Published in Angew Chem Int Ed Engl on May 08, 2012
Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature (2013) 5.04
K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature (2013) 4.43
In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction. Proc Natl Acad Sci U S A (2013) 3.10
Drugging the undruggable RAS: Mission possible? Nat Rev Drug Discov (2014) 2.77
Discovery and characterization of small molecules that target the GTPase Ral. Nature (2014) 2.51
Requirement for interaction of PI3-kinase p110α with RAS in lung tumor maintenance. Cancer Cell (2013) 1.95
Small-molecule inhibitors of protein-protein interactions: progressing toward the reality. Chem Biol (2014) 1.95
KRAS: feeding pancreatic cancer proliferation. Trends Biochem Sci (2014) 1.85
Oncogenic KRAS signalling in pancreatic cancer. Br J Cancer (2014) 1.71
Rational design of small molecule inhibitors targeting the Ras GEF, SOS1. Chem Biol (2014) 1.45
Rho guanine nucleotide exchange factors: regulators of Rho GTPase activity in development and disease. Oncogene (2013) 1.44
Targeting protein-protein interactions as an anticancer strategy. Trends Pharmacol Sci (2013) 1.29
Dissecting fragment-based lead discovery at the von Hippel-Lindau protein:hypoxia inducible factor 1α protein-protein interface. Chem Biol (2012) 1.26
Fragment-based drug discovery using NMR spectroscopy. J Biomol NMR (2013) 1.17
A RAS renaissance: emerging targeted therapies for KRAS-mutated non-small cell lung cancer. Clin Cancer Res (2014) 1.11
KRAS as a Therapeutic Target. Clin Cancer Res (2015) 1.11
Andrographolide derivatives inhibit guanine nucleotide exchange and abrogate oncogenic Ras function. Proc Natl Acad Sci U S A (2013) 1.10
Using a fragment-based approach to target protein-protein interactions. Chembiochem (2013) 1.09
Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α. Angew Chem Int Ed Engl (2012) 1.07
Targeting mutant KRAS for anticancer therapeutics: a review of novel small molecule modulators. J Med Chem (2013) 1.04
Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange. Proc Natl Acad Sci U S A (2014) 1.04
Plucking the high hanging fruit: a systematic approach for targeting protein-protein interactions. Bioorg Med Chem (2012) 1.03
In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C. Proc Natl Acad Sci U S A (2014) 1.02
Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices. Proc Natl Acad Sci U S A (2015) 0.97
Mutant KRAS as a critical determinant of the therapeutic response of colorectal cancer. Genes Dis (2015) 0.94
Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragment-linking approach. J Med Chem (2013) 0.93
Twenty years on: the impact of fragments on drug discovery. Nat Rev Drug Discov (2016) 0.92
High-Affinity Interaction of the K-Ras4B Hypervariable Region with the Ras Active Site. Biophys J (2015) 0.92
RAS isoforms and mutations in cancer at a glance. J Cell Sci (2016) 0.91
GTP Binding and Oncogenic Mutations May Attenuate Hypervariable Region (HVR)-Catalytic Domain Interactions in Small GTPase K-Ras4B, Exposing the Effector Binding Site. J Biol Chem (2015) 0.90
NMR-based approaches for the identification and optimization of inhibitors of protein-protein interactions. Chem Rev (2014) 0.89
Allosteric modulation of Ras and the PI3K/AKT/mTOR pathway: emerging therapeutic opportunities. Front Physiol (2014) 0.88
Targeting protein-protein interactions in hematologic malignancies: still a challenge or a great opportunity for future therapies? Immunol Rev (2015) 0.88
Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design. Nat Rev Drug Discov (2016) 0.88
Lessons from computer simulations of Ras proteins in solution and in membrane. Biochim Biophys Acta (2013) 0.87
Cancer: The Ras renaissance. Nature (2015) 0.85
Structure-based inhibition of protein-protein interactions. Eur J Med Chem (2014) 0.85
Small-molecule inhibitors that target protein-protein interactions in the RAD51 family of recombinases. ChemMedChem (2014) 0.84
Discovery of a Direct Ras Inhibitor by Screening a Combinatorial Library of Cell-Permeable Bicyclic Peptides. ACS Comb Sci (2015) 0.84
Inhibition of Ras signaling by blocking Ras-effector interactions with cyclic peptides. Angew Chem Int Ed Engl (2015) 0.84
The Structural Basis of Oncogenic Mutations G12, G13 and Q61 in Small GTPase K-Ras4B. Sci Rep (2016) 0.83
Systematic Functional Interrogation of Rare Cancer Variants Identifies Oncogenic Alleles. Cancer Discov (2016) 0.83
miR-1298 Inhibits Mutant KRAS-Driven Tumor Growth by Repressing FAK and LAMB3. Cancer Res (2016) 0.83
A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein. PLoS One (2014) 0.82
Targeting RAS-mutant cancers: is ERK the key? Trends Cancer (2015) 0.82
Binding hotspots on K-ras: consensus ligand binding sites and other reactive regions from probe-based molecular dynamics analysis. Proteins (2015) 0.82
A universal isocyanide for diverse heterocycle syntheses. Org Lett (2014) 0.82
Mutant and wild-type Ras: co-conspirators in cancer. Cancer Discov (2013) 0.82
Biophysics in drug discovery: impact, challenges and opportunities. Nat Rev Drug Discov (2016) 0.81
Direct Ras Inhibitors Identified from a Structurally Rigidified Bicyclic Peptide Library. Tetrahedron (2014) 0.81
Inhibition of Acid Sphingomyelinase Depletes Cellular Phosphatidylserine and Mislocalizes K-Ras from the Plasma Membrane. Mol Cell Biol (2015) 0.81
Inhibition of Ras-Effector Interaction by Cyclic Peptides. Medchemcomm (2013) 0.81
Drug discovery: Pocket of opportunity. Nature (2013) 0.81
pMD-Membrane: A Method for Ligand Binding Site Identification in Membrane-Bound Proteins. PLoS Comput Biol (2015) 0.81
Inhibition of RAS function through targeting an allosteric regulatory site. Nat Chem Biol (2016) 0.81
Drugging Ras GTPase: a comprehensive mechanistic and signaling structural view. Chem Soc Rev (2016) 0.80
Combined rational design and a high throughput screening platform for identifying chemical inhibitors of a Ras-activating enzyme. J Biol Chem (2015) 0.80
Systematic Targeting of Protein-Protein Interactions. Trends Pharmacol Sci (2016) 0.79
Drugging the Ral GTPase. Small GTPases (2015) 0.79
Alternative modulation of protein-protein interactions by small molecules. Curr Opin Biotechnol (2015) 0.79
KRAS Engages AGO2 to Enhance Cellular Transformation. Cell Rep (2016) 0.79
Overview of simulation studies on the enzymatic activity and conformational dynamics of the GTPase Ras. Mol Simul (2014) 0.79
Multivalent Small-Molecule Pan-RAS Inhibitors. Cell (2017) 0.79
A method for the second-site screening of K-Ras in the presence of a covalently attached first-site ligand. J Biomol NMR (2014) 0.78
BcL-xL conformational changes upon fragment binding revealed by NMR. PLoS One (2013) 0.78
Activated Ras as a Therapeutic Target: Constraints on Directly Targeting Ras Isoforms and Wild-Type versus Mutated Proteins. ISRN Oncol (2013) 0.78
LIBSA--a method for the determination of ligand-binding preference to allosteric sites on receptor ensembles. J Chem Inf Model (2014) 0.78
KRAS Mutant Pancreatic Cancer: No Lone Path to an Effective Treatment. Cancers (Basel) (2016) 0.77
New Frontiers in Druggability. J Med Chem (2015) 0.77
KRAS insertion mutations are oncogenic and exhibit distinct functional properties. Nat Commun (2016) 0.77
Molecular Mechanism for Conformational Dynamics of Ras·GTP Elucidated from In-Situ Structural Transition in Crystal. Sci Rep (2016) 0.77
Reversing translational suppression and induction of toxicity in pancreatic cancer cells using a chemoprevention gene therapy approach. Mol Pharmacol (2014) 0.77
Translational synthetic chemistry. Nat Chem Biol (2013) 0.77
Automated NMR fragment based screening identified a novel interface blocker to the LARG/RhoA complex. PLoS One (2014) 0.77
Searching for the Chokehold of NRAS Mutant Melanoma. J Invest Dermatol (2016) 0.77
NMR approaches in structure-based lead discovery: recent developments and new frontiers for targeting multi-protein complexes. Prog Biophys Mol Biol (2014) 0.76
Drug developers refocus efforts on RAS. Nat Biotechnol (2016) 0.76
How to Target Activated Ras Proteins: Direct Inhibition vs. Induced Mislocalization. Mini Rev Med Chem (2016) 0.76
Targeting the KRAS Pathway in Non-Small Cell Lung Cancer. Oncologist (2016) 0.76
Distinct dynamics and interaction patterns in H- and K-Ras oncogenic P-loop mutants. Proteins (2017) 0.76
KRAS - An Evolving Cancer Target. Austin J Cancer Clin Res (2016) 0.75
Exploring the interactions of the RAS family in the human protein network and their potential implications in RAS-directed therapies. Oncotarget (2016) 0.75
One step closer to targeting RAS. Cell Cycle (2015) 0.75
Targeting the K-Ras/PDEδ protein-protein interaction: the solution for Ras-driven cancers or just another therapeutic mirage? ChemMedChem (2013) 0.75
Inhibition of prenylated KRAS in a lipid environment. PLoS One (2017) 0.75
Graded inhibition of oncogenic Ras-signaling by multivalent Ras-binding domains. Cell Commun Signal (2014) 0.75
Exonuclease containment by SUMO plus ubiquitin. Cell Cycle (2015) 0.75
Arresting kinase suppressor of Ras in an inactive state. Chin J Cancer (2017) 0.75
An investigation of small GTPases in relation to liver tumorigenesis using traditional Chinese medicine. Biomed Res Int (2014) 0.75
Total Chemical Synthesis and Folding of All-L and All-D Variants of Oncogenic KRas(G12V). J Am Chem Soc (2017) 0.75
Modeling of RAS complexes supports roles in cancer for less studied partners. BMC Biophys (2017) 0.75
RAS Proteins and Their Regulators in Human Disease. Cell (2017) 0.75
Intrinsic protein disorder in oncogenic KRAS signaling. Cell Mol Life Sci (2017) 0.75
Hallmarks of cancer: the next generation. Cell (2011) 140.01
ras oncogenes in human cancer: a review. Cancer Res (1989) 22.03
Small-molecule inhibitors of protein-protein interactions: progressing towards the dream. Nat Rev Drug Discov (2004) 7.84
Discovering high-affinity ligands for proteins: SAR by NMR. Science (1996) 7.10
Essential role for oncogenic Ras in tumour maintenance. Nature (1999) 6.51
RAS oncogenes: weaving a tumorigenic web. Nat Rev Cancer (2011) 6.45
A decade of fragment-based drug design: strategic advances and lessons learned. Nat Rev Drug Discov (2007) 4.82
The structural basis of the activation of Ras by Sos. Nature (1998) 4.50
KRAS mutations in non-small cell lung cancer. Proc Am Thorac Soc (2009) 3.61
Oncogene cooperation in tumor maintenance and tumor recurrence in mouse mammary tumors induced by Myc and mutant Kras. Proc Natl Acad Sci U S A (2008) 2.14
Molecular switch in signal transduction: reaction paths of the conformational changes in ras p21. Proc Natl Acad Sci U S A (1997) 1.95
An orthosteric inhibitor of the Ras-Sos interaction. Nat Chem Biol (2011) 1.91
Activating KRAS mutations and overexpression of epidermal growth factor receptor as independent predictors in metastatic colorectal cancer patients treated with cetuximab. Ann Surg (2010) 1.36
Fragment-based screening using X-ray crystallography and NMR spectroscopy. Curr Opin Chem Biol (2007) 1.32
Non-redundancy within the RAS oncogene family: insights into mutational disparities in cancer. Mol Cells (2009) 1.28
Common occurrence of multiple K-RAS mutations in pancreatic cancers with associated precursor lesions and in biliary cancers. Oncogene (2002) 1.22
Selenomethionine incorporation into a protein by cell-free synthesis. J Struct Funct Genomics (2002) 1.17
An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature (2005) 22.40
Specificity of short interfering RNA determined through gene expression signatures. Proc Natl Acad Sci U S A (2003) 3.74
Structural biology of the Bcl-2 family of proteins. Biochim Biophys Acta (2004) 3.47
Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737. Cancer Res (2007) 3.24
siRNA-mediated off-target gene silencing triggered by a 7 nt complementation. Nucleic Acids Res (2005) 3.21
Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α. Nat Chem Biol (2010) 2.71
Druggability indices for protein targets derived from NMR-based screening data. J Med Chem (2005) 2.67
Structural characterization of a soluble amyloid beta-peptide oligomer. Biochemistry (2009) 2.31
Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design. J Med Chem (2012) 2.23
Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clin Cancer Res (2008) 2.10
Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. J Med Chem (2007) 2.09
Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J Med Chem (2004) 2.05
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. J Med Chem (2008) 1.85
Identification of Ras-related nuclear protein, targeting protein for xenopus kinesin-like protein 2, and stearoyl-CoA desaturase 1 as promising cancer targets from an RNAi-based screen. Cancer Res (2007) 1.81
A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo. Cancer Res (2006) 1.67
Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis. J Med Chem (2006) 1.64
Solution structure of human survivin and its binding interface with Smac/Diablo. Biochemistry (2005) 1.60
Growth inhibition and radiosensitization of glioblastoma and lung cancer cells by small interfering RNA silencing of tumor necrosis factor receptor-associated factor 2. Cancer Res (2008) 1.55
Structure of the N-terminal RNA-binding domain of the SARS CoV nucleocapsid protein. Biochemistry (2004) 1.53
Solution structure of a Bcl-2 homolog from Kaposi sarcoma virus. Proc Natl Acad Sci U S A (2002) 1.52
Regulation of the Apaf-1/caspase-9 apoptosome by caspase-3 and XIAP. J Biol Chem (2002) 1.52
Evaluating hypoxia-inducible factor-1alpha as a cancer therapeutic target via inducible RNA interference in vivo. Cancer Res (2005) 1.49
ALARM NMR: a rapid and robust experimental method to detect reactive false positives in biochemical screens. J Am Chem Soc (2005) 1.48
Defining the optimal parameters for hairpin-based knockdown constructs. RNA (2007) 1.48
The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo. Cancer Chemother Pharmacol (2010) 1.47
Solution structure and mutational analysis of pituitary adenylate cyclase-activating polypeptide binding to the extracellular domain of PAC1-RS. Proc Natl Acad Sci U S A (2007) 1.45
Nuclear magnetic resonance structural studies of a potassium channel-charybdotoxin complex. Biochemistry (2005) 1.43
Similar modes of polypeptide recognition by export chaperones in flagellar biosynthesis and type III secretion. Nat Struct Biol (2003) 1.39
ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo. Mol Cancer Ther (2008) 1.34
Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo. J Med Chem (2006) 1.33
6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases. Proc Natl Acad Sci U S A (2008) 1.33
A chemical genomics screen highlights the essential role of mitochondria in HIF-1 regulation. Proc Natl Acad Sci U S A (2008) 1.33
Defining the p53 DNA-binding domain/Bcl-x(L)-binding interface using NMR. FEBS Lett (2004) 1.33
Survivin depletion preferentially reduces the survival of activated K-Ras-transformed cells. Mol Cancer Ther (2007) 1.31
Development of a tightly regulated U6 promoter for shRNA expression. FEBS Lett (2004) 1.30
A surface groove essential for viral Bcl-2 function during chronic infection in vivo. PLoS Pathog (2005) 1.30
The related effector proteins SopD and SopD2 from Salmonella enterica serovar Typhimurium contribute to virulence during systemic infection of mice. Mol Microbiol (2004) 1.27
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity. J Med Chem (2006) 1.26
Solution structure of the BHRF1 protein from Epstein-Barr virus, a homolog of human Bcl-2. J Mol Biol (2003) 1.26
Allosteric antagonism of insect odorant receptor ion channels. PLoS One (2012) 1.20
Fragment-based drug discovery using NMR spectroscopy. J Biomol NMR (2013) 1.17
Interaction with WDR5 promotes target gene recognition and tumorigenesis by MYC. Mol Cell (2015) 1.16
Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy. J Am Chem Soc (2003) 1.11
Discovery of a novel small molecule binding site of human survivin. Bioorg Med Chem Lett (2007) 1.11
Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies. Chem Biol Drug Des (2007) 1.08
The functional interface between Salmonella and its host cell: opportunities for therapeutic intervention. Trends Pharmacol Sci (2005) 1.06
Micro-computed tomography assessment of the progression of fracture healing in mice. Bone (2012) 1.06
Identification and optimization of small molecules that restore E-cadherin expression and reduce invasion in colorectal carcinoma cells. ACS Chem Biol (2011) 1.06
Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange. Proc Natl Acad Sci U S A (2014) 1.04
A high-throughput fluorescence polarization anisotropy assay for the 70N domain of replication protein A. Anal Biochem (2011) 1.03
Structure-activity relationship of a broad-spectrum insect odorant receptor agonist. ACS Chem Biol (2012) 1.02
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR. Bioorg Med Chem Lett (2010) 1.02
Discovery of aminoglycoside mimetics by NMR-based screening of Escherichia coli A-site RNA. J Am Chem Soc (2003) 1.02
Hypoxia-inducible factor-1 inhibition in combination with temozolomide treatment exhibits robust antitumor efficacy in vivo. Clin Cancer Res (2006) 1.01
Golgi enlargement in Arf-depleted yeast cells is due to altered dynamics of cisternal maturation. J Cell Sci (2013) 1.01
Non-peptide entry inhibitors of HIV-1 that target the gp41 coiled coil pocket. Bioorg Med Chem Lett (2009) 0.98
Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A. J Med Chem (2014) 0.97
Structural analysis of UBL5, a novel ubiquitin-like modifier. Protein Sci (2003) 0.97
Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A. ACS Med Chem Lett (2013) 0.95
Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Bioorg Med Chem Lett (2012) 0.95
Room-temperature Pd-catalyzed amidation of aryl bromides using tert-butyl carbamate. J Org Chem (2009) 0.94
Non-peptidic small molecule inhibitors of XIAP. Bioorg Med Chem Lett (2005) 0.93
Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragment-linking approach. J Med Chem (2013) 0.93
Fragment-based screening of the bromodomain of ATAD2. J Med Chem (2014) 0.92
SOS-NMR: a saturation transfer NMR-based method for determining the structures of protein-ligand complexes. J Am Chem Soc (2004) 0.91
A robust in vivo positive-readout system for monitoring siRNA delivery to xenograft tumors. RNA (2011) 0.89
Bcl-XL represents a druggable molecular vulnerability during aurora B inhibitor-mediated polyploidization. Proc Natl Acad Sci U S A (2010) 0.87
Solution structure and function of an essential CMP kinase of Streptococcus pneumoniae. Protein Sci (2003) 0.87
A strategy for high-throughput assay development using leads derived from nuclear magnetic resonance-based screening. J Biomol Screen (2002) 0.86
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup. Bioorg Med Chem Lett (2011) 0.86
Ligand binding to domain-3 of human serum albumin: a chemometric analysis. J Comput Aided Mol Des (2003) 0.86
NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability. J Med Chem (2002) 0.85
Surface reengineering of RPA70N enables cocrystallization with an inhibitor of the replication protein A interaction motif of ATR interacting protein. Biochemistry (2013) 0.84
Structural studies of Bcl-xL/ligand complexes using 19F NMR. J Biomol NMR (2006) 0.84