Literature DB >> 16480867

Dipeptide nitrile inhibitors of cathepsin K.

Eva Altmann1, Reiner Aichholz, Claudia Betschart, Thomas Buhl, Jonathan Green, René Lattmann, Martin Missbach.   

Abstract

A series of dipeptidyl nitriles as inhibitors of cathepsin K have been explored starting from lead structure 1 (Cbz-Leu-NH-CH2-CN, IC50 = 39 nM). Attachment of non-natural amino acid side chains in P1 and modification of the P3 subunit led to inhibitors with higher potency and improved pharmacokinetic properties.

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Year:  2006        PMID: 16480867     DOI: 10.1016/j.bmcl.2006.01.104

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Photoactivated inhibition of cathepsin K in a 3D tumor model.

Authors:  Mackenzie K Herroon; Rajgopal Sharma; Erandi Rajagurubandara; Claudia Turro; Jeremy J Kodanko; Izabela Podgorski
Journal:  Biol Chem       Date:  2016-06-01       Impact factor: 3.915

2.  Ru(ii) polypyridyl complexes as photocages for bioactive compounds containing nitriles and aromatic heterocycles.

Authors:  Ao Li; Claudia Turro; Jeremy J Kodanko
Journal:  Chem Commun (Camb)       Date:  2018-02-01       Impact factor: 6.222

3.  Light activation of a cysteine protease inhibitor: caging of a peptidomimetic nitrile with Ru(II)(bpy)2.

Authors:  Tomasz Respondek; Robert N Garner; Mackenzie K Herroon; Izabela Podgorski; Claudia Turro; Jeremy J Kodanko
Journal:  J Am Chem Soc       Date:  2011-10-12       Impact factor: 15.419

4.  Inhibition of cathepsin activity in a cell-based assay by a light-activated ruthenium compound.

Authors:  Tomasz Respondek; Rajgopal Sharma; Mackenzie K Herroon; Robert N Garner; Jessica D Knoll; Eric Cueny; Claudia Turro; Izabela Podgorski; Jeremy J Kodanko
Journal:  ChemMedChem       Date:  2014-04-11       Impact factor: 3.466

5.  Ruthenium tris(2-pyridylmethyl)amine as an effective photocaging group for nitriles.

Authors:  Rajgopal Sharma; Jessica D Knoll; Philip D Martin; Izabela Podgorski; Claudia Turro; Jeremy J Kodanko
Journal:  Inorg Chem       Date:  2014-03-24       Impact factor: 5.165

Review 6.  Advances in the discovery of cathepsin K inhibitors on bone resorption.

Authors:  Jun Lu; Maolin Wang; Ziyue Wang; Zhongqi Fu; Aiping Lu; Ge Zhang
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

  6 in total

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