Literature DB >> 12127536

Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis.

Christopher A Willoughby1, Herbert G Bull, Margarita Garcia-Calvo, Joanne Jiang, Kevin T Chapman, Nancy A Thornberry.   

Abstract

A novel class of small molecule human granzyme B inhibitors is reported. Compound 20 has a K(i) of 7 nM against human granzyme B and blocks CTL mediated apoptosis with an IC(50) of 3 micromolar.

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Year:  2002        PMID： 12127536     DOI： 10.1016/s0960-894x(02)00363-3

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


  17 in total

1.  A lead discovery strategy driven by a comprehensive analysis of proteases in the peptide substrate space.

Authors:  Sai Chetan K Sukuru; Florian Nigsch; Jean Quancard; Martin Renatus; Rajiv Chopra; Natasja Brooijmans; Dmitri Mikhailov; Zhan Deng; Allen Cornett; Jeremy L Jenkins; Ulrich Hommel; John W Davies; Meir Glick
Journal:  Protein Sci       Date:  2010-11       Impact factor: 6.725

2.  The major human and mouse granzymes are structurally and functionally divergent.

Authors:  Dion Kaiserman; Catherina H Bird; Jiuru Sun; Antony Matthews; Kheng Ung; James C Whisstock; Philip E Thompson; Joseph A Trapani; Phillip I Bird
Journal:  J Cell Biol       Date:  2006-11-20       Impact factor: 10.539

Review 3.  Death by a thousand cuts: granzyme pathways of programmed cell death.

Authors:  Dipanjan Chowdhury; Judy Lieberman
Journal:  Annu Rev Immunol       Date:  2008       Impact factor: 28.527

4.  Inhibition of Granzyme B by PI-9 protects prostate cancer cells from apoptosis.

Authors:  Manisha Ray; Daniel R Hostetter; Carly R K Loeb; Jeffry Simko; Charles S Craik
Journal:  Prostate       Date:  2011-09-14       Impact factor: 4.104

5.  Live cell evaluation of granzyme delivery and death receptor signaling in tumor cells targeted by human natural killer cells.

Authors:  Alexandra C Vrazo; Adrianne E Hontz; Sarah K Figueira; Braeden L Butler; Julie M Ferrell; Brock F Binkowski; Jinzhu Li; Kimberly A Risma
Journal:  Blood       Date:  2015-06-29       Impact factor: 22.113

6.  The granzyme B-Serpinb9 axis controls the fate of lymphocytes after lysosomal stress.

Authors:  C H Bird; M E Christensen; M S J Mangan; M D Prakash; K A Sedelies; M J Smyth; I Harper; N J Waterhouse; P I Bird
Journal:  Cell Death Differ       Date:  2014-01-31       Impact factor: 15.828

7.  Granzyme B PET Imaging as a Predictive Biomarker of Immunotherapy Response.

Authors:  Benjamin M Larimer; Eric Wehrenberg-Klee; Frank Dubois; Anila Mehta; Taylor Kalomeris; Keith Flaherty; Genevieve Boland; Umar Mahmood
Journal:  Cancer Res       Date:  2017-05-01       Impact factor: 12.701

8.  Granzyme H destroys the function of critical adenoviral proteins required for viral DNA replication and granzyme B inhibition.

Authors:  Felipe Andrade; Edward Fellows; Dieter E Jenne; Antony Rosen; C S H Young
Journal:  EMBO J       Date:  2007-03-15       Impact factor: 11.598

9.  A Novel Serpin Regulatory Mechanism: SerpinB9 IS REVERSIBLY INHIBITED BY VICINAL DISULFIDE BOND FORMATION IN THE REACTIVE CENTER LOOP.

Authors:  Matthew S J Mangan; Catherina H Bird; Dion Kaiserman; Anthony Y Matthews; Corinne Hitchen; David L Steer; Philip E Thompson; Phillip I Bird
Journal:  J Biol Chem       Date:  2015-12-15       Impact factor: 5.157

10.  Granzyme B Induces IRF-3 Phosphorylation through a Perforin-Independent Proteolysis-Dependent Signaling Cascade without Inducing Cell Death.

Authors:  Eric J Gapud; Maria Isabel Trejo-Zambrano; Eduardo Gomez-Banuelos; Eleni Tiniakou; Brendan Antiochos; David J Granville; Felipe Andrade; Livia Casciola-Rosen; Antony Rosen
Journal:  J Immunol       Date:  2020-12-07       Impact factor: 5.422
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