Literature DB >> 17080027

PI3Kgamma inhibition: towards an 'aspirin of the 21st century'?

Thomas Rückle1, Matthias K Schwarz, Christian Rommel.   

Abstract

Class IB phosphatidylinositol 3-kinase p110gamma (PI3Kgamma) has gained increasing attention as a promising drug target for the treatment of inflammatory disease. Extensive target-validation data are available, which are derived from studies using both pharmacological and genetic tools. More recent findings have uncovered further therapeutic applications for PI3Kgamma inhibitors, opening up potentially huge opportunities for these drugs. Several companies have been pursuing small-molecule PI3Kgamma inhibitor projects, but none of them has progressed to the clinic yet. Here, we discuss the insights gained so far and the main challenges that are emerging on the path to developing PI3Kgamma inhibitors for the treatment of human disease.

Entities:  

Mesh:

Substances:

Year:  2006        PMID: 17080027     DOI: 10.1038/nrd2145

Source DB:  PubMed          Journal:  Nat Rev Drug Discov        ISSN: 1474-1776            Impact factor:   84.694


  89 in total

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

Authors:  Giovanna Bergamini; 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
Journal:  Nat Chem Biol       Date:  2012-04-29       Impact factor: 15.040

2.  Chemical space sampling by different scoring functions and crystal structures.

Authors:  Natasja Brooijmans; Christine Humblet
Journal:  J Comput Aided Mol Des       Date:  2010-04-18       Impact factor: 3.686

Review 3.  Molecules in medicine mini-review: isoforms of PI3K in biology and disease.

Authors:  Bart Vanhaesebroeck; Maria A Whitehead; Roberto Piñeiro
Journal:  J Mol Med (Berl)       Date:  2015-12-10       Impact factor: 4.599

Review 4.  Lymphocyte cell motility: the twisting, turning tale of phosphoinositide 3-kinase.

Authors:  J S Oak; M P Matheu; I Parker; M D Cahalan; D A Fruman
Journal:  Biochem Soc Trans       Date:  2007-11       Impact factor: 5.407

Review 5.  Phosphoinositide 3-kinase signalling in lung disease: leucocytes and beyond.

Authors:  David A Medina-Tato; Stephen G Ward; Malcolm L Watson
Journal:  Immunology       Date:  2007-08       Impact factor: 7.397

Review 6.  G protein betagamma subunits as targets for small molecule therapeutic development.

Authors:  Alan V Smrcka; David M Lehmann; Axel L Dessal
Journal:  Comb Chem High Throughput Screen       Date:  2008-06       Impact factor: 1.339

7.  Isoform-selective phosphoinositide 3'-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: a novel therapeutic approach.

Authors:  Matthias Niedermeier; Bryan T Hennessy; Zachary A Knight; Marina Henneberg; Jianhua Hu; Antonina V Kurtova; William G Wierda; Michael J Keating; Kevan M Shokat; Jan A Burger
Journal:  Blood       Date:  2009-03-24       Impact factor: 22.113

Review 8.  PI3K Inhibitors in Cancer: Clinical Implications and Adverse Effects.

Authors:  Rosalin Mishra; Hima Patel; Samar Alanazi; Mary Kate Kilroy; Joan T Garrett
Journal:  Int J Mol Sci       Date:  2021-03-27       Impact factor: 5.923

9.  Evaluating PI3 kinase isoforms using Transcreener ADP assays.

Authors:  Tony A Klink; Karen M Kleman-Leyer; Andrew Kopp; Thane A Westermeyer; Robert G Lowery
Journal:  J Biomol Screen       Date:  2008-06-19

10.  Ras is an indispensable coregulator of the class IB phosphoinositide 3-kinase p87/p110gamma.

Authors:  Barbara Kurig; Aliaksei Shymanets; Thomas Bohnacker; Carsten Brock; Mohammad Reza Ahmadian; Michael Schaefer; Antje Gohla; Christian Harteneck; Matthias P Wymann; Elisabeth Jeanclos; Bernd Nürnberg
Journal:  Proc Natl Acad Sci U S A       Date:  2009-11-11       Impact factor: 11.205

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.