... ( [email protected] ) 3 3 2020 11 4 2020 14 4 2020 15 4 2020 © 2020 The Author(s). Published by Portland Press Limited on behalf of the Biochemical Society 2020 metalloproteases next-generation sequencing protease inhibitor protein engineering protein–protein...

... © 2019 The Author(s). Published by Portland Press Limited on behalf of the Biochemical Society 2019 cathepsin K collagen exosite inhibitor high-throughput screening osteoporosis protease inhibitor Since its first crystal structure reported in 1997 [ 9 ], major interest has been...

... that contains insertions of leucine and asparagine (L38↑N↑L) in the hinge region of protease at position 38. This was isolated from a protease inhibitor naïve infant. Isothermal titration calorimetry showed that 10% less of L38↑N↑L protease was in the active conformation as compared with a reference strain. L38...

... Kunitz protease inhibitor domain (APPI) for inhibition of the oncogenic protease mesotrypsin, in the presence of three competing serine proteases, anionic trypsin, cationic trypsin and kallikrein-6. We generated a variant, designated APPI P13W/M17G/I18F/F34V , with up to 30-fold greater specificity...

... Plasmodium falciparum protease inhibitor substrate specificity In October 2015, the Nobel Prize for medicine was awarded to Youyou Tu for the development of the antimalarial drug, artemisinin. Artemisinin and its derivatives (collectively referred to as the ARTs) are currently the leading...

... of proteinaceous inhibitors, mesotrypsin presents a formidable challenge to the development of biological inhibitors. We used a powerful yeast display platform for directed evolution, employing a novel multi-modal library screening strategy, to engineer the human amyloid precursor protein Kunitz protease inhibitor...

... of TMPRSS2 by the non-specific serine protease inhibitor camostat caused a 10-fold reduction in infection of Calu-3 cells by SARS-CoV [ 19 ]. On the basis of this information, TMPRSS2 could be a potential target for drug design. However, in contrast with many other well-characterized trypsin-like serine...

... potential can be realized, the results of the present study support the feasibility of engineering protein protease inhibitors of mesotrypsin and highlight their therapeutic potential. 1 To whom correspondence should be addressed (email [email protected] ). The atomic co-ordinates...

...Gert SIMONET; Bert BREUGELMANS; Paul PROOST; Ilse CLAEYS; Jozef VAN DAMME; Arnold DE LOOF; Jozef VANDEN BROECK In the last decade, a new serine protease inhibitor family has been described in arthropods. Eight members of the family were purified from locusts and share a conserved cysteine array...

... 2004 5 1 2004 The Biochemical Society, London ©2004 2004 clan compound inhibitor domain repeat MEROPS database peptidase inhibitor protease inhibitor Biochem. J. (2004) 378, 705 716 (Printed in Great Britain) 705 REVIEW ARTICLE Evolutionary families of peptidase inhibitors Neil...

... that of gelatinases rather than collagenases. Hmeprin is inhibited by hydroxamic acid derivatives such as batimastat, galardin and Pro-Leu-Gly-hydroxamate, by TAPI-0 (tumour necrosis factor α protease inhibitor-0) and TAPI-2, and by thiol-based compounds such as captopril. Therapeutic targets for these inhibitors...

[email protected] ). 11 4 2003 15 5 2003 20 5 2003 20 5 2003 The Biochemical Society, London ©2003 The Biochemical Society, London © 2003 gelatinase matrix metalloproteinase protease protease inhibitor zymogen Abbreviations used: APMA, p -aminophenylmercuric acetate...

... of calpastatin synthesis leads to the decrease in its mRNA stability. The existing calpastatin then diminishes, resulting in decreased calpastatin activity in the fusing myoblasts, allowing calpain activation and protein degradation required for fusion. Ca2+-dependent protease cell fusion protease inhibitor...

... latexin was not released. These results show that latexin is synthesized in rat peritoneal mast cells and suggest that it is associated with a unique type of intracellular granules distinct from MCCPA- and histamine-containing secretory granules and lysosomes. heparin histamine protease inhibitor...

... property, possibly acts by suppressing the proteolytic cleavage of envelope glycoprotein gp160 of HIV, which is known to be PC-mediated, particularly by furin and PC7. antiviral property inhibition constant labdane diterpines protease inhibitor Biochem. J. (1999) 338, 107 113 (Printed in Great...