3-O-methylthespesilactam, a new small-molecule anticancer pan-JAK inhibitor against A2058 human melanoma cells

Li, Minyi; Tian, Yan; Shen, Li; Buettner, Ralf; Li, Hongzhi; Liu, Lucy; Yuan, Yate-Ching; Xiao, Qiang; Wu, Jun; Jove, Richard

doi:10.1016/j.bcp.2013.08.065

Cited by 10 publications

(7 citation statements)

References 60 publications

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“…The inhibition of the JAK1/JAK2 activity and its association with apoptosis induction in JAK2 V617F cells, have been reported in previous studies [26,28]. In addition, a link between TYK2 and aberrant STAT3 signals has been reported by others, and the degradation of TYK2 has been proposed to be a promising therapeutic approach for reducing aberrant STAT3 signaling and tumor progression [29,30].…”

Section: Discussionmentioning

confidence: 62%

Resveratrol selectively induces apoptosis in malignant cells with the JAK2V617F mutation by inhibiting the JAK2 pathway

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Espinoza

et al. 2015

Molecular Nutrition Food Res

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Section: Discussionmentioning

confidence: 62%

Resveratrol selectively induces apoptosis in malignant cells with the JAK2V617F mutation by inhibiting the JAK2 pathway

Trung

Espinoza

et al. 2015

Molecular Nutrition Food Res

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“…A natural product isolated from the heartwood of the Portia tree was found to be an inhibitor of JAK1 and TYK2, with selectivity over JAK2 and JAK3 [103]. 3-O-methylthespesilactam (48), a sesquiterpenoid alkaloid, was structurally confirmed by X-ray crystallography and nuclear magnetic resonance spectroscopy.…”

Section: Key Termmentioning

confidence: 87%

Selective JAK Inhibitors

et al. 2014

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Consisting of four members, JAK1, JAK2, JAK3 and TYK2, the JAK kinases have emerged as important targets for proliferative and immune-inflammatory disorders. Recent progress in the discovery of selective inhibitors has been significant, with selective compounds now reported for each isoform. This article summarizes the current state-of-the-art with a discussion of the most recently described selective compounds. X-ray co-crystal structures reveal the molecular reasons for the observed biochemical selectivity. A concluding analysis of JAK inhibitors in the clinic highlights increased clinical trial activity and diversity of indications. Selective JAK inhibitors, as single agents or in combination regimens, have a very promising future in the treatment of oncology, immune and inflammatory diseases.

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“…[21][22][23] Furthermore, the statement of association of increased ROS with melanocytic disorders 24 suggested our hypothesis that JAK/ ROS/Ras may be an effective pathway in lentiginosis development rather than coincidentality of JAK2 attendance and lentigo formation. For the reason that, when we consider the possible association of the Polycythemia Vera and Lentigine in Phenolyzer (http://phenolyzer.usc.edu/), the most striking gene found to be associated with was JAK2 (Fig.…”

Section: Discussionmentioning

confidence: 99%

Lentiginoses in polycythemia vera patient: Is there a role forJAK2 (V617F)mutation?

et al. 2015

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ABSTRACT. Lentiginoses is a clinical feature in which lentigines are remarkably present in large numbers or when they occur in a distinctive distribution on apparently normal skin. This entity may be congenital or acquired and may cover a wide spectrum of diseases ranging from an isolated benign pigmentary disorder to numerous syndromes associated with molecular abnormalities.We present a 59-year-old female patient with multiple lentigines which first emerged 3 y ago concurrently with policytemia vera. The patient had found to be positive for Janus Kinase-2 (JAK-2) mutation. Over activation of the pathway due to JAK-2 V617F mutation is a well-known condition in myeloproliferative diseases but has not been reported in melanocytic disorders. Moreover, several signaling pathways have previously been defined with lentiginosis except JAK-STAT pathway. We want to draw attention to the potential effect of JAK-2 mutation in lentigogenesis with this case report.

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3-O-methylthespesilactam, a new small-molecule anticancer pan-JAK inhibitor against A2058 human melanoma cells

Cited by 10 publications

References 60 publications

Resveratrol selectively induces apoptosis in malignant cells with the JAK2V617F mutation by inhibiting the JAK2 pathway

Resveratrol selectively induces apoptosis in malignant cells with the JAK2V617F mutation by inhibiting the JAK2 pathway

Selective JAK Inhibitors

Lentiginoses in polycythemia vera patient: Is there a role forJAK2 (V617F)mutation?

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