Tankyrase inhibitors: emerging and promising therapeutics for cancer treatment

Verma, Anu; Kumar, Ashwani; Chugh, Arshiya; Kumar, Sunil; Kumar, Parvin

doi:10.1007/s00044-020-02657-7

Cited by 12 publications

(8 citation statements)

References 94 publications

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“…In ovarian tumor tissues, TNKS2 has been discovered to be significantly overexpressed ( 45 ), and PARP, including TNKS1 and TNKS2, are important targets for tumor therapy. Currently, a variety of PARP inhibitors have been entered into clinical studies or marketed for ovarian cancer treatment ( 46 ).…”

Section: Discussionmentioning

confidence: 99%

“…It is reported that TNKS is upregulated in ovarian tumor tissue and its upregulation is negatively correlated with patient survival ( 45 ). TNKS is a novel and a promising target for cancer treatment and several inhibitors have been investigated in clinical trials of various TNKS-associated human cancers, including ovarian cancer ( 46 ). The2X-121, a small molecular targeting the PARP, as well as the tankyrases (TNKS1 and TNKS2), showed anti-tumor activity in patients with various types of solid tumor and are generally well tolerated in Phase 1 trial (NCT01618136) ( 47 ).…”

Section: Introductionmentioning

confidence: 99%

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Icariin attenuates the tumor growth by targeting miR-1-3p/TNKS2/Wnt/β-catenin signaling axis in ovarian cancer

Liu

Long

et al. 2022

Front. Oncol.

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PurposeDespite various therapy advances, ovarian cancer remains an incurable disease for which survival rates have only modestly improved. Natural products are important sources of anti-cancer lead compounds. Icariin exhibited broad anti-cancer efficacy. However, the mechanism of icariin against ovarian cancer is poorly elucidated.MethodsCell viability was detected to evaluate the effect of icariin on SKOV-3 cells. The cell cycle and apoptosis were analyzed. The transcript of SKOV-3 cells was profiled by RNA-seq. GSEA and DEGs analyses were performed to interpret gene expression data. Western blot and TOP/FOP flash assay were applied to detect Wnt/β-catenin signaling. MiRDB database and dual-luciferase reporter assay was applied to study the regulation of miR-1-3p on TNKS2. Anti-tumor efficacy of icariin was evaluated by xenograft mouse model. Immunohistochemistry was performed with antibodies against Ki67.ResultsIcariin significantly suppressed the proliferation of SKOV-3 cells. Furthermore, icariin stalled cell cycle and induced apoptosis by blocking TNKS2/Wnt/β-catenin pathway through upregulating the level of miR-1-3p. Finally, icariin dramatically suppressed tumor growth in vivo.ConclusionsIn this study, we demonstrated for the first time that icariin significantly attenuated the growth of ovarian tumor in xenograft mouse model. Furthermore, we systematically revealed that icariin attenuates the tumor progression by suppressing TNKS2/Wnt/β-catenin signaling via upregulating the level of miR-1-3p in ovarian cancer with transcriptome analysis.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Icariin attenuates the tumor growth by targeting miR-1-3p/TNKS2/Wnt/β-catenin signaling axis in ovarian cancer

Liu

Long

et al. 2022

Front. Oncol.

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“…Tankyrase is a member of the poly(ADP-ribose)polymerase family which mediates Wnt signal transduction and has emerged as a new molecular target for the therapy of different kinds of cancer. Consequently, tankyrase inhibitors are considered as promising therapeutics for cancer treatment [ 197 ].…”

Section: New Marine-derived Cyclopeptides Reported From January 2018 ...mentioning

confidence: 99%

Absolute Stereochemistry Determination of Bioactive Marine-Derived Cyclopeptides by Liquid Chromatography Methods: An Update Review (2018–2022)

et al. 2023

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Cyclopeptides are considered as one of the most important classes of compounds derived from marine sources, due to their structural diversity and a myriad of their biological and pharmacological activities. Since marine-derived cyclopeptides consist of different amino acids, many of which are non-proteinogenic, they possess various stereogenic centers. In this respect, the structure elucidation of new molecular scaffolds obtained from natural sources, including marine-derived cyclopeptides, can become a very challenging task. The determination of the absolute configurations of the amino acid residues is accomplished, in most cases, by performing acidic hydrolysis, followed by analyses by liquid chromatography (LC). In a continuation with the authors’ previous publication, and to analyze the current trends, the present review covers recently published works (from January 2018 to November 2022) regarding new cyclopeptides from marine organisms, with a special focus on their biological/pharmacological activities and the absolute stereochemical assignment of the amino acid residues. Ninety-one unreported marine-derived cyclopeptides were identified during this period, most of which displayed anticancer or antimicrobial activities. Marfey’s method, which involves LC, was found to be the most frequently used for this purpose.

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“…The tankyrase-2 transferase protein molecule with the best interaction from Table 4 is then presented in Table 5, revealing the binding affinities of the N-cycloamino- 4, of all the binding interactions, the synthesized ligands were outstanding in their interaction with colon cancer tankyrase (PDB ID: 6KRO) with binding affinity as high as À11.1 kcal/mol for KS7, with better inhibitory properties when compared to the common colon cancer reference drugs used in this study. Tankyrase is a member of the poly (ADP-ribose) polymerase family that mediates Wingless-related integration sites (Wnts), whose factors regulate cell growth, motility, and differentiation during embryonic development [47]. Wnts act in a paracrine fashion by activating diverse signaling cascades inside target cells.…”

Section: Preparation Of Synthesized Compounds and Reference Drugs As ...mentioning

confidence: 99%

Synthesis and molecular docking studies of novel tricyclic and angular tetracyclic benzothiadiazines via sp³‐C‐Hactivation as potential colon cancer inhibitors

Kolade

Aina

Gordon

et al. 2023

Journal of Heterocyclic Chem

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This paper describes the synthesis of tricyclic and tetracyclic benzothiadiazines and their derivatives, which are known for their versatility as bioactive agents. The starting materials were N‐cycloamino‐4‐substituted‐2‐nitrobenzenesulfonamides 8–16, which were prepared through the condensation of 4‐substituted‐2‐nitrobenzenesulfonyl chlorides 1–3 and cyclic amines 4–7. The intermediates, N‐cycloamino‐4‐substituted‐2‐sulfanilamides 17–25, were obtained through catalytic hydrogenation of N‐cycloamino‐4‐substituted‐2‐nitrobenzenesulfonamides 8–16 using a 10% palladium‐on‐charcoal catalyst. The potentially bioactive tricyclic and angular tetracyclic 1,2,4‐benzothiadizine dioxides 26–34 were then synthesized via metal‐free intramolecular N‐iodosuccinimide (NIS)‐mediated radical oxidative sp3‐C‐H activation aminative cyclization of N‐cycloamino‐4‐substituted‐2‐sulfanilamides 17–25. The yields were good to excellent (68–93%). Docking studies were conducted for N‐cycloamino‐4‐substituted‐2‐nitrobenzenesulfonamides 8–16, N‐cycloamino‐4‐substituted‐2‐sulfanilamides 17–25, and tricyclic and angular tetracyclic 1,2,4‐benzothiadizine dioxides 26–34 for colon cancer using five protein molecules. The results showed that most of the prepared ligands exhibited higher activity than the reference drugs capecitabine, capecitabine, and fluorouracil. Among the compounds synthesized, KS7, a benzothiadiazine, showed the best activity against 6KRO.

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Tankyrase inhibitors: emerging and promising therapeutics for cancer treatment

Cited by 12 publications

References 94 publications

Icariin attenuates the tumor growth by targeting miR-1-3p/TNKS2/Wnt/β-catenin signaling axis in ovarian cancer

Icariin attenuates the tumor growth by targeting miR-1-3p/TNKS2/Wnt/β-catenin signaling axis in ovarian cancer

Absolute Stereochemistry Determination of Bioactive Marine-Derived Cyclopeptides by Liquid Chromatography Methods: An Update Review (2018–2022)

Synthesis and molecular docking studies of novel tricyclic and angular tetracyclic benzothiadiazines via sp³‐C‐Hactivation as potential colon cancer inhibitors

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Tankyrase inhibitors: emerging and promising therapeutics for cancer treatment

Cited by 12 publications

References 94 publications

Icariin attenuates the tumor growth by targeting miR-1-3p/TNKS2/Wnt/β-catenin signaling axis in ovarian cancer

Icariin attenuates the tumor growth by targeting miR-1-3p/TNKS2/Wnt/β-catenin signaling axis in ovarian cancer

Absolute Stereochemistry Determination of Bioactive Marine-Derived Cyclopeptides by Liquid Chromatography Methods: An Update Review (2018–2022)

Synthesis and molecular docking studies of novel tricyclic and angular tetracyclic benzothiadiazines via sp3‐C‐Hactivation as potential colon cancer inhibitors

Contact Info

Product

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Synthesis and molecular docking studies of novel tricyclic and angular tetracyclic benzothiadiazines via sp³‐C‐Hactivation as potential colon cancer inhibitors