Review
Version 2
Preserved in Portico This version is not peer-reviewed
The Pharmacological Tails of Matrix Metalloproteinases and Their Inhibitors
Version 1
: Received: 5 December 2020 / Approved: 7 December 2020 / Online: 7 December 2020 (15:07:30 CET)
Version 2 : Received: 23 March 2021 / Approved: 24 March 2021 / Online: 24 March 2021 (16:23:28 CET)
Version 2 : Received: 23 March 2021 / Approved: 24 March 2021 / Online: 24 March 2021 (16:23:28 CET)
A peer-reviewed article of this Preprint also exists.
Das, N.; Benko, C.; Gill, S.E.; Dufour, A. The Pharmacological TAILS of Matrix Metalloproteinases and Their Inhibitors. Pharmaceuticals 2021, 14, 31. Das, N.; Benko, C.; Gill, S.E.; Dufour, A. The Pharmacological TAILS of Matrix Metalloproteinases and Their Inhibitors. Pharmaceuticals 2021, 14, 31.
Abstract
Matrix metalloproteinases (MMPs) have been demonstrated to have both detrimental and protective functions in inflammatory diseases. Several MMP inhibitors, with the exception of Periostat®, have failed in Phase III clinical trials. As an alternative strategy, recent efforts have been focussed on the development of more selective inhibitors or targeting other domains than their active sites (e.g., exosites, ectosites) through specific small molecule inhibitors or monoclonal antibodies. Here, we present some examples that aim to better understand the mechanisms of conformational changes/allosteric control of MMPs functions. In addition to MMP inhibitors, we discuss unbiased global approaches such as proteomics and N-terminomics to identify new MMP substrates and achieve a better understanding of the roles of these proteases in diseases.
Keywords
Matrix metalloproteinase; MMPs; protease; TIMPs; exosite; small molecule inhibitors; monoclonal antibodies; proteomics; N-terminomics; TAILS
Subject
Medicine and Pharmacology, Immunology and Allergy
Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Comments (1)
We encourage comments and feedback from a broad range of readers. See criteria for comments and our Diversity statement.
Leave a public commentSend a private comment to the author(s)
* All users must log in before leaving a comment
Commenter: Antoine Dufour
Commenter's Conflict of Interests: Author