Research graph
References from Pharmacological translation of cancer missense mutations for therapeutic targeting with small molecules. Local targets link to admitted publications; unresolved targets remain external evidence.
Systematic discovery of mutation-directed neo-protein-protein interactions in cancer
10.1016/j.cell.2022.04.014 · 2022 · External reference
Decoding the functional impact of the cancer genome through protein-protein interactions
2025 · External reference
Hotspots of human mutation
10.1016/j.tig.2020.10.003 · 2021 · External reference
Oncogenes and tumor suppressor genes: functions and roles in cancers
10.1002/mco2.582 · 2024 · External reference
Exploring the genetic orchestra of cancer: the interplay between oncogenes and tumor-suppressor genes
10.3390/cancers17071082 · 2025 · External reference
Cell states in cancer: drivers, passengers, and trailers
10.1158/2159-8290.cd-23-1510 · 2024 · External reference
Implications of disease-related mutations at protein-protein interfaces
10.1016/j.sbi.2021.11.012 · 2022 · External reference
Assessing computational tools for predicting protein stability changes upon missense mutations using a new dataset
10.1002/pro.4861 · 2024 · External reference
mCSM-PPI2: predicting the effects of mutations on protein-protein interactions
10.1093/nar/gkz383 · 2019 · External reference
PremPDI estimates and interprets the effects of missense mutations on protein-DNA interactions
10.1371/journal.pcbi.1006615 · 2018 · External reference
PremPRI: predicting the effects of missense mutations on protein-RNA interactions
10.3390/ijms21155560 · 2020 · External reference
RosettaDDGPrediction for high-throughput mutational scans: from stability to binding
10.1002/pro.4527 · 2023 · External reference
Systematic evaluation of computational tools to predict the effects of mutations on protein stability in the absence of experimental structures
2022 · External reference
Accurate proteome-wide missense variant effect prediction with AlphaMissense
2023 · External reference
AlphaMissense for identifying pathogenic missense mutations in DNA damage repair genes in cancer
2025 · External reference
Unresolved reference
External reference
CADD v1.7: using protein language models, regulatory CNNs and other nucleotide-level scores to improve genome-wide variant predictions
10.1093/nar/gkad989 · 2024 · External reference
Accelerated missense mutation identification in intrinsically disordered proteins using deep learning
10.1021/acs.biomac.4c01124 · 2025 · External reference
Prioritizing disease-associated missense variants with chemoproteomic-detected amino acids
10.1016/j.ajhg.2025.04.017 · 2025 · External reference
Predicting deleterious amino acid substitutions
10.1101/gr.176601 · 2001 · External reference
A method and server for predicting damaging missense mutations
10.1038/nmeth0410-248 · 2010 · External reference
Accurate identification and mechanistic evaluation of pathogenic missense variants with Rhapsody-2
10.1073/pnas.2418100122 · 2025 · External reference
FoldX 5.0: working with RNA, small molecules and a new graphical interface
10.1093/bioinformatics/btz184 · 2019 · External reference
DynaMut: predicting the impact of mutations on protein conformation, flexibility and stability
10.1093/nar/gky300 · 2018 · External reference
REVEL: an ensemble method for predicting the pathogenicity of rare missense variants
10.1016/j.ajhg.2016.08.016 · 2016 · External reference
Inferring the molecular and phenotypic impact of amino acid variants with MutPred2
10.1038/s41467-020-19669-x · 2020 · External reference
Ensemble learning for disease prediction: a review
10.3390/healthcare11121808 · 2023 · External reference
IntOGen-mutations identifies cancer drivers across tumor types
10.1038/nmeth.2642 · 2013 · External reference
Exome-scale discovery of hotspot mutation regions in human cancer using 3D protein structure
10.1158/0008-5472.can-15-3190 · 2016 · External reference
CanDrA: cancer-specific driver missense mutation annotation with optimized features
10.1371/journal.pone.0077945 · 2013 · External reference
Cancer driver mutations: predictions and reality
10.1016/j.molmed.2023.03.007 · 2023 · External reference
10.1093/nar/gkae1090
10.1093/nar/gkae1090 · External reference
COSMIC: a curated database of somatic variants and clinical data for cancer
10.1093/nar/gkad986 · 2024 · External reference
dbNSFP: a lightweight database of human nonsynonymous SNPs and their functional predictions
10.1002/humu.21517 · 2011 · External reference
Variant interpretation using population databases: lessons from gnomAD
10.1002/humu.24309 · 2022 · External reference
Missense mutations in cancer: in silico predictions, developing treatments, and overcoming cell resistance
2025 · External reference
Cancer biomarkers: emerging trends and clinical implications for personalized treatment
10.1016/j.cell.2024.02.041 · 2024 · External reference
Sotorasib: a KRASG12C inhibitor for non-small cell lung cancer
10.1016/j.tips.2022.03.011 · 2022 · External reference
Synthesis of adagrasib (MRTX849), a covalent KRASG12C inhibitor drug for the treatment of cancer
10.1021/acs.orglett.2c04266 · 2023 · External reference
Cracking the EGFR code: cancer biology, resistance mechanisms, and future therapeutic frontiers
10.1016/j.pharmr.2025.100076 · 2025 · External reference
BRAF V600E-mutant cancers treated with vemurafenib alone or in combination with everolimus, sorafenib, or crizotinib or with paclitaxel and carboplatin (VEM-PLUS) study
10.1038/s41698-022-00341-0 · 2023 · External reference
Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3-mutated acute myeloid leukemia
10.1007/s10637-017-0470-z · 2017 · External reference
Precision targeted therapy with BLU-667 for RET-driven cancers
10.1158/2159-8290.cd-18-0338 · 2018 · External reference
Discovery of nanomolar-affinity pharmacological chaperones stabilizing the oncogenic p53 mutant Y220C
10.1021/acsptsci.2c00164 · 2022 · External reference
Discovery of rezatapopt (PC14586), a first-in-class, small-molecule reactivator of p53 Y220C mutant in development
10.1021/acsmedchemlett.4c00379 · 2024 · External reference
Rescuing the function of missense-mutated tumor suppressor VHL using stabilizing small molecules
2026 · External reference
Discovery of AG-120 (ivosidenib): a first-in-class mutant IDH1 inhibitor for the treatment of IDH1 mutant cancers
10.1021/acsmedchemlett.7b00421 · 2018 · External reference
AG-221, a first-in-class therapy targeting acute myeloid leukemia harboring oncogenic IDH2 mutations
10.1158/2159-8290.cd-16-1034 · 2017 · External reference
Insights into the aberrant activity of mutant EGFR kinase domain and drug recognition
10.1016/j.str.2012.11.014 · 2013 · External reference
PF-06463922, an ALK/ROS1 inhibitor, overcomes resistance to first and second generation ALK inhibitors in preclinical models
10.1016/j.ccell.2015.05.010 · 2015 · External reference
The irreversible FLT3 inhibitor FF-10101 is active against a diversity of FLT3 inhibitor resistance mechanisms
10.1158/1535-7163.mct-21-0317 · 2022 · External reference
Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA
10.1038/s41467-023-44376-8 · 2024 · External reference
Principles of cancer therapy: oncogene and non-oncogene addiction
10.1016/j.cell.2009.02.024 · 2009 · External reference
Targeting the BRCA1/2 deficient cancer with PARP inhibitors: clinical outcomes and mechanistic insights
10.3389/fcell.2023.1133472 · 2023 · External reference
Chromatin remodeling and cancer: the critical influence of the SWI/SNF complex
10.1186/s13072-025-00590-w · 2025 · External reference
Synthetic lethality: targeting SMARCA2 ATPase in SMARCA4-deficient tumors - a review of patent literature from 2019-30 June 2023
10.1080/13543776.2024.2338111 · 2024 · External reference
PRT3789 is a first-in-human SMARCA2-selective degrader that induces synthetic lethality in SMARCA4-mutated cancers
10.1158/0008-5472.can-25-1141 · 2026 · External reference
Rational design of potent small-molecule SMARCA2/A4 degraders acting via the recruitment of FBXO22
10.1038/s41467-025-64669-4 · 2025 · External reference
Mechanistic dissection of SMARCA2/4 molecular glues reveals programmable switching between DCAF16 and FBXO22
2026 · External reference
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK)
10.1021/jm2007613 · 2011 · External reference
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation
10.1016/j.bmcl.2013.05.007 · 2013 · External reference
Structural basis of acquired resistance to selpercatinib and pralsetinib mediated by non-gatekeeper RET mutations
10.1016/j.annonc.2020.10.599 · 2021 · External reference
Osimertinib (AZD9291) — a science-driven, collaborative approach to rapid drug design and development
10.1093/annonc/mdw129 · 2016 · External reference
CAPItello-281 Study Group. Capivasertib plus abiraterone in PTEN-deficient metastatic hormone-sensitive prostate cancer: CAPItello-281 phase III study
10.1016/j.annonc.2025.10.004 · 2026 · External reference
Treatment of acute promyelocytic leukaemia with all-trans retinoic acid and arsenic trioxide: a paradigm of synergistic molecular targeting therapy
10.1098/rstb.2007.2026 · 2007 · External reference
Menin inhibitors in KMT2A-rearranged and NPM1-mutated acute leukemia: a scoping review of safety and efficacy
10.1016/j.critrevonc.2025.104783 · 2025 · External reference
Mutant-selective degradation by BRAF-targeting PROTACs
10.1038/s41467-021-21159-7 · 2021 · External reference
Targeted degradation of oncogenic KRAS
10.1021/acscentsci.0c00411 · 2020 · External reference
Effective degradation of EGFRL858R+T790M mutant proteins by CRBN-based PROTACs through both proteasome and autophagy/lysosome degradation systems
10.1016/j.ejmech.2021.113328 · 2021 · External reference
Preclinical evaluation of bavdegalutamide (ARV-110), a novel PROteolysis TArgeting Chimera androgen receptor degrader
10.1158/1535-7163.mct-23-0655 · 2025 · External reference
Oral estrogen receptor PROTAC vepdegestrant (ARV-471) is highly efficacious as monotherapy and in combination with CDK4/6 or PI3K/mTOR pathway inhibitors in preclinical ER+ breast cancer models
10.1158/1078-0432.ccr-23-3465 · 2024 · External reference
Discovery of elironrasib (RMC-6291), a potent and orally bioavailable, RAS(ON) G12C-selective, covalent tricomplex inhibitor for the treatment of patients with RAS G12C-addicted cancers
10.1021/acs.jmedchem.4c02313 · 2025 · External reference
Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase
10.1158/0008-5472.can-03-2868 · 2004 · External reference
Overcoming resistance to HER2 inhibitors through state-specific kinase binding
10.1038/nchembio.2171 · 2016 · External reference
HER2-selective and reversible tyrosine kinase inhibitor tucatinib potentiates the activity of T-DM1 in preclinical models of HER2-positive breast cancer
10.1158/2767-9764.crc-23-0302 · 2023 · External reference
Mechanisms of neratinib resistance in HER2-mutant metastatic breast cancer
10.20517/cdr.2022.48 · 2022 · External reference
Midostaurin treatment in FLT3-mutated acute myeloid leukemia and systemic mastocytosis
10.1080/17512433.2017.1387051 · 2017 · External reference
Characterizing and overriding the structural mechanism of the quizartinib-resistant FLT3 “gatekeeper” F691L mutation with PLX3397
10.1158/2159-8290.cd-15-0060 · 2015 · External reference
Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802)
10.1016/j.bmc.2011.12.021 · 2012 · External reference
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib
10.1021/jm401805h · 2014 · External reference
Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants
10.1182/blood-2009-11-251751 · 2010 · External reference
Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations
10.1038/s43018-023-00630-y · 2023 · External reference
NTRK1-3 point mutations in non-small cell lung cancer: molecular profiling
2025 · External reference
