Progress in the development of small molecule inhibitors of insulin-like growth factor-1 receptor kinase

Sarma, P. V.; Tandon, Ruchi; Gupta, Praful; Dastidar, Sunanda G.; Ray, Abhijit; Das, Biswajit; Cliffe, Ian A.

doi:10.1517/13543776.17.1.25

Cited by 10 publications

(5 citation statements)

References 33 publications

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“…There have been already some reports to summarize the development of small molecule inhibitors up to 2009 [6,[12][13], in this paper we hope to make some different attempts. The small molecule inhibitors herein would be categorized into natural products and chemical compounds firstly.…”

Section: Small Molecule Inhibitors Against Igf-1rmentioning

confidence: 98%

Insulin-like Growth Factor-1 Receptor (IGF-1R) Kinase Inhibitors in Cancer Therapy: Advances and Perspectives

Xue¹,

Cao²,

Zhong³

et al. 2012

CPD

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The insulin-like growth factors (IGF) and their receptors play pivotal roles in cellular signaling transduction and thus regulate cell growth, differentiation, apoptosis, transformation and other important physiological progresses. The insulin-like growth factor 1 receptor (IGF-1R) mainly engages in the Ras/mitogen-activated protein kinase (MAPK) pathway and the phosphoinositide 3-kinase/protein kinase B (PI3K/AKT) pathway, and also forms cross-talk with the epidermal growth factor receptor (EGFR) pathway. Currently, it draws more attention since its overexpression has been demonstrated in various human cancers, such as colorectal cancer, breast cancer, prostate cancer and lung tumors, thus the strategy targeting the IGF-1R would be promising in treatment of these cancers. There are already dozens of agents developed for the inhibition of IGF-1R, which are categorized into monoclonal antibodies, small molecule inhibitors and so on. While in this review, small molecule inhibitors would be the focus for detailed discussion. Herein, we updated previously reported research papers and reviews in this field and summarized developments of small molecule inhibitors up to 2011. Finally, we proposed the application of network pharmacology methods to reconsider the clinical use of inhibitors with concomitant IR inhibition or other kinases inhibition, hoping that more optimal combinations would be obtained for cancer therapy.

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Section: Small Molecule Inhibitors Against Igf-1rmentioning

confidence: 98%

Insulin-like Growth Factor-1 Receptor (IGF-1R) Kinase Inhibitors in Cancer Therapy: Advances and Perspectives

Xue¹,

Cao²,

Zhong³

et al. 2012

CPD

View full text Add to dashboard Cite

show abstract

“…Further, Sarma and colleagues have summarized the patent literature from 2000 to early 2006 regarding the development of small-molecule inhibitors of the IGF1R 225. In addition, ongoing clinical trials for IGF1R-targeted therapeutics in cancer were recently discussed by Ryan and colleagues 36.…”

Section: Inhibition Of the Igf1r By Small Moleculesmentioning

confidence: 99%

“…35,[220][221][222][223][224] Further, Sarma and colleagues have summarized the patent literature from 2000 to early 2006 regarding the development of small-molecule inhibitors of the IGF1R. 225 In addition, ongoing clinical trials for IGF1Rtargeted therapeutics in cancer were recently discussed by Ryan and colleagues. 36 In the following text, we attempt to provide a comprehensive review and update of both the biomedical and patent literature concerning the current state of IGF1R small-molecule inhibitor development.…”

Section: Inhibition Of the Igf1r By Small Moleculesmentioning

confidence: 99%

“…In addition to the background provided above, the complexity of the IGF signaling system and the challenges this complexity poses to the discovery and development of selective IGF1R inhibitors have been reviewed recently by others as well. ,− Further, Sarma and colleagues have summarized the patent literature from 2000 to early 2006 regarding the development of small-molecule inhibitors of the IGF1R . In addition, ongoing clinical trials for IGF1R-targeted therapeutics in cancer were recently discussed by Ryan and colleagues .…”

Section: Inhibition Of the Igf1r By Small Moleculesmentioning

confidence: 99%

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Inhibition of the Insulin-like Growth Factor-1 Receptor (IGF1R) Tyrosine Kinase as a Novel Cancer Therapy Approach

2009

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“…Finally, the methoxy group was directed towards the hinge region in similar fashion to the methyl of cpd 4 and the 4-isopropyl-piperazinyl group was solvent exposed (PDB:3EKN) [35]. Later on, various IGF-1 R inhibitors have been developed based on the fact that the link to cancer was through targeting the kinase activity by binding within the adenosine triphosphate (ATP) binding site [36,37]. Of these, Linsitinib is the most advanced compound currently in phase II studies in a wide range of cancers, in combination with other treatments [38,39].…”

Section: Igf-1rmentioning

confidence: 99%

Pyrrolopyrimidine, A Multifaceted Scaffold in Cancer Targeted Therapy

et al. 2018

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Pyrrolopyrimidine derivatives represent a class of biologically active heterocyclic compounds which can serve as promising scaffolds that display remarkable biological activities, such as anti-inflammatory, antimicrobial, antiviral and anticancer. In the last few years, several pyrrolopyrimidine derivatives have been approved by the US FDA and in other countries for the treatment of different diseases or are currently in phase I/II clinical trials. Due to their inimitable antioxidant and anti-tumor properties, researchers were inspired to develop novel derivatives for the treatment of different types of cancer. The present review summarizes recent literature up to 2017 on the most recent development in the medicinal chemistry of pyrrolopyrimidine derivatives and their potential as anticancer therapeutics, especially compounds acting as kinase inhibitors.

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Progress in the development of small molecule inhibitors of insulin-like growth factor-1 receptor kinase

Cited by 10 publications

References 33 publications

Insulin-like Growth Factor-1 Receptor (IGF-1R) Kinase Inhibitors in Cancer Therapy: Advances and Perspectives

Insulin-like Growth Factor-1 Receptor (IGF-1R) Kinase Inhibitors in Cancer Therapy: Advances and Perspectives

Inhibition of the Insulin-like Growth Factor-1 Receptor (IGF1R) Tyrosine Kinase as a Novel Cancer Therapy Approach

Pyrrolopyrimidine, A Multifaceted Scaffold in Cancer Targeted Therapy

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