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Multi-omics profiling establishes the polypharmacology of FDA Approved CDK4/6 inhibitors and the potential for differential clinical activity

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What this work says

Outgoing claims: the papers this work cites, builds on, or argues with.

inferredcites →https://doi.org/10.1007/s10637-014-0120-7openalex-snapshot

Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine

inferredcites →https://doi.org/10.1016/j.breast.2016.07.015openalex-snapshot

The genomic landscape of breast cancer and its interaction with host immunity

inferredcites →https://doi.org/10.1016/j.ccell.2016.02.006openalex-snapshot

Overcoming Therapeutic Resistance in HER2-Positive Breast Cancers with CDK4/6 Inhibitors

inferredcites →https://doi.org/10.1016/j.cell.2012.02.053openalex-snapshot

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

inferredcites →https://doi.org/10.1016/j.cels.2018.07.001openalex-snapshot

Coral: Clear and Customizable Visualization of Human Kinome Data

inferredcites →https://doi.org/10.1016/s1470-2045(15)00613-0openalex-snapshot

Fulvestrant plus palbociclib versus fulvestrant plus placebo for treatment of hormone-receptor-positive, HER2-negative metastatic breast cancer that progressed on previous endocrine therapy (PALOMA-3): final analysis of the multicentre, double-blind, phase 3 randomised controlled trial

inferredcites →https://doi.org/10.1021/ac301572topenalex-snapshot

Increasing the Multiplexing Capacity of TMTs Using Reporter Ion Isotopologues with Isobaric Masses

inferredcites →https://doi.org/10.1021/acs.analchem.5b04123openalex-snapshot

Phosphoproteomics in the Age of Rapid and Deep Proteome Profiling

inferredcites →https://doi.org/10.1021/cb500135fopenalex-snapshot

An Inhibitor’s-Eye View of the ATP-Binding Site of CDKs in Different Regulatory States

inferredcites →https://doi.org/10.1021/jm049354hopenalex-snapshot

Discovery of a Potent and Selective Inhibitor of Cyclin-Dependent Kinase 4/6

inferredcites →https://doi.org/10.1021/pr5012608openalex-snapshot

Optimized Chemical Proteomics Assay for Kinase Inhibitor Profiling

inferredcites →https://doi.org/10.1038/nbt.3882openalex-snapshot

Alternative drug sensitivity metrics improve preclinical cancer pharmacogenomics

inferredcites →https://doi.org/10.1038/nbt0517-395openalex-snapshot

Astex shapes CDK4/6 inhibitor for approval

inferredcites →https://doi.org/10.1038/nbt1068openalex-snapshot

A small molecule–kinase interaction map for clinical kinase inhibitors

inferredcites →https://doi.org/10.1038/nmeth.3853openalex-snapshot

Growth rate inhibition metrics correct for confounders in measuring sensitivity to cancer drugs

inferredcites →https://doi.org/10.1038/nrc4000openalex-snapshot

MEK1 and MEK2 inhibitors and cancer therapy: the long and winding road

inferredcites →https://doi.org/10.1038/nrclinonc.2016.26openalex-snapshot

Treating cancer with selective CDK4/6 inhibitors

inferredcites →https://doi.org/10.1038/nrd4504openalex-snapshot

The history and future of targeting cyclin-dependent kinases in cancer therapy

inferredcites →https://doi.org/10.1038/onc.2010.154openalex-snapshot

Therapeutic CDK4/6 inhibition in breast cancer: key mechanisms of response and failure

inferredcites →https://doi.org/10.1038/onc.2016.379openalex-snapshot

Acquired CDK6 amplification promotes breast cancer resistance to CDK4/6 inhibitors and loss of ER signaling and dependence

inferredcites →https://doi.org/10.1038/sj.onc.1210414openalex-snapshot

The ERK1/2 mitogen-activated protein kinase pathway as a master regulator of the G1- to S-phase transition

inferredcites →https://doi.org/10.1056/nejmoa1609709openalex-snapshot

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

inferredcites →https://doi.org/10.1073/pnas.1120985109openalex-snapshot

Oncogene-specific activation of tyrosine kinase networks during prostate cancer progression

inferredcites →https://doi.org/10.1101/003236openalex-snapshot

Characterization of directed differentiation by high-throughput single-cell RNA-Seq

inferredcites →https://doi.org/10.1124/dmd.114.062745openalex-snapshot

Brain Exposure of Two Selective Dual CDK4 and CDK6 Inhibitors and the Antitumor Activity of CDK4 and CDK6 Inhibition in Combination with Temozolomide in an Intracranial Glioblastoma Xenograft

inferredcites →https://doi.org/10.1126/science.1132939openalex-snapshot

The Connectivity Map: Using Gene-Expression Signatures to Connect Small Molecules, Genes, and Disease

inferredcites →https://doi.org/10.1126/science.aan4368openalex-snapshot

The target landscape of clinical kinase drugs

inferredcites →https://doi.org/10.1158/0008-5472.can-15-0728openalex-snapshot

Early Adaptation and Acquired Resistance to CDK4/6 Inhibition in Estrogen Receptor–Positive Breast Cancer

inferredcites →https://doi.org/10.1158/1078-0432.ccr-17-0369openalex-snapshot

Single-Cell Dynamics Determines Response to CDK4/6 Inhibition in Triple-Negative Breast Cancer

inferredcites →https://doi.org/10.1158/1535-7163.1427.3.11openalex-snapshot

Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts

inferredcites →https://doi.org/10.1158/1535-7163.mct-16-0300openalex-snapshot

Spectrum and Degree of CDK Drug Interactions Predicts Clinical Performance

inferredcites →https://doi.org/10.1158/1535-7163.mct-17-0290openalex-snapshot

Preclinical Activity of Abemaciclib Alone or in Combination with Antimitotic and Targeted Therapies in Breast Cancer

inferredcites →https://doi.org/10.1158/1535-7163.targ-13-pr02openalex-snapshot

Abstract PR02: LEE011: An orally bioavailable, selective small molecule inhibitor of CDK4/6– Reactivating Rb in cancer.

inferredcites →https://doi.org/10.1158/1538-7445.am2014-4756openalex-snapshot

Abstract 4756: In vivo efficacy of combined targeting of CDK4/6, ER and PI3K signaling in ER+ breast cancer

inferredcites →https://doi.org/10.1158/1538-7445.am2016-2830openalex-snapshot

Abstract 2830: The major human metabolites of abemaciclib are inhibitors of CDK4 and CDK6

inferredcites →https://doi.org/10.1158/1541-7786.mcr-17-0468openalex-snapshot

Competitive Kinase Enrichment Proteomics Reveals that Abemaciclib Inhibits GSK3β and Activates WNT Signaling

inferredcites →https://doi.org/10.1158/2159-8290.cd-13-0286openalex-snapshot

Molecular Profiling of the Residual Disease of Triple-Negative Breast Cancers after Neoadjuvant Chemotherapy Identifies Actionable Therapeutic Targets

inferredcites →https://doi.org/10.1158/2159-8290.cd-15-0894openalex-snapshot

Targeting CDK4 and CDK6: From Discovery to Therapy

inferredcites →https://doi.org/10.1158/2159-8290.cd-16-0095openalex-snapshot

Efficacy and Safety of Abemaciclib, an Inhibitor of CDK4 and CDK6, for Patients with Breast Cancer, Non–Small Cell Lung Cancer, and Other Solid Tumors

inferredcites →https://doi.org/10.1158/2159-8290.cd-16-0563openalex-snapshot

CDK4/6 Inhibitors: Promising Opportunities beyond Breast Cancer

inferredcites →https://doi.org/10.1158/2159-8290.cd-nb2016-074openalex-snapshot

New Driver Mutations Detected in NSCLC

inferredcites →https://doi.org/10.1182/blood.v96.2.393.014k47_393_397openalex-snapshot

Protein kinase inhibitors flavopiridol and 7-hydroxy-staurosporine down-regulate antiapoptosis proteins in B-cell chronic lymphocytic leukemia

inferredcites →https://doi.org/10.1186/bcr2419openalex-snapshot

PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro

inferredcites →https://doi.org/10.1200/jco.18.00925openalex-snapshot

Cyclin E1 Expression and Palbociclib Efficacy in Previously Treated Hormone Receptor–Positive Metastatic Breast Cancer

inferredcites →https://doi.org/10.1200/jco.2016.34.15_suppl.510openalex-snapshot

MONARCH1: Results from a phase II study of abemaciclib, a CDK4 and CDK6 inhibitor, as monotherapy, in patients with HR+/HER2- breast cancer, after chemotherapy for advanced disease.

inferredcites →https://doi.org/10.1200/jco.2017.73.7585openalex-snapshot

MONARCH 2: Abemaciclib in Combination With Fulvestrant in Women With HR+/HER2− Advanced Breast Cancer Who Had Progressed While Receiving Endocrine Therapy

inferredcites →https://doi.org/10.1200/jco.2017.73.9375openalex-snapshot

Cyclin-Dependent Kinase 4/6 Inhibitors in the Treatment of Breast Cancer: More Breakthroughs and an Embarrassment of Riches

inferredcites →https://doi.org/10.18632/oncotarget.17778openalex-snapshot

Preclinical characterization of abemaciclib in hormone receptor positive breast cancer

inferredcites →https://doi.org/10.18632/oncotarget.18435openalex-snapshot

Biological specificity of CDK4/6 inhibitors: dose response relationship,in vivosignaling, and composite response signature

inferredcites →https://doi.org/10.18632/oncotarget.2270openalex-snapshot

CDK4/6 inhibitors have potent activity in combination with pathway selective therapeutic agents in models of pancreatic cancer

What points at this work

Incoming claims: where this work appears in other papers’ reference lists and arguments.

inferred← citeshttps://doi.org/10.1021/acs.jmedchem.8b00049openalex-snapshot

How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?

inferred← citeshttps://doi.org/10.1186/s13058-019-1230-0openalex-snapshot

Elacestrant (RAD1901) exhibits anti-tumor activity in multiple ER+ breast cancer models resistant to CDK4/6 inhibitors

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