Sensitivity to splicing modulation of BCL2 family genes defines cancer therapeutic strategies for splicing modulators

Targeting splicing abnormalities in cancer

(2018) Anant A Agrawal et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers

(2018) Michael Seiler et al.   NATURE MEDICINE

Somatic Mutational Landscape of Splicing Factor Genes and Their Functional Consequences across 33 Cancer Types

(2018) Michael Seiler et al.   Cell Reports

Synergistic drug combinations for cancer identified in a CRISPR screen for pairwise genetic interactions

(2017) Kyuho Han et al.   NATURE BIOTECHNOLOGY

Selective degradation of splicing factor CAPERα by anticancer sulfonamides

(2017) Taisuke Uehara et al.   Nature Chemical Biology

From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors

(2017) Avi Ashkenazi et al.   NATURE REVIEWS DRUG DISCOVERY

Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15

(2017) Ting Han et al.   SCIENCE

Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity

(2016) Edward J. Hennessy   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Cobimetinib combined with vemurafenib in advanced BRAFV600-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial

(2016) Paolo A Ascierto et al.   LANCET ONCOLOGY

BCL2 Inhibitors as Anticancer Drugs: A Plethora of Misleading BH3 Mimetics

(2016) R. S. Soderquist et al.   MOLECULAR CANCER THERAPEUTICS

Modulation of splicing catalysis for therapeutic targeting of leukemia with mutations in genes encoding spliceosomal proteins

(2016) Stanley Chun-Wei Lee et al.   NATURE MEDICINE

Therapeutic targeting of splicing in cancer

(2016) Stanley Chun-Wei Lee et al.   NATURE MEDICINE

Combine and conquer: challenges for targeted therapy combinations in early phase trials

(2016) Juanita S. Lopez et al.   Nature Reviews Clinical Oncology

Generation 2.5 Antisense Oligonucleotides Targeting the Androgen Receptor and Its Splice Variants Suppress Enzalutamide-Resistant Prostate Cancer Cell Growth

(2015) Y. Yamamoto et al.   CLINICAL CANCER RESEARCH

The SF3B1 inhibitor spliceostatin A (SSA) elicits apoptosis in chronic lymphocytic leukaemia cells through downregulation of Mcl-1

(2015) M Larrayoz et al.   LEUKEMIA

The spliceosome is a therapeutic vulnerability in MYC-driven cancer

(2015) Tiffany Y.-T. Hsu et al.   NATURE

MYC regulates the core pre-mRNA splicing machinery as an essential step in lymphomagenesis

(2015) Cheryl M. Koh et al.   NATURE

Cancer-Associated SF3B1 Hotspot Mutations Induce Cryptic 3′ Splice Site Selection through Use of a Different Branch Point

(2015) Rachel B. Darman et al.   Cell Reports

Antisense oligonucleotides in cancer

(2014) Daniela Castanotto et al.   CURRENT OPINION IN ONCOLOGY

Combined Vemurafenib and Cobimetinib in BRAF-Mutated Melanoma

(2014) James Larkin et al.   NEW ENGLAND JOURNAL OF MEDICINE

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity

(2014) Zhi-Fu Tao et al.   ACS Medicinal Chemistry Letters

Chemical Perturbation of Mcl-1 Pre-mRNA Splicing to Induce Apoptosis in Cancer Cells

(2013) Yang Gao et al.   ACS Chemical Biology

Genome-wide RNAi screens in human brain tumor isolates reveal a novel viability requirement for PHF5A

(2013) C. G. Hubert et al.   GENES & DEVELOPMENT

Pan-cancer patterns of somatic copy number alteration

(2013) Travis I Zack et al.   NATURE GENETICS

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

(2013) Andrew J Souers et al.   NATURE MEDICINE

BCL2A1is a lineage-specific antiapoptotic melanoma oncogene that confers resistance to BRAF inhibition

(2013) Rizwan Haq et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Chemical Genomics Identifies Small-Molecule MCL1 Repressors and BCL-xL as a Predictor of MCL1 Dependency

(2012) Guo Wei et al.   CANCER CELL

Differential GC Content between Exons and Introns Establishes Distinct Strategies of Splice-Site Recognition

(2012) Maayan Amit et al.   Cell Reports

A Blueprint for Advancing Genetics-Based Cancer Therapy

(2011) William R. Sellers   CELL

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Single-vector inducible lentiviral RNAi system for oncology target validation

(2011) Dmitri Wiederschain et al.   CELL CYCLE

Biological validation that SF3b is a target of the antitumor macrolide pladienolide

(2011) Akira Yokoi et al.   FEBS Journal

Frequent pathway mutations of splicing machinery in myelodysplasia

(2011) Kenichi Yoshida et al.   NATURE

The pINDUCER lentiviral toolkit for inducible RNA interference in vitro and in vivo

(2011) Kristen L. Meerbrey et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of SAP155 as the Target of GEX1A (Herboxidiene), an Antitumor Natural Product

(2010) Makoto Hasegawa et al.   ACS Chemical Biology

Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity

(2010) Wyndham H Wilson et al.   LANCET ONCOLOGY

ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor

(2008) C. Tse et al.   CANCER RESEARCH

The BCL-2 protein family: opposing activities that mediate cell death

(2007) Richard J. Youle et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY