Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs

2018 ◽  
Vol 26 (14) ◽  
pp. 4310-4319 ◽  
Author(s):  
Zahira Tber ◽  
Mylène Wartenberg ◽  
Jean-Eddy Jacques ◽  
Vincent Roy ◽  
Fabien Lecaille ◽  
...  
Keyword(s):  
Selective Inhibition ◽  
Cathepsin S ◽  
Human Cathepsin

Azepanone-based inhibitors of human cathepsin S: Optimization of selectivity via the P2 substituent

2011 ◽  
Vol 21 (15) ◽  
pp. 4409-4415 ◽  
Author(s):  
Jeffrey K. Kerns ◽  
Hong Nie ◽  
William Bondinell ◽  
Katherine L. Widdowson ◽  
Dennis S. Yamashita ◽  
...  
Keyword(s):  
Cathepsin S ◽  
Human Cathepsin

scholarly journals Novel Opportunities for Cathepsin S Inhibitors in Cancer Immunotherapy by Nanocarrier-Mediated Delivery

Cells ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 2021
Author(s):  
Natalie Fuchs ◽  
Mergim Meta ◽  
Detlef Schuppan ◽  
Lutz Nuhn ◽  
Tanja Schirmeister
Keyword(s):  
Therapeutic Strategy ◽  
Selective Inhibition ◽  
Cell Polarization ◽  
Matrix Proteins ◽  
Cathepsin S ◽  
Cancer Immunity ◽  
Anti Cancer ◽  
Orally Bioavailable ◽  
Antigen Presenting

Cathepsin S (CatS) is a secreted cysteine protease that cleaves certain extracellular matrix proteins, regulates antigen presentation in antigen-presenting cells (APC), and promotes M2-type macrophage and dendritic cell polarization. CatS is overexpressed in many solid cancers, and overall, it appears to promote an immune-suppressive and tumor-promoting microenvironment. While most data suggest that CatS inhibition or knockdown promotes anti-cancer immunity, cell-specific inhibition, especially in myeloid cells, appears to be important for therapeutic efficacy. This makes the design of CatS selective inhibitors and their targeting to tumor-associated M2-type macrophages (TAM) and DC an attractive therapeutic strategy compared to the use of non-selective immunosuppressive compounds or untargeted approaches. The selective inhibition of CatS can be achieved through optimized small molecule inhibitors that show good pharmacokinetic profiles and are orally bioavailable. The targeting of these inhibitors to TAM is now more feasible using nanocarriers that are functionalized for a directed delivery. This review discusses the role of CatS in the immunological tumor microenvironment and upcoming possibilities for a nanocarrier-mediated delivery of potent and selective CatS inhibitors to TAM and related APC to promote anti-tumor immunity.

scholarly journals Crystal structure of human cathepsin S

1998 ◽  
Vol 7 (6) ◽  
pp. 1294-1302 ◽  
Author(s):  
Mary E. Mcgrath ◽  
James T. Palmer ◽  
Ddeter Brömme ◽  
John R. Somoza
Keyword(s):  
Crystal Structure ◽  
Cathepsin S ◽  
Human Cathepsin

scholarly journals High level expression and crystallization of recombinant human cathepsin S

1996 ◽  
Vol 5 (4) ◽  
pp. 789-791 ◽  
Author(s):  
Dieter Brömme ◽  
Mary E. Mcgrath
Keyword(s):  
Cathepsin S ◽  
High Level Expression ◽  
Human Cathepsin ◽  
High Level

Structure of a Cys25→Ser mutant of human cathepsin S

2002 ◽  
Vol 58 (3) ◽  
pp. 451-455 ◽  
Author(s):  
Johan P. Turkenburg ◽  
Marieke B. A. C. Lamers ◽  
A. Marek Brzozowski ◽  
Lisa M. Wright ◽  
Roderick E. Hubbard ◽  
...  
Keyword(s):  
Cathepsin S ◽  
Human Cathepsin

Controlled Peptide Solvation in Portion-Mixing Libraries of FRET Peptides:  Improved Specificity Determination for Dengue 2 Virus NS2B-NS3 Protease and Human Cathepsin S

2007 ◽  
Vol 9 (4) ◽  
pp. 627-634 ◽  
Author(s):  
Fabiana M. Alves ◽  
Izaura Y. Hirata ◽  
Iuri E. Gouvea ◽  
Marcio F. M. Alves ◽  
Morten Meldal ◽  
...  
Keyword(s):  
Cathepsin S ◽  
Human Cathepsin ◽  
Ns3 Protease

scholarly journals Phylogenetic conservation of cysteine proteinases. Cloning and expression of a cDNA coding for human cathepsin S.

1992 ◽  
Vol 267 (19) ◽  
pp. 13708-13713 ◽  
Author(s):  
B Wiederanders ◽  
D Brömme ◽  
H Kirschke ◽  
K von Figura ◽  
B Schmidt ◽  
...  
Keyword(s):  
Cloning And Expression ◽  
Cathepsin S ◽  
Cysteine Proteinases ◽  
Phylogenetic Conservation ◽  
Human Cathepsin

scholarly journals Human cathepsin S gene (CTSS) promoter −25G/A polymorphism

2000 ◽  
Vol 45 (2) ◽  
pp. 94-95 ◽  
Author(s):  
Henian Cao ◽  
Robert A. Hegele
Keyword(s):  
Cathepsin S ◽  
S Gene ◽  
Human Cathepsin
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