(Q26797238)

English

Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway

scientific article (publication date: 2015)

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scholarly article

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8 February 2021

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PubMed publication ID

Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway (English)

0 references

1 reference

19 September 2019

protein-serine-threonine kinases

1 reference

28 September 2019

protein kinase inhibitors

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2 October 2019

TGFβ superfamily receptor

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15 December 2019

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ChEBI release 2020-05-28

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14 September 2020

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19 December 2020

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8 February 2021

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17 September 2019

author name string

Stephan Herbertz

1

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J Scott Sawyer

2

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Anja J Stauber

3

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Ivelina Gueorguieva

4

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Kyla E Driscoll

5

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Shawn T Estrem

6

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Ann L Cleverly

7

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Durisala Desaiah

8

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Susan C Guba

9

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Karim A Benhadji

10

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Christopher A Slapak

11

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Michael M Lahn

12

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language of work or name

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publication date

10 August 2015

11 references

3 April 2019

20 June 2019

31 July 2019

17 September 2019

19 September 2019

28 September 2019

2 October 2019

15 December 2019

14 September 2020

19 December 2020

8 February 2021

Drug Design, Development and Therapy

11 references

3 April 2019

20 June 2019

31 July 2019

17 September 2019

19 September 2019

28 September 2019

2 October 2019

15 December 2019

14 September 2020

19 December 2020

8 February 2021

9

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4479-99

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copyright license

Creative Commons Attribution-NonCommercial

11 references

3 April 2019

20 June 2019

31 July 2019

17 September 2019

19 September 2019

28 September 2019

2 October 2019

15 December 2019

14 September 2020

19 December 2020

8 February 2021

on focus list of Wikimedia project

0 references

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Cardiac Safety of TGF-β Receptor I Kinase Inhibitor LY2157299 Monohydrate in Cancer Patients in a First-in-Human Dose Study

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Transforming growth factor-β as a therapeutic target in hepatocellular carcinoma

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Alterations in components of the TGF-beta superfamily signaling pathways in human cancer

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TGF-beta inhibitors for the treatment of cancer

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Development of TGF-beta signalling inhibitors for cancer therapy

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Transforming the TGFbeta pathway: convergence of distinct lead generation strategies on a novel kinase pharmacophore for TbetaRI (ALK5).

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Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 September 2017

Lifetime exposure to a soluble TGF-beta antagonist protects mice against metastasis without adverse side effects

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 September 2017

TGF-beta signaling in cancer--a double-edged sword

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 September 2017

Specificity, diversity, and regulation in TGF-beta superfamily signaling.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 September 2017

Transforming growth factor-beta in breast cancer: a working hypothesis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 September 2017

GS domain mutations that constitutively activate T beta R-I, the downstream signaling component in the TGF-beta receptor complex

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 September 2017

New class of transforming growth factors potentiated by epidermal growth factor: isolation from non-neoplastic tissues

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 September 2017

Transforming growth factors: isolation of polypeptides from virally and chemically transformed cells by acid/ethanol extraction

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 September 2017

Induction of c-sis mRNA and activity similar to platelet-derived growth factor by transforming growth factor beta: a proposed model for indirect mitogenesis involving autocrine activity

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 September 2017

Production of transforming growth factor beta by human T lymphocytes and its potential role in the regulation of T cell growth

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 September 2017

Brain perfusion and permeability in patients with advanced, refractory glioblastoma treated with lomustine and the transforming growth factor-β receptor I kinase inhibitor LY2157299 monohydrate.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

31 May 2018

Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherap

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

31 May 2018

The role of shear-induced transforming growth factor-β signaling in the endothelium

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

31 May 2018

Dependency of colorectal cancer on a TGF-β-driven program in stromal cells for metastasis initiation

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

31 May 2018

Analysis and variability of TGFbeta measurements in cancer patients with skeletal metastases.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

31 May 2018

Activated type I TGFbeta receptor kinase enhances the survival of mammary epithelial cells and accelerates tumor progression

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

31 May 2018

Reduced transforming growth factor-beta type II receptor (TGF-beta RII) expression in adenocarcinoma of the lung.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

31 May 2018

Synergistic interaction of two classes of transforming growth factors from murine sarcoma cells

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

31 May 2018

The transforming growth factor-beta system, a complex pattern of cross-reactive ligands and receptors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

31 May 2018

Anti-tumor activity of the TGF-β receptor kinase inhibitor galunisertib (LY2157299 monohydrate) in patient-derived tumor xenografts.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Combined treatment with erlotinib and a transforming growth factor-β type I receptor inhibitor effectively suppresses the enhanced motility of erlotinib-resistant non-small-cell lung cancer cells.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Plasma levels of transforming growth factor-beta 1 before and after removal of low- and high-grade astrocytomas

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Sorafenib reduces hepatic infiltrated regulatory T cells in hepatocellular carcinoma patients by suppressing TGF-beta signal.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-β and BMP-associated proinflammatory and proangiogenic signals.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Nodal/Activin signaling drives self-renewal and tumorigenicity of pancreatic cancer stem cells and provides a target for combined drug therapy.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

VEGFR2 expression and TGF-β signaling in initial and recurrent high-grade human glioma.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Induction of heart valve lesions by small-molecule ALK5 inhibitors.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Effect of gastric pH on the pharmacokinetics of a BCS class II compound in dogs: utilization of an artificial stomach and duodenum dissolution model and GastroPlus,™ simulations to predict absorption

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Application of T cell-based transcriptomics to identify three candidate biomarkers for monitoring anti-TGFβR therapy

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Companies waver in efforts to target transforming growth factor beta in cancer.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

VEGF and inhibitors of TGFbeta type-I receptor kinase synergistically promote blood-vessel formation by inducing alpha5-integrin expression.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Imaging transforming growth factor-beta signaling dynamics and therapeutic response in breast cancer bone metastasis.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

TGF-beta increases glioma-initiating cell self-renewal through the induction of LIF in human glioblastoma.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

High TGFbeta-Smad activity confers poor prognosis in glioma patients and promotes cell proliferation depending on the methylation of the PDGF-B gene

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Transforming growth factor-beta receptor inhibition enhances adenoviral infectability of carcinoma cells via up-regulation of Coxsackie and Adenovirus Receptor in conjunction with reversal of epithelial-mesenchymal transition.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Laminin-5 with transforming growth factor-beta1 induces epithelial to mesenchymal transition in hepatocellular carcinoma

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Mutational inactivation of transforming growth factor beta receptor type II in microsatellite stable colon cancers.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Transforming growth factor beta: potential autocrine growth inhibitor of estrogen receptor-negative human breast cancer cells

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4539082

28 November 2018

Comparison of cytogenetics, cytokine secretion, and oncogene expression in primary cultures of renal carcinoma cells

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Plasma levels of interleukin-6 and its soluble receptor are associated with prostate cancer progression and metastasis

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

TGF-β signalling-related markers in cancer patients with bone metastasis

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A pharmacokinetic-pharmacodynamic model for predicting tumour growth inhibition in mice: a useful tool in oncology drug development

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Preoperative plasma levels of transforming growth factor beta(1) (TGF-beta(1)) strongly predict progression in patients undergoing radical prostatectomy

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Transforming growth factor betas and their signaling receptors in human hepatocellular carcinoma

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Anti-transforming growth factor (TGF)-beta antibodies inhibit breast cancer cell tumorigenicity and increase mouse spleen natural killer cell activity. Implications for a possible role of tumor cell/host TGF-beta interactions in human breast cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Shear stress as an inhibitor of vascular smooth muscle cell proliferation. Role of transforming growth factor-beta 1 and tissue-type plasminogen activator

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Transforming growth factor beta1 and soluble Fas serum levels in hepatocellular carcinoma

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Regulatory T cells and cytokines in malignant pleural effusions secondary to mesothelioma and carcinoma

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Regulatory mechanisms for transforming growth factor beta as an autocrine inhibitor in human hepatocellular carcinoma: implications for roles of smads in its growth

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Plasma transforming growth factor beta1 as a predictor of radiation pneumonitis

1 reference

https://pubmed.ncbi.nlm.nih.gov/26309397

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.2147/DDDT.S86621

1 reference

Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

release_pmvyz6ta6valvi5h7uwqx42a24

0 references

OpenCitations bibliographic resource ID

1 reference

Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

PMC publication ID

1 reference

Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

PubMed publication ID

1 reference

Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

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