(Q36654909)

15 August 2017

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title

New approaches to molecular cancer therapeutics (English)

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15 August 2017

2

Paul Workman

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15 August 2017

Ian Collins

1

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15 August 2017

1 December 2006

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15 August 2017

Nature Chemical Biology

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15 August 2017

2

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15 August 2017

689-700

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15 August 2017

12

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https://scigraph.springernature.com/pub.10.1038/nchembio840

15 August 2017

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Cancer biomarkers--an invitation to the table

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High throughput screening for protein kinase inhibitors

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Complex phenotypic assays in high-throughput screening

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Protein kinase inhibitors: insights into drug design from structure.

21 January 2018

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A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma

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How much gets there and what does it do?: The need for better pharmacokinetic and pharmacodynamic endpoints in contemporary drug discovery and development

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A small molecule-kinase interaction map for clinical kinase inhibitors

21 January 2018

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Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy

21 January 2018

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RNAi-based screening of the human kinome identifies Akt-cooperating kinases: a new approach to designing efficacious multitargeted kinase inhibitors.

21 January 2018

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The new era in cancer research

21 January 2018

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Drugging the cancer kinome: progress and challenges in developing personalized molecular cancer therapeutics

21 January 2018

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Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors

21 January 2018

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Cancer genes and the pathways they control

21 January 2018

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21 January 2018

The Hallmarks of Cancer

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Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer

21 January 2018

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Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug

21 January 2018

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Cancer. Addiction to oncogenes--the Achilles heal of cancer

21 January 2018

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Validating cancer drug targets

21 January 2018

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BRAF mutation predicts sensitivity to MEK inhibition

21 January 2018

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Integrative genomic analyses identify MITF as a lineage survival oncogene amplified in malignant melanoma

21 January 2018

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A census of human cancer genes

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Mutations of the BRAF gene in human cancer

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Mechanisms of cutaneous toxicities to EGFR inhibitors.

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Hexachlorophene inhibits Wnt/beta-catenin pathway by promoting Siah-mediated beta-catenin degradation.

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Finding the target after screening the phenotype

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

A genome-wide overexpression screen in yeast for small-molecule target identification

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Target discovery in small-molecule cell-based screens by in situ proteome reactivity profiling

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Identification of Akt pathway inhibitors using redistribution screening on the FLIPR and the IN Cell 3000 analyzer

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Automated high content screening for phosphoinositide 3 kinase inhibition using an AKT 1 redistribution assay.

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

A chemical genetic screen identifies inhibitors of regulated nuclear export of a Forkhead transcription factor in PTEN-deficient tumor cells

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Fragment-based lead discovery

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation.

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Is there a difference between leads and drugs? A historical perspective

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Molecular properties that influence the oral bioavailability of drug candidates

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Characteristic physical properties and structural fragments of marketed oral drugs.

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

A Common Mechanism Underlying Promiscuous Inhibitors from Virtual and High-Throughput Screening

21 January 2018

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Nonleadlikeness and leadlikeness in biochemical screening

21 January 2018

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Docking and scoring in virtual screening for drug discovery: methods and applications

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Identification of compounds with nanomolar binding affinity for checkpoint kinase-1 using knowledge-based virtual screening.

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Identification of potent Ras signaling inhibitors by pathway-selective phenotype-based screening

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Target-family-oriented focused libraries for kinases--conceptual design aspects and commercial availability

21 January 2018

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Medicinal chemistry of target family-directed masterkeys

21 January 2018

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Discovery of protein phosphatase inhibitor classes by biology-oriented synthesis

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Diversity-oriented synthesis: exploring the intersections between chemistry and biology

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Lessons from natural molecules

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Navigating chemical space for biology and medicine

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Targeting protein-protein interactions for cancer therapy

21 January 2018

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Rational design of inhibitors that bind to inactive kinase conformations

21 January 2018

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Protein kinases--the major drug targets of the twenty-first century?

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition.

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation

21 January 2018

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Structure of the FKBP12-rapamycin complex interacting with the binding domain of human FRAP

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Mutation of threonine 766 in the epidermal growth factor receptor reveals a hotspot for resistance formation against selective tyrosine kinase inhibitors

21 January 2018

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https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Novel chemical genetic approaches to the discovery of signal transduction inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Structural bioinformatics-based design of selective, irreversible kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

A small molecule designed to bind to the adenine nucleotide pocket of Hsp90 causes Her2 degradation and the growth arrest and differentiation of breast cancer cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Structural snapshots of human HDAC8 provide insights into the class I histone deacetylases

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histone and tubulin acetylation

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Components of successful lead generation

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Design and synthesis of protein superfamily-targeted chemical libraries for lead identification and optimization

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Design and discovery of small molecules targeting raf-1 kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Biochemical mechanisms of drug action: what does it take for success?

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Ligand efficiency: a useful metric for lead selection

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Features of selective kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Selective kinase inhibition by exploiting differential pathway sensitivity

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

The specificities of protein kinase inhibitors: an update

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Molecular mechanisms of drug resistance

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Improving the decision-making process in the structural modification of drug candidates: enhancing metabolic stability

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Contributions of human tumor xenografts to anticancer drug development

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Genetically engineered models have advantages over xenografts for preclinical studies

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Keynote review: in vitro safety pharmacology profiling: an essential tool for successful drug development

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

The purinome, a complex mix of drug and toxicity targets

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Gastrointestinal stromal tumours (GIST): biology and treatment

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Overriding imatinib resistance with a novel ABL kinase inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Preclinical and clinical development of the oral multikinase inhibitor sorafenib in cancer treatment

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Phase I pharmacokinetic and pharmacodynamic study of 17-allylamino, 17-demethoxygeldanamycin in patients with advanced malignancies

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Drug insight: Histone deacetylase inhibitors--development of the new targeted anticancer agent suberoylanilide hydroxamic acid

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

The Discovery of NVP-LAQ824: From Concept to Clinic

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Opportunities and challenges in the development of kinase inhibitor therapy for cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Clinical biomarkers in drug discovery and development

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Challenges of PK/PD measurements in modern drug development

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Telomerase as a Target for Cancer Immunotherapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

In vivo activation of the p53 pathway by small-molecule antagonists of MDM2

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

An inhibitor of Bcl-2 family proteins induces regression of solid tumours

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Global mapping of pharmacological space

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

The NCI60 human tumour cell line anticancer drug screen

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

The mighty mouse: genetically engineered mouse models in cancer drug development

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Systematic discovery of multicomponent therapeutics

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Systems biology and combination therapy in the quest for clinical efficacy.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

The TSC1-2 tumor suppressor controls insulin-PI3K signaling via regulation of IRS proteins

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

21 January 2018

Drugging the PI3 kinome.

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Stuart Schreiber: biology from a chemist's perspective. Interview by Joanna Owens.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Applications of high-throughput ADME in drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

Stem Cells and Cancer: Two Faces of Eve

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

A three-hybrid approach to scanning the proteome for targets of small molecule kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Genomics and the second golden era of cancer drug development

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Inhibitors of the HSP90 molecular chaperone: attacking the master regulator in cancer

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Sensitive mutation detection in heterogeneous cancer specimens by massively parallel picoliter reactor sequencing

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Exploring the sounds of silence: RNAi-mediated gene silencing for target identification and validation

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Identification of inhibitors of the kinase activity of oncogenic V600E BRAF in an enzyme cascade high-throughput screen

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Influence of molecular flexibility and polar surface area metrics on oral bioavailability in the rat

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Natural products in cancer chemotherapy: past, present and future

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Substrate and inhibitor specificity of class 1 and class 2 histone deacetylases

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Synthesis and target identification of hymenialdisine analogs

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Biopharmaceutics classification by high throughput solubility assay and PAMPA

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Combined application of parallel artificial membrane permeability assay and Caco-2 permeability assays in drug discovery

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Preclinical pharmacokinetics and metabolism of a novel diaryl pyrazole resorcinol series of heat shock protein 90 inhibitors

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Genomic profiling of cancer: what next?

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Minimally invasive pharmacokinetic and pharmacodynamic technologies in hypothesis-testing clinical trials of innovative therapies

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Phase II studies of modern drugs directed against new targets: if you are fazed, too, then resist RECIST

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Tools for kinetic modeling of biochemical networks

1 reference

https://api.crossref.org/works/10.1038%2FNCHEMBIO840

7 January 2021

Identifiers

DOI

10.1038/NCHEMBIO840

1 reference

15 August 2017

1 reference

PubMed ID

17108987