Predictive Gene Signature for Pyrazolopyrimidine Derivative c-Src Inhibitor 10a Sensitivity in Melanoma Cells

Kucukkaraduman, Baris; Turk, Can; Fallacara, Anna Lucia; Isbilen, Murat; Senses, Kerem Mert; Ayyildiz, Zeynep Ozge; Akbar, Muhammad Waqas; Lotem, Michal; Botta, Maurizio; Gure, Ali Osmay

doi:10.1021/acsmedchemlett.9b00679

Cited by 3 publications

(2 citation statements)

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“…In glioblastoma, NSUN2 is a target gene of nuclear respiratory factor 1 (NRF1), and its high expression is associated with resistance to temozolomide (TMZ) therapy [64]. In melanoma, the increased expression of NSUN5 is used to predict the sensitivity of melanoma cells to the pyrazopyrimidine derivative c-Src inhibitor 10a [159].…”

Section: Rna Methyltransferases In Cancer Therapymentioning

confidence: 99%

5-methylcytosine RNA methyltransferases and their potential roles in cancer

Tao

Zhao

et al. 2022

J Transl Med

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In recent years, 5-methylcytosine (m5C) RNA modification has emerged as a key player in regulating RNA metabolism and function through coding as well as non-coding RNAs. Accumulating evidence has shown that m5C modulates the stability, translation, transcription, nuclear export, and cleavage of RNAs to mediate cell proliferation, differentiation, apoptosis, stress responses, and other biological functions. In humans, m5C RNA modification is catalyzed by the NOL1/NOP2/sun (NSUN) family and DNA methyltransferase 2 (DNMT2). These RNA modifiers regulate the expression of multiple oncogenes such as fizzy-related-1, forkhead box protein C2, Grb associated-binding protein 2, and TEA domain transcription factor 1, facilitating the pathogenesis and progression of cancers. Furthermore, the aberrant expression of methyltransferases have been identified in various cancers and used to predict the prognosis of patients. In this review, we present a comprehensive overview of m5C RNA methyltransferases. We specifically highlight the potential mechanism of action of m5C in cancer. Finally, we discuss the prospect of m5C-relative studies.

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Section: Rna Methyltransferases In Cancer Therapymentioning

confidence: 99%

5-methylcytosine RNA methyltransferases and their potential roles in cancer

Tao

Zhao

et al. 2022

J Transl Med

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“…Baris et al reported pyrazolopyrimidine derivative 39 (Figure 6) and showed that it was a potent inhibitor (IC 50 = 0.09–9.01µM) of 15 melanoma cells. [ 62 ] The variation in inhibitory activity suggests various underlying mechanisms of action on melanoma cells. Therefore, the gene signature of chemo‐selectivity for compound 39 was identified.…”

Section: Anticancer/antiproliferative Activitymentioning

confidence: 99%

Pyrazolopyrimidines as attractive pharmacophores in efficient drug design: A recent update

Dorababu¹

2022

Archiv der Pharmazie

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Among the menacing diseases, cancer needs the most attention as millions of people are affected by it worldwide. Genetic and environmental factors play a pivotal role in causing cancer. Although a wide range of underlying mechanisms of cancer has been discovered, efficient treatments have not been discovered to date. Additionally, diseases caused by microbes such as viruses, bacteria, protozoa, and so forth, persistently result in several deaths. Also, inflammation is a major factor that leads to several health issues. For decades, drug design has become a major part of drug discovery and development for curing various diseases. Among the large number of pharmacological agents that have been synthesized, only very few have emerged as efficient drug molecules. Most of them are heterocyclic compounds, which are promising candidates for the design of efficient drug molecules. Furthermore, fused heterocycles showed comparatively stronger pharmacological activities than monocyclic heterocycles. The literature reveals that pyrazolopyrimidines have outstanding biological activity. Hence, here, the diverse pharmacological activities shown by pyrazolopyrimidine derivatives reported in the last 5 years are collated and reviewed systematically. This review is classified into various sections focusing on anticancer, antimicrobial, anti-inflammatory, and enzyme inhibitors.Structure-activity relationships are discussed in brief, which will help researchers design potent pharmacological agents.

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