Steroid-linked nitrogen mustards as potential anticancer therapeutics: A review

Saha, Pijus; Debnath, Chhanda; Bérubé, Gervais

doi:10.1016/j.jsbmb.2013.05.004

Cited by 49 publications

(22 citation statements)

References 116 publications

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“…The first report about the therapeutic application of a conjugate of an estrogen plus the anticancer agent estramustine (Estracyt) was published in 1972 [64]. Since then numerous further conjugates or complexes have been designed [6,65]. Site-specific delivery of the anticancer agents is one of the leading reasons for the synthesis of these molecules.…”

Section: Conjugates Of Estradiol-related Compounds and Anticancer Agentsmentioning

confidence: 99%

Steroidal Anticancer Agents: An Overview of Estradiol-related Compounds

Minorics

Zupkó

2018

ACAMC

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Research of steroidal compounds as anticancer agents started almost 50 years ago. During the past decades, several innovative new steroids, like cyproterone, finasteride, estramustin, exemestane and fulvestrant have successfully become a part of routine clinical practice. Meanwhile, a vast amount of new information have accumulated about the functions of the endogenous steroid system (including the characterization of enzymes, receptors, transcription pathways, etc.) and about the role of steroids in carcinogenesis. Therefore, it is regularly required to review the latest published results, focusing on a well-defined part within this research field that has definitely developed into a highly diversified speciality by now. Herein, we make an attempt to summarize the most recent results reported about anticancer agents of estrane backbone, focusing on their mechanisms of action and their structure-activity relationships. Due to the vast number and various accessibilities of scientific publications, neither other reviews nor this one can be considered as absolutely exhaustive. In spite of these restrictive factors, the current review makes a good opportunity to define the recent scientific trends in the field of estradiol-related anticancer agents.

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Section: Conjugates Of Estradiol-related Compounds and Anticancer Agentsmentioning

confidence: 99%

Steroidal Anticancer Agents: An Overview of Estradiol-related Compounds

Minorics

Zupkó

2018

ACAMC

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“… Carmustine [ 25 ], a potential anticancer agent, activated the MAPK (MEK/ERK, and JNK) pathway via ER→SHC→RAS, and inhibited PI3K/AKT, HSP90/HIF, and AMPK pathways in MCF7 (see Additional file 2 : Figure S1). An’s work proved that carmustine induced phosphorylation of the MAPKs, such as ERK, JNK, and p38, etc.…”

Section: Resultsmentioning

confidence: 99%

A linear programming computational framework integrates phosphor-proteomics and prior knowledge to predict drug efficacy

Wang

Yan

et al. 2017

BMC Syst Biol

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BackgroundIn recent years, the integration of ‘omics’ technologies, high performance computation, and mathematical modeling of biological processes marks that the systems biology has started to fundamentally impact the way of approaching drug discovery. The LINCS public data warehouse provides detailed information about cell responses with various genetic and environmental stressors. It can be greatly helpful in developing new drugs and therapeutics, as well as improving the situations of lacking effective drugs, drug resistance and relapse in cancer therapies, etc.ResultsIn this study, we developed a Ternary status based Integer Linear Programming (TILP) method to infer cell-specific signaling pathway network and predict compounds’ treatment efficacy. The novelty of our study is that phosphor-proteomic data and prior knowledge are combined for modeling and optimizing the signaling network. To test the power of our approach, a generic pathway network was constructed for a human breast cancer cell line MCF7; and the TILP model was used to infer MCF7-specific pathways with a set of phosphor-proteomic data collected from ten representative small molecule chemical compounds (most of them were studied in breast cancer treatment). Cross-validation indicated that the MCF7-specific pathway network inferred by TILP were reliable predicting a compound’s efficacy. Finally, we applied TILP to re-optimize the inferred cell-specific pathways and predict the outcomes of five small compounds (carmustine, doxorubicin, GW-8510, daunorubicin, and verapamil), which were rarely used in clinic for breast cancer. In the simulation, the proposed approach facilitates us to identify a compound’s treatment efficacy qualitatively and quantitatively, and the cross validation analysis indicated good accuracy in predicting effects of five compounds.ConclusionsIn summary, the TILP model is useful for discovering new drugs for clinic use, and also elucidating the potential mechanisms of a compound to targets.Electronic supplementary materialThe online version of this article (10.1186/s12918-017-0501-6) contains supplementary material, which is available to authorized users.

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“…A total of 98 small molecule drugs that have common subpathways with OS metastasis were identified, including a number of anti-cancer drugs. For example, semustine, a chloroethyl nitrosourea, is known to be therapeutically effective against murine models of several tumor types (18)(19)(20). In addition, a number of the drugs identified have been proven to possess potential anti-OS effects.…”

Section: Discussionmentioning

confidence: 99%

Identification of candidate drugs for the treatment of metastatic osteosarcoma through a subpathway analysis method

Yan

2017

Oncology Letters

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Abstract. Osteosarcoma (OS) is the third most frequent type of cancer in adolescents and represents >56% of all bone tumors. In addition, metastatic OS frequently demonstrates resistance to conventional chemotherapy; thus, the development of novel therapeutic agents for the treatment of patients with metastatic OS is warranted. In the present study, the metabolic mechanisms underlying OS metastasis were investigated using a subpathway analysis method and lead to the identification of candidate drugs for the treatment of metastatic OS. Using the GSE14827 microarray dataset from the Gene Expression Omnibus database, 546 differentially expressed genes were identified between samples from patients with OS who did or did not develop metastatic OS. Furthermore, nine significantly enriched metabolic subpathways were identified, which may be involved in OS metastasis. Finally, using an integrated analysis of metastatic OS-associated subpathways and drug-affected subpathways, 98 small molecule drug candidates capable of targeting the metastatic OS-associated subpathways were identified. This method identified existing anti-cancer drugs, including semustine, in addition to predicting potential drugs, such as lansoprazole, for the treatment of metastatic OS. Transwell and wound healing assays demonstrated that lansoprazole reduced the invasiveness and migration of U2OS cells. These small molecule drug candidates identified through a bioinformatics approach may provide insights into novel therapy options for the treatment of patients with metastatic OS.

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Steroid-linked nitrogen mustards as potential anticancer therapeutics: A review

Cited by 49 publications

References 116 publications

Steroidal Anticancer Agents: An Overview of Estradiol-related Compounds

Steroidal Anticancer Agents: An Overview of Estradiol-related Compounds

A linear programming computational framework integrates phosphor-proteomics and prior knowledge to predict drug efficacy

Identification of candidate drugs for the treatment of metastatic osteosarcoma through a subpathway analysis method

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