotics (BLA) are the most widely used and safest antibiotics in the clinic and include several classes such as penicillins, cephalosporins and carbapenems. However, historically these agents have not been used to treat TB. There are two mechanisms of resistance to BLA in Mtb: the cell envelope rich in lipoglycans which acts as a barrier for the penetration of many drugs, including BLA, and the expression of BlaC, a specific beta-lactamase enzyme capable of hydrolyze and inactivate the BLA. Recent studies have shown that the combination of meropenem (a beta-lactam carbapenem), amoxicillin (a beta-lactam penicillin) and clavulanate (a beta-Lactamase inhibitor) markedly reduced the Mtb load in the patients sputum after two weeks, therefore giving new hope to the use of BLA to tackle the tuberculosis epidemic.
This proposal aims to develop new compounds that behave as BLA adjuvant for anti-Mtb treatment with a dual mechanism of action. We will design and synthesize novel Boronic Acid Transition State Inhibitors (BATSIs) as inhibitors of BlaC, the beta-lactamase expressed in Mtb, and investigate whether they can be derivatized to become disrupting agents of Mtbs unique outer capsule made of lipoglycans, to promote better penetration of drugs into the cell. This project will also investigate the possibility of improving the penetration of molecules into the necrotic granuloma formed in vivo as part of the disease process, by developing a lipid-based prodrug strategy.
To achieve these specific objectives, the project will be divided into three main work packages, involving a combination of biological, chemical, and analytical expertise.

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HORIZON-TMA-MSCA-PF-EF - HORIZON TMA MSCA Postdoctoral Fellowships - European Fellowships

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Call for proposal

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(opens in new window) HORIZON-MSCA-2023-PF-01

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Coordinator

UNIVERSITA DEGLI STUDI DI MODENA E REGGIO EMILIA
Net EU contribution

Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.

€ 172 750,08
Address
VIA UNIVERSITA 4
41121 Modena
Italy

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Region
Nord-Est Emilia-Romagna Modena
Activity type
Higher or Secondary Education Establishments
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Total cost

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