Literature DB >> 22863202

Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.

Ian Bruce1, Mohammed Akhlaq, Graham C Bloomfield, Emma Budd, Brian Cox, Bernard Cuenoud, Peter Finan, Peter Gedeck, Julia Hatto, Judy F Hayler, Denise Head, Thomas Keller, Louise Kirman, Catherine Leblanc, Darren Le Grand, Clive McCarthy, Desmond O'Connor, Charles Owen, Mrinalini S Oza, Gaynor Pilgrim, Nicola E Press, Lilya Sviridenko, Lewis Whitehead.   

Abstract

Using a parallel synthesis approach to target a non-conserved region of the PI3K catalytic domain a pan-PI3K inhibitor 1 was elaborated to provide alpha, delta and gamma isoform selective Class I PI3K inhibitors 21, 24, 26 and 27. The compounds had good cellular activity and were selective against protein kinases and other members of the PI3K superfamily including mTOR and DNA-PK.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22863202     DOI： 10.1016/j.bmcl.2012.07.042

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


  11 in total

1.  Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α.

Authors:  Kira Gritsman; Haluk Yuzugullu; Thanh Von; Howard Yan; Linda Clayton; Christine Fritsch; Sauveur-Michel Maira; Gregory Hollingworth; Christine Choi; Tulasi Khandan; Mahnaz Paktinat; Rachel O Okabe; Thomas M Roberts; Jean J Zhao
Journal:  J Clin Invest       Date:  2014-02-24       Impact factor: 14.808

2.  Non-canonical Bromodomain within DNA-PKcs Promotes DNA Damage Response and Radioresistance through Recognizing an IR-Induced Acetyl-Lysine on H2AX.

Authors:  Li Wang; Ling Xie; Srinivas Ramachandran; YuanYu Lee; Zhen Yan; Li Zhou; Krzysztof Krajewski; Feng Liu; Cheng Zhu; David J Chen; Brian D Strahl; Jian Jin; Nikolay V Dokholyan; Xian Chen
Journal:  Chem Biol       Date:  2015-06-25

3.  Dermatologic adverse events related to the PI3Kα inhibitor alpelisib (BYL719) in patients with breast cancer.

Authors:  Diana G Wang; Dulce M Barrios; Victoria S Blinder; Jacqueline F Bromberg; Pamela R Drullinsky; Samuel A Funt; Komal L Jhaveri; Diana E Lake; Tomas Lyons; Shanu Modi; Pedram Razavi; Michelle Sidel; Tiffany A Traina; Linda T Vahdat; Mario E Lacouture
Journal:  Breast Cancer Res Treat       Date:  2020-06-29       Impact factor: 4.872

4.  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

Review 5.  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

6.  High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds.

Authors:  Jia Wang; Grace Qun Gong; Yan Zhou; Woo-Jeong Lee; Christina Maree Buchanan; William Alexander Denny; Gordon William Rewcastle; Jackie Diane Kendall; James Michael Jeremy Dickson; Jack Urquhart Flanagan; Peter Robin Shepherd; De-Hua Yang; Ming-Wei Wang
Journal:  Acta Pharmacol Sin       Date:  2018-07-10       Impact factor: 6.150

7.  Disease-related mutations in PI3Kγ disrupt regulatory C-terminal dynamics and reveal a path to selective inhibitors.

Authors:  Zied Gaieb; Kaelin D Fleming; Manoj K Rathinaswamy; Chiara Borsari; Noah J Harris; Brandon E Moeller; Matthias P Wymann; Rommie E Amaro; John E Burke
Journal:  Elife       Date:  2021-03-04       Impact factor: 8.140

Review 8.  The role of PI3Kγ in the immune system: new insights and translational implications.

Authors:  Stephen M Lanahan; Matthias P Wymann; Carrie L Lucas
Journal:  Nat Rev Immunol       Date:  2022-03-23       Impact factor: 53.106

Review 9.  Recent development of ATP-competitive small molecule phosphatidylinostitol-3-kinase inhibitors as anticancer agents.

Authors:  Yu Liu; Wen-Zhu Wan; Yan Li; Guan-Lian Zhou; Xin-Guang Liu
Journal:  Oncotarget       Date:  2017-01-24

10.  A PI3K p110β-Rac signalling loop mediates Pten-loss-induced perturbation of haematopoiesis and leukaemogenesis.

Authors:  Haluk Yuzugullu; Lukas Baitsch; Thanh Von; Allison Steiner; Haoxuan Tong; Jing Ni; Linda K Clayton; Roderick Bronson; Thomas M Roberts; Kira Gritsman; Jean J Zhao
Journal:  Nat Commun       Date:  2015-10-07       Impact factor: 14.919
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