Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides

SF Chowdhury, J Sivaraman, J Wang… - Journal of medicinal …, 2002 - ACS Publications
… series of noncovalent inhibitors of cathepsin L have been designed to mimic the mode of
autoinhibition of procathepsin L. Just like the propeptide, these peptide-based inhibitors have a …

Non-covalent cathepsin K inhibitors for the treatment of osteoporosis

TS Kim, AS Tasker - Current topics in medicinal chemistry, 2006 - ingentaconnect.com
… amides based on dipeptidyl anilines for cathepsin K inhibition. These new non-covalent
inhibitors exhibit single digit nM inhibition of the cathepsin family. Molecular modeling studies on …

Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors

E Altmann, J Renaud, J Green, D Farley… - Journal of medicinal …, 2002 - ACS Publications
… against rabbit and human cysteine proteases cathepsins K, L… non-covalent inhibitors of
cathepsin K. Compounds 4b, 4e, and 4g exhibit high potency toward rabbit and human cathepsin

Identification of a potent and selective noncovalent cathepsin S inhibitor

RL Thurmond, S Sun, CA Sehon, SM Baker… - … of Pharmacology and …, 2004 - ASPET
… Here, we describe the first nonpeptidic and noncovalent inhibitor of cathepsin S that has high
… other cathepsins makes it an excellent tool for exploring the role of cathepsin S in humans. …

Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors

DJ Gustin, CA Sehon, J Wei, H Cai, SP Meduna… - Bioorganic & medicinal …, 2005 - Elsevier
… = 20 nM) and selective noncovalent cathepsin S inhibitor 2 have recently … inhibitors with a
ketobenzimidazole piperidine resulted in a new series of potent, noncovalent CatS inhibitors. …

Structural basis for development of cathepsin B-specific noncovalent-type inhibitor: crystal structure of cathepsin B–E64c complex

A Yamamoto, K Tomoo, K Matsugi, T Hara, Y In… - … et Biophysica Acta (BBA …, 2002 - Elsevier
… —information that will be useful in the design of the noncovalent-type inhibitor. … spleen
cathepsin B–E64c complex. We would also like to propose a noncovalent-type inhibitor that can …

Discovery and In Vivo Anti-inflammatory Activity Evaluation of a Novel Non-peptidyl Non-covalent Cathepsin C Inhibitor

X Chen, Y Yan, Z Zhang, F Zhang, M Liu… - Journal of Medicinal …, 2021 - ACS Publications
… derivative could be used as an effective cathepsin C inhibitor and encouraged us to …
To verify the cysteine cathepsin selectivity for our “non-peptidyl non-covalent Cat C inhibitors”, …

MD-Based Assessment of Covalent Inhibitors in Noncovalent Association Complexes: Learning from Cathepsin K as a Test Case

E Endres, N Yuan Chen, C Sotriffer - Journal of Chemical …, 2023 - ACS Publications
… Thus, the aim of this study was to investigate the noncovalent interactions of covalent
inhibitors. Using MD simulations, common structural features between different warhead types …

Recent advances in the design of cathepsin S inhibitors

J JM Wiener, S Sun… - Current topics in medicinal …, 2010 - ingentaconnect.com
… , of late, noncovalent inhibitors. This review details advances in cathepsin S inhibitor design
as … on structure-activity relationships of the various covalent and noncovalent inhibitor series. …

Toward very potent, non-covalent organophosphonate inhibitors of cathepsin C and related enzymes by 2-amino-1-hydroxy-alkanephosphonates dipeptides

M Drąg, E Wieczerzak, M Pawełczak, Ł Berlicki… - Biochimie, 2013 - Elsevier
… , most strategies to date have yielded covalent inhibitors. Here we present a series of non-covalent
β-amino-α-hydroxyalkanephosphonate dipeptidic inhibitors of cathepsin C, ranking …