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References from CDK2 Inhibition Exerts RB-Independent Antitumor Activity in CDK4/6 Inhibitor–Resistant HR+/HER2− Breast Cancer. Local targets link to admitted publications; unresolved targets remain external evidence.
MONARCH 3: abemaciclib as initial therapy for advanced breast cancer
10.1200/jco.2017.75.6155 · 2017 · External reference
Ribociclib as first-line therapy for HR-positive, advanced breast cancer
10.1056/nejmoa1609709 · 2016 · External reference
Palbociclib and letrozole in advanced breast cancer
10.1056/nejmoa1607303 · 2016 · External reference
The cyclin-dependent kinase 4/6 inhibitor palbociclib in combination with letrozole versus letrozole alone as first-line treatment of oestrogen receptor-positive, HER2-negative, advanced breast cancer (PALOMA-1/TRIO-18): a randomised phase 2 study
10.1016/s1470-2045(14)71159-3 · 2015 · External reference
Overall survival with ribociclib plus fulvestrant in advanced breast cancer
10.1056/nejmoa1911149 · 2020 · External reference
Overall survival with palbociclib and fulvestrant in advanced breast cancer
10.1056/nejmoa1810527 · 2018 · External reference
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
10.1186/bcr2419 · 2009 · External reference
Treating cancer with selective CDK4/6 inhibitors
10.1038/nrclinonc.2016.26 · 2016 · External reference
Targeting CDK4 and CDK6 in cancer
10.1038/s41568-022-00456-3 · 2022 · External reference
Cancer cell cycle dystopia: heterogeneity, plasticity, and therapy
10.1016/j.trecan.2022.04.006 · 2022 · External reference
Polyclonal RB1 mutations and acquired resistance to CDK 4/6 inhibitors in patients with metastatic breast cancer
10.1093/annonc/mdx784 · 2018 · External reference
The genomic landscape of intrinsic and acquired resistance to cyclin-dependent kinase 4/6 inhibitors in patients with hormone receptor-positive metastatic breast cancer
10.1158/2159-8290.cd-19-1390 · 2020 · External reference
MicroRNA-mediated suppression of the TGF-β pathway confers transmissible and reversible CDK4/6 inhibitor resistance
10.1016/j.celrep.2019.02.023 · 2019 · External reference
Acquired CDK6 amplification promotes breast cancer resistance to CDK4/6 inhibitors and loss of ER signaling and dependence
10.1038/onc.2016.379 · 2017 · External reference
The AMBRA1 E3 ligase adaptor regulates the stability of cyclin D
10.1038/s41586-021-03474-7 · 2021 · External reference
PTEN loss mediates clinical cross-resistance to CDK4/6 and PI3Kα inhibitors in breast cancer
10.1158/2159-8290.cd-18-0830 · 2020 · External reference
Loss of the FAT1 tumor suppressor promotes resistance to CDK4/6 inhibitors via the Hippo pathway
10.1016/j.ccell.2018.11.006 · 2018 · External reference
AMBRA1 regulates cyclin D to guard S-phase entry and genomic integrity
10.1038/s41586-021-03422-5 · 2021 · External reference
CRL4AMBRA1 is a master regulator of D-type cyclins
10.1038/s41586-021-03445-y · 2021 · External reference
Mechanisms of sensitivity and resistance to CDK4/6 inhibition
10.1016/j.ccell.2020.03.010 · 2020 · External reference
Cyclin E1 expression and palbociclib efficacy in previously treated hormone receptor-positive metastatic breast cancer
10.1200/jco.18.00925 · 2019 · External reference
Early adaptation and acquired resistance to CDK4/6 inhibition in estrogen receptor-positive breast cancer
10.1158/0008-5472.can-15-0728 · 2016 · External reference
Abstract 1279: development of a selective CDK2-E inhibitor in CCNE driven cancers
10.1158/1538-7445.am2021-1279 · 2021 · External reference
Novel CDK2 inhibitors for treating cancer
10.1021/acsmedchemlett.0c00500 · 2020 · External reference
Expanding control of the tumor cell cycle with a CDK2/4/6 inhibitor
10.1016/j.ccell.2021.08.009 · 2021 · External reference
Abstract ND06: first disclosure of AZD8421, a highly selective CDK2 inhibitor to address resistance to CDK4/6 inhibitors in breast and CCNE1-high cancers
10.1158/1538-7445.am2024-nd06 · 2024 · External reference
BLU-222, an investigational, oral, potent, and highly selective CDK2 inhibitor (CDK2i), as monotherapy in patients (pts) with advanced solid tumors and in combination with ribociclib (RIBO) and fulvestrant (FUL) in HR+/HER2− breast cancer (BC)
10.1200/jco.2024.42.16_suppl.1056 · 2024 · External reference
Cyclin-dependent kinase 2 (CDK2) inhibitors and others novel CDK inhibitors (CDKi) in breast cancer: clinical trials, current impact, and future directions
10.1016/j.critrevonc.2024.104324 · 2024 · External reference
Long-term breast cancer response to CDK4/6 inhibition defined by TP53-mediated geroconversion
10.1016/j.ccell.2024.10.013 · 2024 · External reference
Discrete vulnerability to pharmacological CDK2 inhibition is governed by heterogeneity of the cancer cell cycle
10.1038/s41467-025-56674-4 · 2025 · External reference
Tumor suppressors condition differential responses to the selective CDK2 inhibitor BLU-222
10.1158/0008-5472.can-24-2244 · 2025 · External reference
INX-315, a selective CDK2 inhibitor, induces cell cycle arrest and senescence in solid tumors
10.1158/2159-8290.cd-23-0954 · 2024 · External reference
A code of mono-phosphorylation modulates the function of RB
10.1016/j.molcel.2019.01.004 · 2019 · External reference
SynergyFinder 2.0: visual analytics of multi-drug combination synergies
10.1093/nar/gkaa216 · 2020 · External reference
Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors
10.1016/0065-2571(84)90007-4 · 1984 · External reference
SynergyFinder plus: toward better interpretation and annotation of drug combination screening datasets
10.1016/j.gpb.2022.01.004 · 2022 · External reference
Discovery and saturation analysis of cancer genes across 21 tumour types
10.1038/nature12912 · 2014 · External reference
Multiplexed quantitative phosphoproteomics of cell line and tissue samples
10.1016/bs.mie.2019.07.027 · 2019 · External reference
Multiplexed quantitative proteomics for high-throughput comprehensive proteome comparisons of human cell lines
10.1007/978-1-4939-3341-9_1 · 2016 · External reference
Evaluating multiplexed quantitative phosphopeptide analysis on a hybrid quadrupole mass filter/linear ion trap/orbitrap mass spectrometer
10.1021/ac503934f · 2015 · External reference
MultiNotch MS3 enables accurate, sensitive, and multiplexed detection of differential expression across cancer cell line proteomes
10.1021/ac502040v · 2014 · External reference
Integrated in vivo multiomics analysis identifies p21-activated kinase signaling as a driver of colitis
10.1126/scisignal.aan3580 · 2018 · External reference
A tissue-specific atlas of mouse protein phosphorylation and expression
10.1016/j.cell.2010.12.001 · 2010 · External reference
MS3 eliminates ratio distortion in isobaric multiplexed quantitative proteomics
10.1038/nmeth.1714 · 2011 · External reference
limma powers differential expression analyses for RNA-sequencing and microarray studies
10.1093/nar/gkv007 · 2015 · External reference
GSEApy: a comprehensive package for performing gene set enrichment analysis in Python
10.1093/bioinformatics/btac757 · 2023 · External reference
Molecular signatures database (MSigDB) 3.0
10.1093/bioinformatics/btr260 · 2011 · External reference
Gene set enrichment analysis: a knowledge-based approach for interpreting genome-wide expression profiles
10.1073/pnas.0506580102 · 2005 · External reference
A curated resource for phosphosite-specific signature analysis
10.1074/mcp.tir118.000943 · 2019 · External reference
An atlas of substrate specificities for the human serine/threonine kinome
10.1038/s41586-022-05575-3 · 2023 · External reference
The KSEA App: a web-based tool for kinase activity inference from quantitative phosphoproteomics
10.1093/bioinformatics/btx415 · 2017 · External reference
First-in-human phase 1/2a study of a potent and novel CDK2-selective inhibitor PF-07104091 in patients (pts) with advanced solid tumors, enriched for CDK4/6 inhibitor resistant HR+/HER2− breast cancer
10.1200/jco.2023.41.16_suppl.3010 · 2023 · External reference
WAF1, a potential mediator of p53 tumor suppression
10.1016/0092-8674(93)90500-p · 1993 · External reference
Antibody-based profiling of the phosphoinositide 3-kinase pathway in clinical prostate cancer
10.1158/1078-0432.ccr-04-0130 · 2004 · External reference
Rapid adaptation to CDK2 inhibition exposes intrinsic cell-cycle plasticity
10.1016/j.cell.2023.05.013 · 2023 · External reference
Aberrant FGFR signaling mediates resistance to CDK4/6 inhibitors in ER+ breast cancer
10.1038/s41467-019-09068-2 · 2019 · External reference
Multiomics profiling establishes the polypharmacology of FDA-approved CDK4/6 inhibitors and the potential for differential clinical activity
10.1016/j.chembiol.2019.05.005 · 2019 · External reference
Cdk1 is sufficient to drive the mammalian cell cycle
10.1038/nature06046 · 2007 · External reference
A novel landscape of nuclear human CDK2 substrates revealed by in situ phosphorylation
10.1126/sciadv.aaz9899 · 2020 · External reference
p53 in the DNA-damage-repair process
10.1101/cshperspect.a026070 · 2016 · External reference
Co-targeting CDK2 and CDK4/6 overcomes resistance to aromatase and CDK4/6 inhibitors in ER+ breast cancer
10.1038/s41698-022-00311-6 · 2022 · External reference
CDK4/6 inhibitors induce replication stress to cause long-term cell cycle withdrawal
10.15252/embj.2021108599 · 2022 · External reference
CDK2 regulates collapsed replication fork repair in CCNE1-amplified ovarian cancer cells via homologous recombination
10.1093/narcan/zcad039 · 2023 · External reference
Mechanisms of resistance to CDK4/6 blockade in advanced hormone receptor-positive, HER2-negative breast cancer and emerging therapeutic opportunities
10.1158/1078-0432.ccr-21-2947 · 2022 · External reference
