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Synthesis and structure–activity relationships of pyrazole-based inhibitors of meprin α and β

Autor: Kathrin Tan, Christian Jäger, Stefanie Geissler, Dagmar Schlenzig, Mirko Buchholz, Daniel Ramsbeck

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 38, Iss 1 (2023)

Targeting metalloproteinases has been in the focus of drug design for a long time. However, meprin α and β emerged as potential drug targets just recently and are linked to several diseases with different pathological background. Nevertheless, the

Externí odkaz: https://doaj.org/article/6cf1ad89dd504526bad8c27cce359ded

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Heteroaromatic Inhibitors of the Astacin Proteinases Meprin α, Meprin β and Ovastacin Discovered by a Scaffold-Hopping Approach

Autor: Mirko Buchholz, Christian Jäger, Stefanie Geissler, Daniel Ramsbeck, Kathrin Tan, Dagmar Schlenzig, Walter Stöcker, Hagen Körschgen

Publikováno v: Chemmedchem

Astacin metalloproteinases, in particular meprins α and β, as well as ovastacin, are emerging drug targets. Drug‐discovery efforts have led to the development of the first potent and selective inhibitors in the last few years. However, the most r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::06bea260fe451d5839ed36838f04fb7c
https://pubmed.ncbi.nlm.nih.gov/33369214

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Primary Evaluation of Potential Small Molecule Inhibitors of the Astacin Metalloproteinase Ovastacin, A Novel Drug Target in Female Infertility Treatment

Autor: Hagen Körschgen, Christian Jäger, Kathrin Tan, Mirko Buchholz, Walter Stöcker, Daniel Ramsbeck

Despite huge progress in hormonal therapy and improved in vitro fertilization methods, the success rates in infertility treatment are still limited. A recently discovered mechanism revealed the interplay between the plasma protein fetuin-B and the co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b44f6a53d7d8a5134b19574b64aa8f5
https://doi.org/10.26434/chemrxiv.11306867

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Tertiary-Amine-Based Inhibitors of the Astacin Protease Meprin α

Autor: Stephan Schilling, Mirko Buchholz, Dagmar Schlenzig, Christian Jäger, Daniel Ramsbeck, Kathrin Tan

Publikováno v: ChemMedChem. 13(16)

Metalloproteinases of the astacin family are drawing ever increasing attention as potential drug targets. However, knowledge regarding inhibitors thereof is limited in most cases. Crucial for the development of metalloprotease inhibitors is high sele

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9eab5e24640187eefed2cf6d23eb60a5
https://pubmed.ncbi.nlm.nih.gov/29927060

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