Literature DB >> 22544264

A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation.

Giovanna Bergamini1, Kathryn Bell, Satoko Shimamura, Thilo Werner, Andrew Cansfield, Katrin Müller, Jessica Perrin, Christina Rau, Katie Ellard, Carsten Hopf, Carola Doce, Daniel Leggate, Raffaella Mangano, Toby Mathieson, Alison O'Mahony, Ivan Plavec, Faiza Rharbaoui, Friedrich Reinhard, Mikhail M Savitski, Nigel Ramsden, Emilio Hirsch, Gerard Drewes, Oliver Rausch, Marcus Bantscheff, Gitte Neubauer.   

Abstract

We devised a high-throughput chemoproteomics method that enabled multiplexed screening of 16,000 compounds against native protein and lipid kinases in cell extracts. Optimization of one chemical series resulted in CZC24832, which is to our knowledge the first selective inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with efficacy in in vitro and in vivo models of inflammation. Extensive target- and cell-based profiling of CZC24832 revealed regulation of interleukin-17-producing T helper cell (T(H)17) differentiation by PI3Kγ, thus reinforcing selective inhibition of PI3Kγ as a potential treatment for inflammatory and autoimmune diseases.

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Year:  2012        PMID： 22544264     DOI： 10.1038/nchembio.957

Source DB:  PubMed          Journal:  Nat Chem Biol        ISSN： 1552-4450            Impact factor:   15.040


  48 in total

1.  Rapid structure-activity and selectivity analysis of kinase inhibitors by BioMAP analysis in complex human primary cell-based models.

Authors:  Eric J Kunkel; Ivan Plavec; Dat Nguyen; Jennifer Melrose; Elen S Rosler; Leon T Kao; Yuker Wang; Evangelos Hytopoulos; Anthony C Bishop; Raynard Bateman; Kevan M Shokat; Eugene C Butcher; Ellen L Berg
Journal:  Assay Drug Dev Technol       Date:  2004-08       Impact factor: 1.738

2.  Delayed fragmentation and optimized isolation width settings for improvement of protein identification and accuracy of isobaric mass tag quantification on Orbitrap-type mass spectrometers.

Authors:  Mikhail M Savitski; Gavain Sweetman; Manor Askenazi; Jarrod A Marto; Manja Lang; Nico Zinn; Marcus Bantscheff
Journal:  Anal Chem       Date:  2011-11-04       Impact factor: 6.986

Review 3.  The emerging mechanisms of isoform-specific PI3K signalling.

Authors:  Bart Vanhaesebroeck; Julie Guillermet-Guibert; Mariona Graupera; Benoit Bilanges
Journal:  Nat Rev Mol Cell Biol       Date:  2010-04-09       Impact factor: 94.444

4.  Receptor tyrosine kinases and TLR/IL1Rs unexpectedly activate myeloid cell PI3kγ, a single convergent point promoting tumor inflammation and progression.

Authors:  Michael C Schmid; Christie J Avraamides; Holly C Dippold; Irene Franco; Philippe Foubert; Lesley G Ellies; Lissette M Acevedo; Joan R E Manglicmot; Xiaodan Song; Wolfgang Wrasidlo; Sara L Blair; Mark H Ginsberg; David A Cheresh; Emilio Hirsch; Seth J Field; Judith A Varner
Journal:  Cancer Cell       Date:  2011-06-14       Impact factor: 31.743

5.  Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes.

Authors:  Marcus Bantscheff; Carsten Hopf; Mikhail M Savitski; Antje Dittmann; Paola Grandi; Anne-Marie Michon; Judith Schlegl; Yann Abraham; Isabelle Becher; Giovanna Bergamini; Markus Boesche; Manja Delling; Birgit Dümpelfeld; Dirk Eberhard; Carola Huthmacher; Toby Mathieson; Daniel Poeckel; Valérie Reader; Katja Strunk; Gavain Sweetman; Ulrich Kruse; Gitte Neubauer; Nigel G Ramsden; Gerard Drewes
Journal:  Nat Biotechnol       Date:  2011-01-23       Impact factor: 54.908

6.  Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis.

Authors:  Montserrat Camps; Thomas Rückle; Hong Ji; Vittoria Ardissone; Felix Rintelen; Jeffrey Shaw; Chiara Ferrandi; Christian Chabert; Corine Gillieron; Bernard Françon; Thierry Martin; Denise Gretener; Dominique Perrin; Didier Leroy; Pierre-Alain Vitte; Emilio Hirsch; Matthias P Wymann; Rocco Cirillo; Matthias K Schwarz; Christian Rommel
Journal:  Nat Med       Date:  2005-08-28       Impact factor: 53.440

7.  Treatment with a neutralizing anti-murine interleukin-17 antibody after the onset of collagen-induced arthritis reduces joint inflammation, cartilage destruction, and bone erosion.

Authors:  Erik Lubberts; Marije I Koenders; Birgitte Oppers-Walgreen; Liduine van den Bersselaar; Christina J J Coenen-de Roo; Leo A B Joosten; Wim B van den Berg
Journal:  Arthritis Rheum       Date:  2004-02

8.  PI3Kgamma modulates the cardiac response to chronic pressure overload by distinct kinase-dependent and -independent effects.

Authors:  Enrico Patrucco; Antonella Notte; Laura Barberis; Giulio Selvetella; Angelo Maffei; Mara Brancaccio; Stefano Marengo; Giovanni Russo; Ornella Azzolino; Sergei D Rybalkin; Lorenzo Silengo; Fiorella Altruda; Reinhard Wetzker; Matthias P Wymann; Giuseppe Lembo; Emilio Hirsch
Journal:  Cell       Date:  2004-08-06       Impact factor: 41.582

9.  A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling.

Authors:  Zachary A Knight; Beatriz Gonzalez; Morri E Feldman; Eli R Zunder; David D Goldenberg; Olusegun Williams; Robbie Loewith; David Stokoe; Andras Balla; Balazs Toth; Tamas Balla; William A Weiss; Roger L Williams; Kevan M Shokat
Journal:  Cell       Date:  2006-04-27       Impact factor: 41.582

10.  A selective PIKfyve inhibitor blocks PtdIns(3,5)P(2) production and disrupts endomembrane transport and retroviral budding.

Authors:  Harold B J Jefferies; Frank T Cooke; Parmjit Jat; Christine Boucheron; Tomonobu Koizumi; Masahiko Hayakawa; Hiroyuki Kaizawa; Takahide Ohishi; Paul Workman; Michael D Waterfield; Peter J Parker
Journal:  EMBO Rep       Date:  2008-01-11       Impact factor: 8.807
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  47 in total

Review 1.  Metabolic control of the Treg/Th17 axis.

Authors:  Joseph Barbi; Drew Pardoll; Fan Pan
Journal:  Immunol Rev       Date:  2013-03       Impact factor: 12.988

2.  Catalytic in vivo protein knockdown by small-molecule PROTACs.

Authors:  Daniel P Bondeson; Alina Mares; Ian E D Smith; Eunhwa Ko; Sebastien Campos; Afjal H Miah; Katie E Mulholland; Natasha Routly; Dennis L Buckley; Jeffrey L Gustafson; Nico Zinn; Paola Grandi; Satoko Shimamura; Giovanna Bergamini; Maria Faelth-Savitski; Marcus Bantscheff; Carly Cox; Deborah A Gordon; Ryan R Willard; John J Flanagan; Linda N Casillas; Bartholomew J Votta; Willem den Besten; Kristoffer Famm; Laurens Kruidenier; Paul S Carter; John D Harling; Ian Churcher; Craig M Crews
Journal:  Nat Chem Biol       Date:  2015-06-10       Impact factor: 15.040

Review 3.  The critical role of Akt in cardiovascular function.

Authors:  Prasanna Abeyrathna; Yunchao Su
Journal:  Vascul Pharmacol       Date:  2015-05-27       Impact factor: 5.773

4.  Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694.

Authors:  Yiming Zhong; Shuai Dong; Ethan Strattan; Li Ren; Jonathan P Butchar; Kelsey Thornton; Anjali Mishra; Pierluigi Porcu; J Michael Bradshaw; Angelina Bisconte; Timothy D Owens; Erik Verner; Ken A Brameld; Jens Oliver Funk; Ronald J Hill; Amy J Johnson; Jason A Dubovsky
Journal:  J Biol Chem       Date:  2015-01-15       Impact factor: 5.157

5.  Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor.

Authors:  Douglas W Thomson; Daniel Poeckel; Nico Zinn; Christina Rau; Katrin Strohmer; Anne J Wagner; Alan P Graves; Jessica Perrin; Marcus Bantscheff; Birgit Duempelfeld; Viera Kasparcova; Joshi M Ramanjulu; G Scott Pesiridis; Marcel Muelbaier; Giovanna Bergamini
Journal:  ACS Med Chem Lett       Date:  2019-03-11       Impact factor: 4.345

6.  Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.

Authors:  Catherine A Evans; Tao Liu; André Lescarbeau; Somarajan J Nair; Louis Grenier; Johan A Pradeilles; Quentin Glenadel; Thomas Tibbitts; Ann M Rowley; Jonathan P DiNitto; Erin E Brophy; Erin L O'Hearn; Janid A Ali; David G Winkler; Stanley I Goldstein; Patrick O'Hearn; Christian M Martin; Jennifer G Hoyt; John R Soglia; Culver Cheung; Melissa M Pink; Jennifer L Proctor; Vito J Palombella; Martin R Tremblay; Alfredo C Castro
Journal:  ACS Med Chem Lett       Date:  2016-07-22       Impact factor: 4.345

7.  CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model.

Authors:  Andrew D Cansfield; Tammy Ladduwahetty; Mihiro Sunose; Katie Ellard; Rosemary Lynch; Anthea L Newton; Ann Lewis; Gavin Bennett; Nico Zinn; Douglas W Thomson; Anne J Rüger; John T Feutrill; Oliver Rausch; Alan P Watt; Giovanna Bergamini
Journal:  ACS Med Chem Lett       Date:  2016-06-10       Impact factor: 4.345

Review 8.  Recent syntheses of PI3K/Akt/mTOR signaling pathway inhibitors.

Authors:  Mark E Welker; George Kulik
Journal:  Bioorg Med Chem       Date:  2013-05-09       Impact factor: 3.641

9.  Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.

Authors:  Tanya Paquet; Claire Le Manach; Diego González Cabrera; Yassir Younis; Philipp P Henrich; Tara S Abraham; Marcus C S Lee; Rajshekhar Basak; Sonja Ghidelli-Disse; María José Lafuente-Monasterio; Marcus Bantscheff; Andrea Ruecker; Andrew M Blagborough; Sara E Zakutansky; Anne-Marie Zeeman; Karen L White; David M Shackleford; Janne Mannila; Julia Morizzi; Christian Scheurer; Iñigo Angulo-Barturen; María Santos Martínez; Santiago Ferrer; Laura María Sanz; Francisco Javier Gamo; Janette Reader; Mariette Botha; Koen J Dechering; Robert W Sauerwein; Anchalee Tungtaeng; Pattaraporn Vanachayangkul; Chek Shik Lim; Jeremy Burrows; Michael J Witty; Kennan C Marsh; Christophe Bodenreider; Rosemary Rochford; Suresh M Solapure; María Belén Jiménez-Díaz; Sergio Wittlin; Susan A Charman; Cristina Donini; Brice Campo; Lyn-Marie Birkholtz; Kirsten K Hanson; Gerard Drewes; Clemens H M Kocken; Michael J Delves; Didier Leroy; David A Fidock; David Waterson; Leslie J Street; Kelly Chibale
Journal:  Sci Transl Med       Date:  2017-04-26       Impact factor: 17.956

10.  A public-private partnership to unlock the untargeted kinome.

Authors:  Stefan Knapp; Paulo Arruda; Julian Blagg; Stephen Burley; David H Drewry; Aled Edwards; Doriano Fabbro; Paul Gillespie; Nathanael S Gray; Bernhard Kuster; Karen E Lackey; Paulo Mazzafera; Nicholas C O Tomkinson; Timothy M Willson; Paul Workman; William J Zuercher
Journal:  Nat Chem Biol       Date:  2013-01       Impact factor: 15.040
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