Signaling Pathways in Cancer: Therapeutic Targets, Combinatorial Treatments, and New Developments

EZH2 Inhibition Sensitizes CARM1-High, Homologous Recombination Proficient Ovarian Cancers to PARP Inhibition

(2020) Sergey Karakashev et al.   CANCER CELL

Population Pharmacokinetics of MCLA-128, a HER2/HER3 Bispecific Monoclonal Antibody, in Patients with Solid Tumors

(2020) Aurelia H. M. de Vries Schultink et al.   CLINICAL PHARMACOKINETICS

Pan-cancer analysis of whole genomes

(2020)   NATURE

Reconstructing kinase network topologies from phosphoproteomics data reveals cancer-associated rewiring

(2020) Maruan Hijazi et al.   NATURE BIOTECHNOLOGY

Monitoring protein communities and their responses to therapeutics

(2020) Hanna G. Budayeva et al.   NATURE REVIEWS DRUG DISCOVERY

Small-molecule MDM2/X inhibitors and PROTAC degraders for cancer therapy: advances and perspectives

(2020) Yuan Fang et al.   Acta Pharmaceutica Sinica B

CHK1 Inhibition Is Synthetically Lethal with Loss of B-Family DNA Polymerase Function in Human Lung and Colorectal Cancer Cells

(2020) Rebecca F. Rogers et al.   CANCER RESEARCH

Capivasertib, an AKT Kinase Inhibitor, as Monotherapy or in Combination With Fulvestrant in Patients With AKT1E17K-Mutant, ER-Positive Metastatic Breast Cancer

(2020) Lillian M Smyth et al.   CLINICAL CANCER RESEARCH

PI3K Inhibitors and Their Role as Novel Agents for Targeted Therapy in Lymphoma

(2020) Vladimir Sapon-Cousineau et al.   CURRENT TREATMENT OPTIONS IN ONCOLOGY

Trastuzumab Deruxtecan: First Approval

(2020) Susan J. Keam   DRUGS

Design and synthesis of selective degraders of EGFRL858R/T790M mutant

(2020) Xin Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Preclinical Activity of HER2-Selective Tyrosine Kinase Inhibitor Tucatinib as a Single Agent or in Combination with Trastuzumab or Docetaxel in Solid Tumor Models

(2020) Anita Kulukian et al.   MOLECULAR CANCER THERAPEUTICS

Synthetic Lethality with Trifluridine/Tipiracil and Checkpoint Kinase 1 Inhibitor for Esophageal Squamous Cell Carcinoma

(2020) Shinya Ohashi et al.   MOLECULAR CANCER THERAPEUTICS

Tumour kinome re-wiring governs resistance to palbociclib in oestrogen receptor positive breast cancers, highlighting new therapeutic modalities

(2020) Sunil Pancholi et al.   ONCOGENE

Combined PARP and ATR inhibition potentiates genome instability and cell death in ATM-deficient cancer cells

(2020) Rebecca L. Lloyd et al.   ONCOGENE

Kinase inhibition profiles as a tool to identify kinases for specific phosphorylation sites

(2020) Nikolaus A. Watson et al.   Nature Communications

The genomic landscape of intrinsic and acquired resistance to cyclin-dependent kinase 4/6 inhibitors in patients with hormone receptor positive metastatic breast cancer

(2020) Seth A. Wander et al.   Cancer Discovery

ATM-Deficient Cancers Provide New Opportunities for Precision Oncology

(2020) Nicholas R. Jette et al.   Cancers

Exploring the Synergy between PARP and CHK1 Inhibition in Matched BRCA2 Mutant and Corrected Cells

(2020) Hannah L Smith et al.   Cancers

Dual HER2 Blockade versus a Single Agent in Trastuzumab-Containing Regimens for HER2-Positive Early Breast Cancer: A Systematic Review and Meta-Analysis of Randomized Controlled Trials

(2020) Liuwen Yu et al.   Journal of Oncology

Unbiased Proteomic Profiling Uncovers a Targetable GNAS/PKA/PP2A Axis in Small Cell Lung Cancer Stem Cells

(2020) Garry L. Coles et al.   CANCER CELL

Rad54 Drives ATP Hydrolysis-Dependent DNA Sequence Alignment during Homologous Recombination

(2020) J. Brooks Crickard et al.   CELL

Intestinal microbiota: a new force in cancer immunotherapy

(2020) Zhujiang Dai et al.   Cell Communication and Signaling

RAS-targeted therapies: is the undruggable drugged?

(2020) Amanda R. Moore et al.   NATURE REVIEWS DRUG DISCOVERY

A Phase II Single Arm Pilot Study of the CHK1 Inhibitor Prexasertib ( LY2606368 ) in BRCA Wild‐Type , Advanced Triple‐Negative Breast Cancer

(2020) Margaret E. Gatti‐Mays et al.   ONCOLOGIST

Control of Glucocorticoid Receptor Levels by PTEN Establishes a Failsafe Mechanism for Tumor Suppression

(2020) Hon Yan K. Yip et al.   MOLECULAR CELL

Palbociclib plus letrozole as first-line therapy in estrogen receptor-positive/human epidermal growth factor receptor 2-negative advanced breast cancer with extended follow-up

(2019) H. S. Rugo et al.   BREAST CANCER RESEARCH AND TREATMENT

Illuminating the dark phosphoproteome

(2019) Elise J. Needham et al.   Science Signaling

Direct CDKN2 modulation of CDK4 alters target engagement of CDK4 inhibitor drugs.

(2019) Jennifer L Green et al.   MOLECULAR CANCER THERAPEUTICS

Olaparib and α-specific PI3K inhibitor alpelisib for patients with epithelial ovarian cancer: a dose-escalation and dose-expansion phase 1b trial

(2019) Panagiotis A Konstantinopoulos et al.   LANCET ONCOLOGY

Combined inhibition of STAT3 and DNA repair in palbociclib-resistant ER-positive breast cancer

(2019) Nicole M. Kettner et al.   CLINICAL CANCER RESEARCH

A Phase II Randomized Study of Neoadjuvant Letrozole Plus Alpelisib for Hormone Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Breast Cancer (NEO-ORB)

(2019) Ingrid A. Mayer et al.   CLINICAL CANCER RESEARCH

Genome-wide interrogation of human cancers identifies EGLN1 dependency in clear cell ovarian cancers

(2019) Colles Price et al.   CANCER RESEARCH

DNA Replication Vulnerabilities Render Ovarian Cancer Cells Sensitive to Poly(ADP-Ribose) Glycohydrolase Inhibitors

(2019) Nisha Pillay et al.   CANCER CELL

Capitalizing on Cancer Replication Stress by Preventing PAR Chain Turnover: A New Type of Synthetic Lethality

(2019) Niamh McDermott et al.   CANCER CELL

Selective Degradation of CDK6 by a Palbociclib Based PROTAC

(2019) Sandeep Rana et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6

(2019) Baishan Jiang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Ribociclib plus Trastuzumab in Advanced, HER2-positive Breast Cancer: Results of A Phase Ib/II trial

(2019) Shom Goel et al.   Clinical Breast Cancer

Phase Ib study of the MEK inhibitor cobimetinib (GDC-0973) in combination with the PI3K inhibitor pictilisib (GDC-0941) in patients with advanced solid tumors

(2019) Geoffrey I. Shapiro et al.   INVESTIGATIONAL NEW DRUGS

Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic

(2019) Savithri Ramurthy et al.   JOURNAL OF MEDICINAL CHEMISTRY

Prioritization of cancer therapeutic targets using CRISPR–Cas9 screens

(2019) Fiona M. Behan et al.   NATURE

Alpelisib for PIK3CA-Mutated, Hormone Receptor–Positive Advanced Breast Cancer

(2019) Fabrice André et al.   NEW ENGLAND JOURNAL OF MEDICINE

Targeting ERK1/2 protein-serine/threonine kinases in human cancers

(2019) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Reactivation of PTEN tumor suppressor for cancer treatment through inhibition of a MYC-WWP1 inhibitory pathway

(2019) Yu-Ru Lee et al.   SCIENCE

Werner syndrome helicase is a selective vulnerability of microsatellite instability-high tumor cells

(2019) Simone Lieb et al.   eLife

FAIRLANE, a double-blind placebo-controlled randomized phase II trial of neoadjuvant ipatasertib plus paclitaxel for early triple-negative breast cancer

(2019) M Oliveira et al.   ANNALS OF ONCOLOGY

The PTEN–PI3K Axis in Cancer

(2019) Papa et al.   Biomolecules

Genetic Aberrations in the CDK4 Pathway Are Associated with Innate Resistance to PD-1 Blockade in Chinese Patients with Non-Cutaneous Melanoma

(2019) Jiayi Yu et al.   CLINICAL CANCER RESEARCH

Biomarker Analyses of Response to Cyclin Dependent Kinase 4/6 Inhibition and Endocrine Therapy in Women With Treatment-Naïve Metastatic Breast Cancer

(2019) Richard S. Finn et al.   CLINICAL CANCER RESEARCH

Amplification of the mutation-carrying BRCA2 allele promotes RAD51 loading and PARP inhibitor resistance in the absence of reversion mutations.

(2019) Pyoung Hwa Park et al.   MOLECULAR CANCER THERAPEUTICS

Development of combination therapies to maximize the impact of KRAS-G12C inhibitors in lung cancer

(2019) Miriam Molina-Arcas et al.   Science Translational Medicine

High-Throughput Assessment of Kinome-wide Activation States

(2019) Thierry Schmidlin et al.   Cell Systems

p21 in Cancer Research

(2019) Shamloo et al.   Cancers

Breast cancer statistics, 2019

(2019) Carol E. DeSantis et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Gain-of-Function Mutant p53 R273H Interacts with Replicating DNA and PARP1 in Breast Cancer

(2019) Gu Xiao et al.   CANCER RESEARCH

The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

(2019) Jude Canon et al.   NATURE

PARP Inhibitor Resistance: A Tug-of-War in BRCA-Mutated Cells

(2019) Sylvie M. Noordermeer et al.   TRENDS IN CELL BIOLOGY

PTEN Loss Mediates Clinical Cross-Resistance to CDK4/6 and PI3Kα Inhibitors in Breast Cancer

(2019) Carlotta Costa et al.   Cancer Discovery

The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients

(2019) Jill Hallin et al.   Cancer Discovery

Third-generation epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small cell lung cancer

(2019) Natalie M. Andrews Wright et al.   Translational Lung Cancer Research

Tucatinib, Trastuzumab, and Capecitabine for HER2-Positive Metastatic Breast Cancer

(2019) Rashmi K. Murthy et al.   NEW ENGLAND JOURNAL OF MEDICINE

Trastuzumab Deruxtecan in Previously Treated HER2-Positive Breast Cancer

(2019) Shanu Modi et al.   NEW ENGLAND JOURNAL OF MEDICINE

Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update

(2019) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Efficacy and Determinants of Response to HER Kinase Inhibition in HER2-Mutant Metastatic Breast Cancer

(2019) Lillian M. Smyth et al.   Cancer Discovery

Unbiased Combinatorial Screening Identifies a Bispecific IgG1 that Potently Inhibits HER3 Signaling via HER2-Guided Ligand Blockade

(2018) Cecile A.W. Geuijen et al.   CANCER CELL

Selective Loss of PARG Restores PARylation and Counteracts PARP Inhibitor-Mediated Synthetic Lethality

(2018) Ewa Gogola et al.   CANCER CELL

Abstract PD4-14: GDC-0077 is a selective PI3Kalpha inhibitor that demonstrates robust efficacy inPIK3CAmutant breast cancer models as a single agent and in combination with standard of care therapies

(2018) R Hong et al.   CANCER RESEARCH

Combined c-Met/Trk inhibition overcomes resistance to CDK4/6 inhibitors in Glioblastoma

(2018) Inan Olmez et al.   CANCER RESEARCH

Oncogenic Signaling Pathways in The Cancer Genome Atlas

(2018) Francisco Sanchez-Vega et al.   CELL

BRCA2 Reversion Mutation Associated With Acquired Resistance to Olaparib in Estrogen Receptor-positive Breast Cancer Detected by Genomic Profiling of Tissue and Liquid Biopsy

(2018) Erica L. Gornstein et al.   Clinical Breast Cancer

U.S. Food and Drug Administration Approval: Neratinib for the Extended Adjuvant Treatment of Early Stage HER2-Positive Breast Cancer

(2018) Harpreet Singh et al.   CLINICAL CANCER RESEARCH

A First-in-Human Study of the New Oral Selective Estrogen Receptor Degrader AZD9496 for ER+/HER2−Advanced Breast Cancer

(2018) Erika P. Hamilton et al.   CLINICAL CANCER RESEARCH

MAPK Reliance via Acquired CDK4/6 Inhibitor Resistance in Cancer

(2018) Renée de Leeuw et al.   CLINICAL CANCER RESEARCH

Phthalimide conjugations for the degradation of oncogenic PI3K

(2018) Wenlu Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Recent Advances in Prostate Cancer Treatment and Drug Discovery

(2018) Ekaterina Nevedomskaya et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Ado-Trastuzumab Emtansine for Patients With HER2-Mutant Lung Cancers: Results From a Phase II Basket Trial

(2018) Bob T. Li et al.   JOURNAL OF CLINICAL ONCOLOGY

N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK632) Promotes Inhibition of BRAF through the Induction of Inhibited Dimers

(2018) Michael Grasso et al.   JOURNAL OF MEDICINAL CHEMISTRY

Buparlisib plus fulvestrant in postmenopausal women with hormone-receptor-positive, HER2-negative, advanced breast cancer progressing on or after mTOR inhibition (BELLE-3): a randomised, double-blind, placebo-controlled, phase 3 trial

(2018) Angelo Di Leo et al.   LANCET ONCOLOGY

Kinome rewiring reveals AURKA limits PI3K-pathway inhibitor efficacy in breast cancer

(2018) Hayley J. Donnella et al.   Nature Chemical Biology

Osimertinib in Untreated EGFR-Mutated Advanced Non–Small-Cell Lung Cancer

(2018) Jean-Charles Soria et al.   NEW ENGLAND JOURNAL OF MEDICINE

Synergistic antitumor effects of histone deacetylase inhibitor scriptaid and bortezomib against ovarian cancer cells

(2018) Karolina Janyst et al.   ONCOLOGY REPORTS

Type II RAF inhibitor causes superior ERK pathway suppression compared to type I RAF inhibitor in cells expressing different BRAF mutant types recurrently found in lung cancer

(2018) Noeparast Amir et al.   Oncotarget

Ras-Mediated Activation of the Raf Family Kinases

(2018) Elizabeth M. Terrell et al.   Cold Spring Harbor Perspectives in Medicine

The Genomic Landscape of Endocrine-Resistant Advanced Breast Cancers

(2018) Pedram Razavi et al.   CANCER CELL

GBR1302: Effect of CD3-HER2, a bispecific T cell engager antibody, in trastuzumab-resistant cancers.

(2018) Jonathan Back et al.   JOURNAL OF CLINICAL ONCOLOGY

Suppression of insulin feedback enhances the efficacy of PI3K inhibitors

(2018) Benjamin D. Hopkins et al.   NATURE

HER kinase inhibition in patients with HER2- and HER3-mutant cancers

(2018) David M. Hyman et al.   NATURE

Androgen-targeted therapy in men with prostate cancer: evolving practice and future considerations

(2018) E. David Crawford et al.   PROSTATE CANCER AND PROSTATIC DISEASES

Loss of the FAT1 Tumor Suppressor Promotes Resistance to CDK4/6 Inhibitors via the Hippo Pathway

(2018) Zhiqiang Li et al.   CANCER CELL

Expression of MT4-MMP, EGFR and RB in triple negative breast cancer strongly sensitizes tumors to erlotinib and palbociclib combination therapy

(2018) Pierre Foidart et al.   CLINICAL CANCER RESEARCH

RAF inhibitor PLX8394 selectively disrupts BRAF dimers and RAS-independent BRAF-mutant-driven signaling

(2018) Zhan Yao et al.   NATURE MEDICINE

EAU-ESTRO-SIOG Guidelines on Prostate Cancer. Part 1: Screening, Diagnosis, and Local Treatment with Curative Intent

(2017) Nicolas Mottet et al.   EUROPEAN UROLOGY

A new approach for generating bispecific antibodies based on a common light chain format and the stable architecture of human immunoglobulin G 1

(2017) Camilla De Nardis et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Somatic BRCA1/2 Recovery as a Resistance Mechanism After Exceptional Response to Poly (ADP-ribose) Polymerase Inhibition

(2017) Stephanie Lheureux et al.   JOURNAL OF CLINICAL ONCOLOGY

Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

(2017) Ian Churcher   JOURNAL OF MEDICINAL CHEMISTRY

Mutant p53 in Cancer: Accumulation, Gain-of-Function, and Therapy

(2017) Xuetian Yue et al.   JOURNAL OF MOLECULAR BIOLOGY

Neratinib after trastuzumab-based adjuvant therapy in HER2-positive breast cancer (ExteNET): 5-year analysis of a randomised, double-blind, placebo-controlled, phase 3 trial

(2017) Miguel Martin et al.   LANCET ONCOLOGY

Ipatasertib plus paclitaxel versus placebo plus paclitaxel as first-line therapy for metastatic triple-negative breast cancer (LOTUS): a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial

(2017) Sung-Bae Kim et al.   LANCET ONCOLOGY

ATM, ATR, and DNA-PK: The Trinity at the Heart of the DNA Damage Response

(2017) Andrew N. Blackford et al.   MOLECULAR CELL

BRCA1–BARD1 promotes RAD51-mediated homologous DNA pairing

(2017) Weixing Zhao et al.   NATURE

CDK4/6 inhibition triggers anti-tumour immunity

(2017) Shom Goel et al.   NATURE

The multifaceted roles of PARP1 in DNA repair and chromatin remodelling

(2017) Arnab Ray Chaudhuri et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

PARP inhibitors: Synthetic lethality in the clinic

(2017) Christopher J. Lord et al.   SCIENCE

CDK4/6 or MAPK blockade enhances efficacy of EGFR inhibition in oesophageal squamous cell carcinoma

(2017) Jin Zhou et al.   Nature Communications

Convergent Akt activation drives acquired EGFR inhibitor resistance in lung cancer

(2017) Kirstine Jacobsen et al.   Nature Communications

Phase I Dose-Escalation Study of Taselisib, an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors

(2017) Dejan Juric et al.   Cancer Discovery

HDAC inhibitor PAC-320 induces G2/M cell cycle arrest and apoptosis in human prostate cancer

(2017) Zhixiong Dong et al.   Oncotarget

Phosphoproteomics of Primary Cells Reveals Druggable Kinase Signatures in Ovarian Cancer

(2017) Chiara Francavilla et al.   Cell Reports

First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib

(2016) Dominic I. James et al.   ACS Chemical Biology

First-in-human phase I study of copanlisib (BAY 80-6946), an intravenous pan-class I phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors and non-Hodgkin's lymphomas

(2016) A. Patnaik et al.   ANNALS OF ONCOLOGY

Pictilisib PI3Kinase inhibitor (a phosphatidylinositol 3-kinase [PI3K] inhibitor) plus paclitaxel for the treatment of hormone receptor-positive, HER2-negative, locally recurrent, or metastatic breast cancer: interim analysis of the multicentre, placebo-controlled, phase II randomised PEGGY study

(2016) P. Vuylsteke et al.   ANNALS OF ONCOLOGY

Macrodomains: Structure, Function, Evolution, and Catalytic Activities

(2016) Johannes Gregor Matthias Rack et al.   Annual Review of Biochemistry

An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling

(2016) Zoi Karoulia et al.   CANCER CELL

PDK1-SGK1 Signaling Sustains AKT-Independent mTORC1 Activation and Confers Resistance to PI3Kα Inhibition

(2016) Pau Castel et al.   CANCER CELL

A Landscape of Pharmacogenomic Interactions in Cancer

(2016) Francesco Iorio et al.   CELL

A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER + /HER2 − Metastatic Breast Cancer

(2016) Ingrid A. Mayer et al.   CLINICAL CANCER RESEARCH

Combined Inhibition of Both p110α and p110β Isoforms of Phosphatidylinositol 3-Kinase Is Required for Sustained Therapeutic Effect in PTEN-Deficient, ER + Breast Cancer

(2016) Sarah R. Hosford et al.   CLINICAL CANCER RESEARCH

Phase Ib Study of Safety and Pharmacokinetics of the PI3K Inhibitor SAR245408 with the HER3-Neutralizing Human Antibody SAR256212 in Patients with Solid Tumors

(2016) Vandana G. Abramson et al.   CLINICAL CANCER RESEARCH

Hereditary truncating mutations of DNA repair and other genes inBRCA1/BRCA2/PALB2-negatively tested breast cancer patients

(2016) F. Lhota et al.   CLINICAL GENETICS

Chronic p53-independent p21 expression causes genomic instability by deregulating replication licensing

(2016) Panagiotis Galanos et al.   NATURE CELL BIOLOGY

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

Ribociclib as First-Line Therapy for HR-Positive, Advanced Breast Cancer

(2016) Gabriel N. Hortobagyi et al.   NEW ENGLAND JOURNAL OF MEDICINE

The somatic mutation profiles of 2,433 breast cancers refines their genomic and transcriptomic landscapes

(2016) Bernard Pereira et al.   Nature Communications

Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer

(2016) X. Le et al.   Cancer Discovery

Efficacy of the combination of MEK and CDK4/6 inhibitors in vitro and in vivo in KRAS mutant colorectal cancer models

(2016) Michael S. Lee et al.   Oncotarget

Genome Stability Requires p53

(2016) Christine M. Eischen   Cold Spring Harbor Perspectives in Medicine

A role for the p53 tumour suppressor in regulating the balance between homologous recombination and non-homologous end joining

(2016) Sylvie Moureau et al.   Open Biology

Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras

(2016) Honorine Lebraud et al.   ACS Central Science

EGFR-independent mechanisms of acquired resistance to AZD9291 in EGFR T790M-positive NSCLC patients

(2015) D. Planchard et al.   ANNALS OF ONCOLOGY

Targeting HER2 for the Treatment of Breast Cancer

(2015) Mothaffar F. Rimawi et al.   Annual Review of Medicine

ATR inhibition induces synthetic lethality and overcomes chemoresistance in TP53- or ATM-defective chronic lymphocytic leukemia cells

(2015) M. Kwok et al.   BLOOD

Measurement of PIP3 Levels Reveals an Unexpected Role for p110β in Early Adaptive Responses to p110α-Specific Inhibitors in Luminal Breast Cancer

(2015) Carlotta Costa et al.   CANCER CELL

Feedback Suppression of PI3Kα Signaling in PTEN-Mutated Tumors Is Relieved by Selective Inhibition of PI3Kβ

(2015) Sarit Schwartz et al.   CANCER CELL

Alike but Different: RAF Paralogs and Their Signaling Outputs

(2015) Enrico Desideri et al.   CELL

Integrative Clinical Genomics of Advanced Prostate Cancer

(2015) Dan Robinson et al.   CELL

FDA Approval: Idelalisib Monotherapy for the Treatment of Patients with Follicular Lymphoma and Small Lymphocytic Lymphoma

(2015) B. W. Miller et al.   CLINICAL CANCER RESEARCH

Acquired BRAF inhibitor resistance: A multicenter meta-analysis of the spectrum and frequencies, clinical behaviour, and phenotypic associations of resistance mechanisms

(2015) Douglas B. Johnson et al.   EUROPEAN JOURNAL OF CANCER

Inherited Mutations in 17 Breast Cancer Susceptibility Genes Among a Large Triple-Negative Breast Cancer Cohort Unselected for Family History of Breast Cancer

(2015) Fergus J. Couch et al.   JOURNAL OF CLINICAL ONCOLOGY

RAF inhibitors that evade paradoxical MAPK pathway activation

(2015) Chao Zhang et al.   NATURE

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

AZD9291 in EGFR Inhibitor–Resistant Non–Small-Cell Lung Cancer

(2015) Pasi A. Jänne et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Phase IIb Trial Assessing the Addition of Disulfiram to Chemotherapy for the Treatment of Metastatic Non-Small Cell Lung Cancer

(2015) H. Nechushtan et al.   ONCOLOGIST

The PTEN Tumor Suppressor Forms Homodimers in Solution

(2015) Frank Heinrich et al.   STRUCTURE

The demographics of the ubiquitin system

(2015) Michael J. Clague et al.   TRENDS IN CELL BIOLOGY

A phase IB trial of the oral MEK inhibitor trametinib (GSK1120212) in combination with everolimus in patients with advanced solid tumors

(2014) A. W. Tolcher et al.   ANNALS OF ONCOLOGY

CDK 4/6 Inhibitors Sensitize PIK3CA Mutant Breast Cancer to PI3K Inhibitors

(2014) Sadhna R. Vora et al.   CANCER CELL

Phase I study of the MEK inhibitor trametinib in combination with the AKT inhibitor afuresertib in patients with solid tumors and multiple myeloma

(2014) Anthony W. Tolcher et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Oral epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small cell lung cancer: Comparative pharmacokinetics and drug–drug interactions

(2014) Solange Peters et al.   CANCER TREATMENT REVIEWS

Cancer-Associated PTEN Mutants Act in a Dominant-Negative Manner to Suppress PTEN Protein Function

(2014) Antonella Papa et al.   CELL

FDA Approval: Ado-Trastuzumab Emtansine for the Treatment of Patients with HER2-Positive Metastatic Breast Cancer

(2014) L. Amiri-Kordestani et al.   CLINICAL CANCER RESEARCH

A Phase Ib Dose-Escalation Study of the Oral Pan-PI3K Inhibitor Buparlisib (BKM120) in Combination with the Oral MEK1/2 Inhibitor Trametinib (GSK1120212) in Patients with Selected Advanced Solid Tumors

(2014) P. L. Bedard et al.   CLINICAL CANCER RESEARCH

Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial

(2014) Yi-Long Wu et al.   LANCET ONCOLOGY

SGK3 Mediates INPP4B-Dependent PI3K Signaling in Breast Cancer

(2014) Jessica A. Gasser et al.   MOLECULAR CELL

Convergent loss of PTEN leads to clinical resistance to a PI(3)Kα inhibitor

(2014) Dejan Juric et al.   NATURE

Association of p53/p21 expression and cigarette smoking with tumor progression and poor prognosis in non-small cell lung cancer patients

(2014) DEYAO XIE et al.   ONCOLOGY REPORTS

The Dual RAF/MEK Inhibitor CH5126766/RO5126766 May Be a Potential Therapy for RAS-Mutated Tumor Cells

(2014) Makoto Wada et al.   PLoS One

Assessing PIK3CA and PTEN in Early-Phase Trials with PI3K/AKT/mTOR Inhibitors

(2014) Filip Janku et al.   Cell Reports

A Kinase-Independent Function of CDK6 Links the Cell Cycle to Tumor Angiogenesis

(2013) Karoline Kollmann et al.   CANCER CELL

Antitumor Activity of the Selective Pan-RAF Inhibitor TAK-632 in BRAF Inhibitor-Resistant Melanoma

(2013) A. Nakamura et al.   CANCER RESEARCH

Enhanced Inhibition of ERK Signaling by a Novel Allosteric MEK Inhibitor, CH5126766, That Suppresses Feedback Reactivation of RAF Activity

(2013) Nobuya Ishii et al.   CANCER RESEARCH

Glucocorticoid Receptor Confers Resistance to Antiandrogens by Bypassing Androgen Receptor Blockade

(2013) Vivek K. Arora et al.   CELL

Targeting Activated Akt with GDC-0068, a Novel Selective Akt Inhibitor That Is Efficacious in Multiple Tumor Models

(2013) J. Lin et al.   CLINICAL CANCER RESEARCH

Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma

(2013) J. Rader et al.   CLINICAL CANCER RESEARCH

The recognition and removal of cellular poly(ADP-ribose) signals

(2013) Eva Barkauskaite et al.   FEBS Journal

ATR phosphorylates SMARCAL1 to prevent replication fork collapse

(2013) F. B. Couch et al.   GENES & DEVELOPMENT

Pharmacodynamic Effects and Mechanisms of Resistance to Vemurafenib in Patients With Metastatic Melanoma

(2013) Kerstin Trunzer et al.   JOURNAL OF CLINICAL ONCOLOGY

Phosphoproteomic Profiling Identifies Focal Adhesion Kinase as a Mediator of Docetaxel Resistance in Castrate-Resistant Prostate Cancer

(2013) B. Y. Lee et al.   MOLECULAR CANCER THERAPEUTICS

Panitumumab–FOLFOX4 Treatment and RAS Mutations in Colorectal Cancer

(2013) Jean-Yves Douillard et al.   NEW ENGLAND JOURNAL OF MEDICINE

Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs

(2013) J. Hines et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

mTORC1 Inhibition Is Required for Sensitivity to PI3K p110  Inhibitors in PIK3CA-Mutant Breast Cancer

(2013) M. Elkabets et al.   Science Translational Medicine

Prognostic significance of p21, p27 and survivin protein expression in patients with oral squamous cell carcinoma

(2013) MINGBIN ZHANG et al.   Oncology Letters

The Genetic Landscape of Clinical Resistance to RAF Inhibition in Metastatic Melanoma

(2013) E. M. Van Allen et al.   Cancer Discovery

Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors

(2012) J. Murai et al.   CANCER RESEARCH

Dynamic Reprogramming of the Kinome in Response to Targeted MEK Inhibition in Triple-Negative Breast Cancer

(2012) James S. Duncan et al.   CELL

BRCA1-associated exclusion of 53BP1 from DNA damage sites underlies temporal control of DNA repair

(2012) J. R. Chapman et al.   JOURNAL OF CELL SCIENCE

DNA breaks and chromosome pulverization from errors in mitosis

(2012) Karen Crasta et al.   NATURE

Comprehensive molecular portraits of human breast tumours

(2012) Daniel C. Koboldt et al.   NATURE

Increased Survival with Enzalutamide in Prostate Cancer after Chemotherapy

(2012) Howard I. Scher et al.   NEW ENGLAND JOURNAL OF MEDICINE

Synthetic lethality of Chk1 inhibition combined with p53 and/or p21 loss during a DNA damage response in normal and tumor cells

(2012) S Origanti et al.   ONCOGENE

Melanoma whole-exome sequencing identifies V600E B-RAF amplification-mediated acquired B-RAF inhibitor resistance

(2012) Hubing Shi et al.   Nature Communications

PI3K Inhibition Impairs BRCA1/2 Expression and Sensitizes BRCA-Proficient Triple-Negative Breast Cancer to PARP Inhibition

(2012) Yasir H. Ibrahim et al.   Cancer Discovery

Combining a PI3K Inhibitor with a PARP Inhibitor Provides an Effective Therapy for BRCA1-Related Breast Cancer

(2012) Ashish Juvekar et al.   Cancer Discovery

The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy

(2011) Suzanne E. Wardell et al.   BIOCHEMICAL PHARMACOLOGY

A Systematic Screen for CDK4/6 Substrates Links FOXM1 Phosphorylation to Senescence Suppression in Cancer Cells

(2011) Lars Anders et al.   CANCER CELL

Phosphoinositide-3-Kinase Catalytic Alpha and KRAS Mutations are Important Predictors of Resistance to Therapy with Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Patients with Advanced Non-small Cell Lung Cancer

(2011) Vienna Ludovini et al.   Journal of Thoracic Oncology

Coexistence of PIK3CA and Other Oncogene Mutations in Lung Adenocarcinoma-Rationale for Comprehensive Mutation Profiling

(2011) J. E. Chaft et al.   MOLECULAR CANCER THERAPEUTICS

Abiraterone and Increased Survival in Metastatic Prostate Cancer

(2011) Johann S. de Bono et al.   NEW ENGLAND JOURNAL OF MEDICINE

Nonhomologous end joining drives poly(ADP-ribose) polymerase (PARP) inhibitor lethality in homologous recombination-deficient cells

(2011) A. G. Patel et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Genotypic and Histological Evolution of Lung Cancers Acquiring Resistance to EGFR Inhibitors

(2011) L. V. Sequist et al.   Science Translational Medicine

ER -Dependent E2F Transcription Can Mediate Resistance to Estrogen Deprivation in Human Breast Cancer

(2011) T. W. Miller et al.   Cancer Discovery

Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF

(2010) Sonja J. Heidorn et al.   CELL

Preventing Nonhomologous End Joining Suppresses DNA Repair Defects of Fanconi Anemia

(2010) Adele Adamo et al.   MOLECULAR CELL

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

(2010) Poulikos I. Poulikakos et al.   NATURE

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

(2010) Georgia Hatzivassiliou et al.   NATURE

Triggers for genomic rearrangements: insights into genomic, cellular and environmental influences

(2010) Ram-Shankar Mani et al.   NATURE REVIEWS GENETICS

Allele-specific tumor spectrum in Pten knockin mice

(2010) H. Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Ku70 Corrupts DNA Repair in the Absence of the Fanconi Anemia Pathway

(2010) P. Pace et al.   SCIENCE

AKT-Independent Signaling Downstream of Oncogenic PIK3CA Mutations in Human Cancer

(2009) Krishna M. Vasudevan et al.   CANCER CELL

Strongly Enhanced Antitumor Activity of Trastuzumab and Pertuzumab Combination Treatment on HER2-Positive Human Xenograft Tumor Models

(2009) W. Scheuer et al.   CANCER RESEARCH

Acquired Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non–Small-Cell Lung Cancers Dependent on the Epidermal Growth Factor Receptor Pathway

(2009) Kim-Son H. Nguyen et al.   Clinical Lung Cancer

PTEN hamartoma tumor syndrome: An overview

(2009) Judith A Hobert et al.   GENETICS IN MEDICINE

A History of Cancer Chemotherapy

(2008) Vincent T. DeVita et al.   CANCER RESEARCH

PIK3CA Cooperates with Other Phosphatidylinositol 3'-Kinase Pathway Mutations to Effect Oncogenic Transformation

(2008) K. Oda et al.   CANCER RESEARCH

p21 and p27: roles in carcinogenesis and drug resistance

(2008) Abde M. Abukhdeir et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

Testosterone Surge: Rationale for Gonadotropin-Releasing Hormone Blockers?

(2008) Hendrik van Poppel et al.   UROLOGY