Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents (Q34609385)

3 August 2017

title

Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents (English)

1 reference

3 August 2017

11

Michael H Gelb

1 reference

3 August 2017

Steven Fletcher

1

1 reference

3 August 2017

Erin Pusateri Keaney

2

1 reference

3 August 2017

Christopher G Cummings

3

1 reference

3 August 2017

Michelle A Blaskovich

4

1 reference

3 August 2017

Michael A Hast

5

1 reference

3 August 2017

Matthew P Glenn

6

1 reference

3 August 2017

Sung-Youn Chang

7

1 reference

3 August 2017

Cynthia J Bucher

8

1 reference

3 August 2017

Ryan J Floyd

9

1 reference

3 August 2017

William P Katt

10

1 reference

3 August 2017

Wesley C Van Voorhis

12

1 reference

3 August 2017

Lorena S Beese

13

1 reference

3 August 2017

Said M Sebti

14

1 reference

3 August 2017

Andrew D Hamilton

15

1 reference

3 August 2017

language of work or name

English

0 references

publication date

1 October 2010

1 reference

Journal of Medicinal Chemistry

3 August 2017

published in

1 reference

3 August 2017

volume

53

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3 August 2017

issue

19

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3 August 2017

page(s)

6867-6888

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Discovery of a new class of protein farnesyltransferase inhibitors in the arylthiophene series

3 August 2017

cites work

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7 July 2018

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Structural Basis for Binding and Selectivity of Antimalarial and Anticancer Ethylenediamine Inhibitors to Protein Farnesyltransferase

7 July 2018

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7 July 2018

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Potent, Plasmodium-selective farnesyltransferase inhibitors that arrest the growth of malaria parasites: structure-activity relationships of ethylenediamine-analogue scaffolds and homology model validation.

7 July 2018

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Farnesyltransferase inhibitors: a detailed chemical view on an elusive biological problem

7 July 2018

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Geranylgeranyltransferase I inhibitors target RalB to inhibit anchorage-dependent growth and induce apoptosis and RalA to inhibit anchorage-independent growth

7 July 2018

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Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites

7 July 2018

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Structure-based design of imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase.

7 July 2018

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Lipid posttranslational modifications. Farnesyl transferase inhibitors

7 July 2018

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Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.

7 July 2018

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Phase III double-blind placebo-controlled study of farnesyl transferase inhibitor R115777 in patients with refractory advanced colorectal cancer

7 July 2018

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Farnesyltransferase inhibitors as anticancer agents: critical crossroads.

7 July 2018

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Crystal structures of the anticancer clinical candidates R115777 (Tipifarnib) and BMS-214662 complexed with protein farnesyltransferase suggest a mechanism of FTI selectivity

7 July 2018

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Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?

7 July 2018

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Farnesyl protein transferase inhibitor ZARNESTRA R115777 - history of a discovery

7 July 2018

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Farnesyltransferase inhibitors: mechanism and applications

7 July 2018

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Design and synthesis of potent nonpeptidic farnesyltransferase inhibitors based on a terphenyl scaffold.

7 July 2018

1 reference

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The crystal structure of human protein farnesyltransferase reveals the basis for inhibition by CaaX tetrapeptides and their mimetics

7 July 2018

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Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity

7 July 2018

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RhoB alteration is necessary for apoptotic and antineoplastic responses to farnesyltransferase inhibitors

7 July 2018

1 reference

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

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3045627

Probing the hydrophobic pocket of farnesyltransferase: aromatic substitution of CAAX peptidomimetics leads to highly potent inhibitors

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3045627

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

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3045627

Development and validation of a genetic algorithm for flexible docking

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3045627

Protein geranylgeranylation, not farnesylation, is required for the G1 to S phase transition in mouse fibroblasts.

7 July 2018

1 reference

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Protein prenylation: molecular mechanisms and functional consequences

7 July 2018

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Harvey murine sarcoma virus p21 ras protein: biological and biochemical significance of the cysteine nearest the carboxy terminus

7 July 2018

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p21ras is modified by a farnesyl isoprenoid

7 July 2018

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ras oncogenes in human cancer: a review

7 July 2018

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Isoprenoid modification and plasma membrane association: critical factors for ras oncogenicity

7 July 2018

1 reference

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Biochemistry of protein prenylation

7 July 2018

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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3045627

A phase II study of farnesyl transferase inhibitor R115777 in pancreatic cancer: a Southwest oncology group (SWOG 9924) study

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3045627

Structurally simple farnesyltransferase inhibitors arrest the growth of malaria parasites

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3045627

Resistance to a protein farnesyltransferase inhibitor in Plasmodium falciparum

26 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3045627

Targeted inhibition of farnesyltransferase in locally advanced breast cancer: a phase I and II trial of tipifarnib plus dose-dense doxorubicin and cyclophosphamide

26 October 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/20822181

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Both farnesylated and geranylgeranylated RhoB inhibit malignant transformation and suppress human tumor growth in nude mice

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/20822181

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Design and structural requirements of potent peptidomimetic inhibitors of p21ras farnesyltransferase

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/20822181

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1021/JM1001748

1 reference

3 August 2017

1 reference

3 August 2017

1 reference