Research graph
References from PDE6D Inhibitors with a New Design Principle Selectively Block K-Ras Activity. Local targets link to admitted publications; unresolved targets remain external evidence.
Drugging RAS: Know the enemy
10.1126/science.aam7622 · 2017 · External reference
Inhibition of the Prenylation of K-Ras, but Not H- or N-Ras, Is Highly Resistant to CAAX Peptidomimetics and Requires Both a Farnesyltransferase and a Geranylgeranyltransferase I Inhibitor in Human Tumor Cell Lines
10.1038/sj.onc.1201296 · 1997 · External reference
Small-Molecule Modulation of Ras Signaling
10.1038/nchembio.1560 · 2014 · External reference
K-Ras(G12C) Inhibitors Allosterically Control GTP Affinity and Effector Interactions
10.1038/nature12796 · 2013 · External reference
Allele-Specific Inhibitors Inactivate Mutant KRAS G12C by a Trapping Mechanism
10.1126/science.aad6204 · 2016 · External reference
Discovery of Potent SOS1 Inhibitors That Block RAS Activation via Disruption of the RAS-SOS1 Interaction
10.1073/pnas.1812963116 · 2019 · External reference
Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor
10.1016/j.cell.2018.01.006 · 2018 · External reference
The Clinical KRAS(G12C) Inhibitor AMG 510 Drives Anti-Tumour Immunity
10.1038/s41586-019-1694-1 · 2019 · External reference
In Silico Discovery of Small-Molecule Ras Inhibitors That Display Antitumor Activity by Blocking the Ras-Effector Interaction
10.1073/pnas.1217730110 · 2013 · External reference
Discovery of High-Affinity Noncovalent Allosteric KRAS Inhibitors That Disrupt Effector Binding
10.1021/acsomega.8b03308 · 2019 · External reference
The GDI-like solubilizing factor PDEδ sustains the spatial organization and signalling of Ras family proteins
10.1038/ncb2394 · 2011 · External reference
Structural basis of recognition of farnesylated and methylated KRAS4b by PDEδ
10.1073/pnas.1615316113 · 2016 · External reference
KRas Localizes to the Plasma Membrane by Spatial Cycles of Solubilization, Trapping and Vesicular Transport
10.1016/j.cell.2014.02.051 · 2014 · External reference
Arl2-GTP and Arl3-GTP Regulate a GDI-Like Transport System for Farnesylated Cargo
10.1038/nchembio.686 · 2011 · External reference
Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling
10.1038/nature12205 · 2013 · External reference
Identification of Pyrazolopyridazinones as PDEδ Inhibitors
10.1038/ncomms11360 · 2016 · External reference
A PDE6δ-KRas Inhibitor Chemotype with up to Seven H-Bonds and Picomolar Affinity that Prevents Efficient Inhibitor Release by Arl2
10.1002/anie.201610957 · 2017 · External reference
Fragment-based drug discovery of triazole inhibitors to block PDEδ-RAS protein-protein interaction
10.1016/j.ejmech.2018.12.018 · 2019 · External reference
Prodrugs of Phosphates and Phosphonates
10.1021/jm701260b · 2008 · External reference
2,2-Disubstituted 4-Acylthio-3-Oxobutyl Groups as Esterase- and Thermolabile Protecting Groups of Phosphodiesters
10.1021/jo302421u · 2013 · External reference
Computational and Biochemical Characterization of Two Partially Overlapping Interfaces and Multiple Weak-Affinity K-Ras Dimers
10.1038/srep40109 · 2017 · External reference
Opposite Feedback From mTORC1 to H-Ras and K-ras4B Downstream of SREBP1
10.1038/s41598-017-09387-8 · 2017 · External reference
Rapalogs Can Promote Cancer Cell Stemness in Vitro in a Galectin-1 and H-Ras-Dependent Manner
10.18632/oncotarget.17819 · 2017 · External reference
Antitumor Efficacy of a Novel Class of Non-Thiol-Containing Peptidomimetic Inhibitors of Farnesyltransferase and Geranylgeranyltransferase I
1999 · External reference
Cancer Stem Cell Drugs Target K-Ras Signaling in a Stemness Context
10.1038/onc.2016.59 · 2016 · External reference
Characterizing Cancer Cells with Cancer Stem Cell-Like Features in 293T Human Embryonic Kidney Cells
10.1186/1476-4598-9-180 · 2010 · External reference
Small-Molecule Inhibition of the UNC119-Cargo Interaction
10.1002/ange.201701905 · 2017 · External reference
ARL13B, PDE6D, and CEP164 Form a Functional Network for INPP5E Ciliary Targeting
10.1073/pnas.1210916109 · 2012 · External reference
A HomozygousPDE6DMutation in Joubert Syndrome Impairs Targeting of Farnesylated INPP5E Protein to the Primary Cilium
10.1002/humu.22470 · 2013 · External reference
PDE6δ-Mediated Sorting of INPP5E Into the Cilium Is Determined by Cargo-Carrier Affinity
10.1038/ncomms11366 · 2016 · External reference
EMT Programs Promote Basal Mammary Stem Cell and Tumor-Initiating Cell Stemness by Inducing Primary Ciliogenesis and Hedgehog Signaling
10.1073/pnas.1711534114 · 2017 · External reference
A Small-Molecule Inhibitor of Isoprenylcysteine Carboxyl Methyltransferase with Antitumor Activity in Cancer Cells
10.1073/pnas.0408107102 · 2005 · External reference
Integrative Clinical Genomics of Metastatic Cancer
10.1038/nature23306 · 2017 · External reference
Lessons From the Cancer Genome
10.1016/j.cell.2013.03.002 · 2013 · External reference
Maximizing the Therapeutic Potential of HSP90 Inhibitors
10.1158/1541-7786.mcr-15-0234 · 2015 · External reference
Quantitative Analysis of Hsp90-Client Interactions Reveals Principles of Substrate Recognition
10.1016/j.cell.2012.06.047 · 2012 · External reference
Automated High-Throughput Fluorescence Lifetime Imaging Microscopy to Detect Protein-Protein Interactions
10.1177/2211068215606048 · 2016 · External reference
The Efficacy of Raf Kinase Recruitment to the GTPase H-Ras Depends on H-Ras Membrane Conformer-Specific Nanoclustering
10.1074/jbc.m113.537001 · 2014 · External reference
Quantitative Scoring of Differential Drug Sensitivity for Individually Optimized Anticancer Therapies
10.1038/srep05193 · 2014 · External reference
K-Ras4A splice variant is widely expressed in cancer and uses a hybrid membrane-targeting motif
10.1073/pnas.1412811112 · 2015 · External reference
Development and validation of a genetic algorithm for flexible docking 1 1Edited by F. E. Cohen
10.1006/jmbi.1996.0897 · 1997 · External reference
KRAS Prenylation Is Required for Bivalent Binding with CaM in a Nucleotide Independent Manner
10.1016/j.bpj.2019.02.004 · 2019 · External reference
Galectin-1 Dimers Can Scaffold Raf-Effectors to Increase H-Ras Nanoclustering
10.1038/srep24165 · 2016 · External reference
Farnesylated and Methylated KRAS4b: High Yield Production of Protein Suitable for Biophysical Studies of Prenylated Protein-Lipid Interactions
10.1038/srep15916 · 2015 · External reference
