Watch the recording now: Assessing MMP-13 functions in osteoarthritis and aortic aneurysm through targeted protein inhibition with BI-4394
02 April, 2024
Watch the recording of our opnMe online seminar from March 21, 2024, and follow the journey of our selective MMP-13 inhibitor from our bench to scientific research labs around the world. Learn how BI-4394 helped to shed light on the role of MMP-13 in cartilage degeneration in osteoarthritis and to uncover new insights into the enzyme’s role in aortic aneurysm formation1,2.
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About MMP-13 antagonist BI-4394:
BI-4394 is the result of an elegant structure-based drug design, leading to a highly potent inhibitor of MMP-13 for research purposes with excellent selectivity against several other MMPs 3,4. MMP-13, also known as collagenase-3 (CLG3) is a key enzyme in the matrix metalloproteinase (MMP) family, involved in the breakdown of extracellular matrix in normal physiological processes and disease progression such as arthritis and metastasis. MMP-13 is the most efficient enzyme of this class at degrading collagen II, a crucial step in articular cartilage degradation. Broad-spectrum MMP-13 inhibitors have failed in clinical trials at least in part due to inhibition of MMPs other than MMP-13. Therefore, high selectivity of the antagonist for MMP-13 over other MMPs is favorable.
About opnMe:
opnMe.com, the open science portal of Boehringer Ingelheim, aims to accelerate research initiatives to enable new insights of disease biology in areas of high unmet medical need by sharing well-characterized molecules and offer collaborations for science. In the spirit of collaboration, our molecules are provided to the scientific community to help unlock and fulfill their full potential. These molecules are either freely available as “Molecules to Order” or applied via scientific research submissions as “Molecules for Collaboration”. As part of our third pillar, our “opn2EXPERTS” program, we also enlist scientific advice on key biologic issues to fuel further drug discovery and deliver novel solutions that benefit unmet patient needs.
About opnMe online seminars:
We invite you to watch recordings of our previous online seminars on opnMe. Follow the journey of the PROTAC ACBI1, a cooperative degrader of BAF subunits SMARCA2 and 4, which are essential parts of the chromatin remodeler BAF (SWI/SNF) complex.
1Zimmermann L.M.A. et al. Targeting MMP-13 prevents aortic aneurysm formation in Marfan mice. bioRxiv. 2022. DOI: 10.1101/2022.11.30.518511
2Zimmermann L.M.A. et al. Controlling BMP growth factor bioavailability: The extracellular matrix as multiskilled platform. Cell Signal. 2021, 85:110071. DOI: 10.1016/j.cellsig.2021.110071
3Heim-Riether A. et al. Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors. Bioorg Med Chem Lett. 2009, 19(18):5321-4. DOI: 10.1016/j.bmcl.2009.07.151
4Gao D. et al. SAR studies of non-zinc-chelating MMP-13 inhibitors: Improving selectivity and metabolic stability. Bioorg Med Chem Lett. 2010, 20(17):5039-43. DOI: 10.1016/j.bmcl.2010.07.036