Targeting mutant KRAS for anticancer therapeutics: a review of novel small molecule modulators (Q34659415)

3 August 2017

title

Targeting mutant KRAS for anticancer therapeutics: a review of novel small molecule modulators (English)

1 reference

3 August 2017

Yuanxiang Wang

1

1 reference

3 August 2017

Christine E Kaiser

series ordinal

2

1 reference

3 August 2017

Brendan Frett

series ordinal

3

1 reference

3 August 2017

Hong-Yu Li

series ordinal

4

1 reference

3 August 2017

language of work or name

English

0 references

publication date

23 April 2013

1 reference

Journal of Medicinal Chemistry

3 August 2017

published in

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3 August 2017

volume

56

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3 August 2017

issue

13

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3 August 2017

page(s)

5219-5230

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Fendiline inhibits K-Ras plasma membrane localization and blocks K-Ras signal transmission

3 August 2017

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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Regulation of the Forkhead transcription factor AFX by Ral-dependent phosphorylation of threonines 447 and 451

7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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7 July 2018

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Cell signaling by receptor tyrosine kinases

7 July 2018

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7 July 2018

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Understanding Ras: 'it ain't over 'til it's over'.

7 July 2018

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The Ras branch of small GTPases: Ras family members don't fall far from the tree

7 July 2018

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Essential role for oncogenic Ras in tumour maintenance

7 July 2018

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Cloning and characterization of a mammalian prenyl protein-specific protease

7 July 2018

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Mammalian prenylcysteine carboxyl methyltransferase is in the endoplasmic reticulum

7 July 2018

1 reference

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Membrane association and targeting of prenylated Ras-like GTPases

7 July 2018

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Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts

7 July 2018

1 reference

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Farnesyltransferase inhibitors and cancer treatment: targeting simply Ras?

7 July 2018

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K- and N-Ras are geranylgeranylated in cells treated with farnesyl protein transferase inhibitors

7 July 2018

1 reference

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Modulation of Ras and a-factor function by carboxyl-terminal proteolysis

7 July 2018

1 reference

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Novel mechanisms of RTK signal generation

7 July 2018

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Oncogenic Ras activation of Raf/mitogen-activated protein kinase-independent pathways is sufficient to cause tumorigenic transformation

7 July 2018

1 reference

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Ras-Raf complexes: analyses of complexes formed in vivo

7 July 2018

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Requirement for Ras in Raf activation is overcome by targeting Raf to the plasma membrane

7 July 2018

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Membrane-targeting potentiates guanine nucleotide exchange factor CDC25 and SOS1 activation of Ras transforming activity

7 July 2018

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Phosphatidylinositol-3-OH kinase as a direct target of Ras

7 July 2018

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Activated Ras interacts with the Ral guanine nucleotide dissociation stimulator

7 July 2018

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Regulation of signal transduction and signal diversity by receptor oligomerization

7 July 2018

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Dimerization of cell surface receptors in signal transduction

7 July 2018

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Farnesyl derivatives of rigid carboxylic acids-inhibitors of ras-dependent cell growth

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Selective inhibition of Ras-dependent cell growth by farnesylthiosalisylic acid

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Ras CAAX Peptidomimetic FTI-277 Selectively Blocks Oncogenic Ras Signaling by Inducing Cytoplasmic Accumulation of Inactive Ras-Raf Complexes

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Activation of Rac1, RhoA, and mitogen-activated protein kinases is required for Ras transformation

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Ras recruits Raf-1 to the plasma membrane for activation by tyrosine phosphorylation

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Posttranslational modification of the Ha-ras oncogene protein: evidence for a third class of protein carboxyl methyltransferases

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

p21ras is modified by a farnesyl isoprenoid

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

All ras proteins are polyisoprenylated but only some are palmitoylated

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

A polybasic domain or palmitoylation is required in addition to the CAAX motif to localize p21ras to the plasma membrane

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

The Saccharomyces cerevisiae STE14 gene encodes a methyltransferase that mediates C-terminal methylation of a-factor and RAS proteins

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

A phase II study of the Ras-MAPK signaling pathway inhibitor TLN-4601 in patients with glioblastoma at first progression.

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

A phase II study of Lonafarnib (SCH66336) in patients with chemorefractory, advanced squamous cell carcinoma of the head and neck.

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Identification of key residues in the A-Raf kinase important for phosphoinositide lipid binding specificity.

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Immobilized metal ion affinity-based fluorescence polarization (IMAP): advances in kinase screening

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Phase II study of R115777, a farnesyl transferase inhibitor, in myelodysplastic syndrome

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Antitumor effect and potentiation or reduction in cytotoxic drug activity in human colon carcinoma cells by the Raf kinase inhibitor (RKI) BAY 43-9006.

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Farnesyltransferase inhibitor R115777 in myelodysplastic syndrome: clinical and biologic activities in the phase 1 setting

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Functional analysis of a phosphatidic acid binding domain in human Raf-1 kinase: mutations in the phosphatidate binding domain lead to tail and trunk abnormalities in developing zebrafish embryos

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Efficacy of the farnesyl transferase inhibitor R115777 in chronic myeloid leukemia and other hematologic malignancies

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Clinical and biologic activity of the farnesyltransferase inhibitor R115777 in adults with refractory and relapsed acute leukemias: a phase 1 clinical-laboratory correlative trial

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

A phase II trial of tipifarnib in myelofibrosis: primary, post-polycythemia vera and post-essential thrombocythemia

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4666308

Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase inhibitor B956

9 December 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/23566315

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Phase 1 study of lonafarnib (SCH 66336) and imatinib mesylate in patients with chronic myeloid leukemia who have failed prior single-agent therapy with imatinib

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/23566315

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1021/JM3017706

1 reference

3 August 2017

1 reference

3 August 2017

1 reference