Literature DB >> 34127844

PI3K inhibitors are finally coming of age.

Bart Vanhaesebroeck1, Matthew W D Perry2, Jennifer R Brown3, Fabrice André4, Klaus Okkenhaug5.   

Abstract

Overactive phosphoinositide 3-kinase (PI3K) in cancer and immune dysregulation has spurred extensive efforts to develop therapeutic PI3K inhibitors. Although progress has been hampered by issues such as poor drug tolerance and drug resistance, several PI3K inhibitors have now received regulatory approval - the PI3Kα isoform-selective inhibitor alpelisib for the treatment of breast cancer and inhibitors mainly aimed at the leukocyte-enriched PI3Kδ in B cell malignancies. In addition to targeting cancer cell-intrinsic PI3K activity, emerging evidence highlights the potential of PI3K inhibitors in cancer immunotherapy. This Review summarizes key discoveries that aid the clinical translation of PI3Kα and PI3Kδ inhibitors, highlighting lessons learnt and future opportunities.
© 2021. Springer Nature Limited.

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Year:  2021        PMID： 34127844      PMCID： PMC9297732          DOI： 10.1038/s41573-021-00209-1

Source DB:  PubMed          Journal:  Nat Rev Drug Discov        ISSN： 1474-1776            Impact factor:   112.288


  353 in total

1.  Characterization of a novel p110β-specific inhibitor BL140 that overcomes MDV3100-resistance in castration-resistant prostate cancer cells.

Authors:  Chenchen He; Shaofeng Duan; Liang Dong; Yifen Wang; Qingting Hu; Chunjing Liu; Marcus L Forrest; Jeffrey M Holzbeierlein; Suxia Han; Benyi Li
Journal:  Prostate       Date:  2017-06-20       Impact factor: 4.104

2.  Rheumatic immune-related adverse events secondary to anti-programmed death-1 antibodies and preliminary analysis on the impact of corticosteroids on anti-tumour response: A case series.

Authors:  Emma L Mitchell; Peter Kar Han Lau; Chloe Khoo; David Liew; Jessica Leung; Bonnia Liu; Adam Rischin; Albert G Frauman; Damien Kee; Kortnye Smith; Benjamin Brady; Danny Rischin; Andrew Gibson; Linda Mileshkin; Oliver Klein; Andrew Weickhardt; Surein Arulananda; Mark Shackleton; Grant McArthur; Andrew Östör; Jonathan Cebon; Benjamin Solomon; Russell Rc Buchanan; Ian P Wicks; Serigne Lo; Rodney J Hicks; Shahneen Sandhu
Journal:  Eur J Cancer       Date:  2018-11-13       Impact factor: 9.162

3.  PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy.

Authors:  Chiara Tarantelli; Eugenio Gaudio; Alberto J Arribas; Ivo Kwee; Petra Hillmann; Andrea Rinaldi; Luciano Cascione; Filippo Spriano; Elena Bernasconi; Francesca Guidetti; Laura Carrassa; Roberta Bordone Pittau; Florent Beaufils; Reto Ritschard; Denise Rageot; Alexander Sele; Barbara Dossena; Francesca Maria Rossi; Antonella Zucchetto; Monica Taborelli; Valter Gattei; Davide Rossi; Anastasios Stathis; Georg Stussi; Massimo Broggini; Matthias P Wymann; Andreas Wicki; Emanuele Zucca; Vladimir Cmiljanovic; Doriano Fabbro; Francesco Bertoni
Journal:  Clin Cancer Res       Date:  2017-10-24       Impact factor: 12.531

4.  A selective inhibitor of the p110delta isoform of PI 3-kinase inhibits AML cell proliferation and survival and increases the cytotoxic effects of VP16.

Authors:  C Billottet; V L Grandage; R E Gale; A Quattropani; C Rommel; B Vanhaesebroeck; A Khwaja
Journal:  Oncogene       Date:  2006-05-15       Impact factor: 9.867

5.  Randomized Phase II Study Evaluating Akt Blockade with Ipatasertib, in Combination with Abiraterone, in Patients with Metastatic Prostate Cancer with and without PTEN Loss.

Authors:  Johann S de Bono; Ugo De Giorgi; Daniel Nava Rodrigues; Christophe Massard; Sergio Bracarda; Albert Font; Jose Angel Arranz Arija; Kent C Shih; George Daniel Radavoi; Na Xu; Wai Y Chan; Han Ma; Steven Gendreau; Ruth Riisnaes; Premal H Patel; Daniel J Maslyar; Viorel Jinga
Journal:  Clin Cancer Res       Date:  2018-07-23       Impact factor: 12.531

6.  Molecular Alterations and Everolimus Efficacy in Human Epidermal Growth Factor Receptor 2-Overexpressing Metastatic Breast Cancers: Combined Exploratory Biomarker Analysis From BOLERO-1 and BOLERO-3.

Authors:  Fabrice André; Sara Hurvitz; Angelica Fasolo; Ling-Ming Tseng; Guy Jerusalem; Sharon Wilks; Ruth O'Regan; Claudine Isaacs; Masakazu Toi; Howard Burris; Wei He; Douglas Robinson; Markus Riester; Tetiana Taran; David Chen; Dennis Slamon
Journal:  J Clin Oncol       Date:  2016-04-18       Impact factor: 44.544

7.  Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations.

Authors:  Zachary S Zumsteg; Natasha Morse; Gabriel Krigsfeld; Gaorav Gupta; Daniel S Higginson; Nancy Y Lee; Luc Morris; Ian Ganly; Stephan L Shiao; Simon N Powell; Christine H Chung; Maurizio Scaltriti; José Baselga
Journal:  Clin Cancer Res       Date:  2015-11-20       Impact factor: 12.531

8.  Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine.

Authors:  E H Walker; M E Pacold; O Perisic; L Stephens; P T Hawkins; M P Wymann; R L Williams
Journal:  Mol Cell       Date:  2000-10       Impact factor: 17.970

9.  Genomic Alterations in PIK3CA-Mutated Breast Cancer Result in mTORC1 Activation and Limit the Sensitivity to PI3Kα Inhibitors.

Authors:  Yanyan Cai; Guotai Xu; Fan Wu; Flavia Michelini; Carmen Chan; Xuan Qu; Pier Selenica; Erik Ladewig; Pau Castel; Yuanming Cheng; Alison Zhao; Komal Jhaveri; Eneda Toska; Marta Jimenez; Alexandra Jacquet; Alicia Tran-Dien; Fabrice Andre; Sarat Chandarlapaty; Jorge S Reis-Filho; Pedram Razavi; Maurizio Scaltriti
Journal:  Cancer Res       Date:  2021-03-08       Impact factor: 13.312

10.  Quantification of sensitivity and resistance of breast cancer cell lines to anti-cancer drugs using GR metrics.

Authors:  Marc Hafner; Laura M Heiser; Elizabeth H Williams; Mario Niepel; Nicholas J Wang; James E Korkola; Joe W Gray; Peter K Sorger
Journal:  Sci Data       Date:  2017-11-07       Impact factor: 6.444
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  42 in total

Review 1.  Targeting oncogene and non-oncogene addiction to inflame the tumour microenvironment.

Authors:  Giulia Petroni; Aitziber Buqué; Lisa M Coussens; Lorenzo Galluzzi
Journal:  Nat Rev Drug Discov       Date:  2022-03-15       Impact factor: 84.694

Review 2.  Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021.

Authors:  Qing Wu; Wei Qian; Xiaoli Sun; Shaojie Jiang
Journal:  J Hematol Oncol       Date:  2022-10-08       Impact factor: 23.168

3.  Linear ubiquitination of PTEN impairs its function to promote prostate cancer progression.

Authors:  Yanmin Guo; Jianfeng He; Hailong Zhang; Ran Chen; Lian Li; Xiaojia Liu; Caihu Huang; Zhe Qiang; Zihan Zhou; Yanli Wang; Jian Huang; Xian Zhao; Junke Zheng; Guo-Qiang Chen; Jianxiu Yu
Journal:  Oncogene       Date:  2022-10-03       Impact factor: 8.756

Review 4.  Harnessing TRAIL-induced cell death for cancer therapy: a long walk with thrilling discoveries.

Authors:  Antonella Montinaro; Henning Walczak
Journal:  Cell Death Differ       Date:  2022-10-04       Impact factor: 12.067

5.  Reciprocal regulation of Daxx and PIK3CA promotes colorectal cancer cell growth.

Authors:  Yen-Sung Huang; Chang-Chieh Wu; Che-Chang Chang; Shiu-Feng Huang; Hong-Yi Kuo; Hsiu-Ming Shih
Journal:  Cell Mol Life Sci       Date:  2022-06-19       Impact factor: 9.207

6.  The onset of PI3K-related vascular malformations occurs during angiogenesis and is prevented by the AKT inhibitor miransertib.

Authors:  Piotr Kobialka; Helena Sabata; Sandra D Castillo; Mariona Graupera; Odena Vilalta; Leonor Gouveia; Ana Angulo-Urarte; Laia Muixí; Jasmina Zanoncello; Oscar Muñoz-Aznar; Nagore G Olaciregui; Lucia Fanlo; Anna Esteve-Codina; Cinzia Lavarino; Biola M Javierre; Veronica Celis; Carlota Rovira; Susana López-Fernández; Eulàlia Baselga; Jaume Mora
Journal:  EMBO Mol Med       Date:  2022-06-13       Impact factor: 14.260

7.  Precision Targeting of Mutant PI3Kα in Cancer by Selective Degradation.

Authors:  Bart Vanhaesebroeck; John E Burke; Ralitsa R Madsen
Journal:  Cancer Discov       Date:  2022-01       Impact factor: 38.272

8.  Overcoming resistance to immune checkpoint therapy in PTEN-null prostate cancer by intermittent anti-PI3Kα/β/δ treatment.

Authors:  Zhi Qi; Zihan Xu; Liuzhen Zhang; Yongkang Zou; Jinping Li; Wenyu Yan; Cheng Li; Ningshu Liu; Hong Wu
Journal:  Nat Commun       Date:  2022-01-10       Impact factor: 17.694

Review 9.  Expanding role of PI5P4Ks in cancer: A promising druggable target.

Authors:  Gurpreet K Arora; Lavinia Palamiuc; Brooke M Emerling
Journal:  FEBS Lett       Date:  2021-12-07       Impact factor: 3.864

Review 10.  At a crossroads: how to translate the roles of PI3K in oncogenic and metabolic signalling into improvements in cancer therapy.

Authors:  Neil Vasan; Lewis C Cantley
Journal:  Nat Rev Clin Oncol       Date:  2022-04-28       Impact factor: 65.011
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