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Updated: Sep 23, 2026

A Mass Spectrometry-Based Approach to Identify Phosphoprotein Phosphatases and their Interactors
Published on: April 29, 2022
Phosphinic acid-based MMP-13 inhibitors that spare MMP-1 and MMP-3
Lawrence A Reiter1, Peter G Mitchell, Gary J Martinelli
1Pfizer Inc, Global Reseach & Development, Groton Laboratories, Eastern Point Rd., 06340, Groton, CT, USA. lawrence_a_reiter@groton.pfizer.com
Abstract:
Phosphinic acid-based inhibitors of MMP-13 have been investigated with the aim of identifying potent inhibitors with high selectivity versus MMP-1. Independent variation of the substituents on a P(1)' phenethyl group and a P(2) benzyl group improved potencies in both cases around 3-fold over the unsubstituted parent. Combining improved P(1)' and P(2) groups into a single molecule gave an inhibitor with a 4.5 nM IC(50) against MMP-13 and which is 270-fold selective over MMP-1.
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