Shp1 in Solid Cancers and Their Therapy

Varone, Alessia; Spano, Daniela; Corda, Daniela

doi:10.3389/fonc.2020.00935

Cited by 38 publications

(32 citation statements)

References 104 publications

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“…We explored the versatility of our B2H system by assessing its ability to detect the inactivation of several other diseases-relevant PTPs. In short, we swapped out the gene for PTP1B with genes for PTPN2, PTPN6, or PTPN12; these enzymes are targets for immunotherapeutic enhancement 48 , the treatment of ovarian cancer 49 , and acute myocardial infarction 50 , respectively. Their catalytic domains share 31-65% sequence identity with the catalytic domain of PTP1B.…”

Section: Design Of Alternative Ptp-speci C Objectivesmentioning

confidence: 99%

Microbially Guided Discovery and Biosynthesis of Biologically Active Natural Products

et al. 2021

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The design of small molecules that inhibit disease-relevant proteins represents a longstanding challenge of medicinal chemistry. Here, we describe an approach for encoding this challenge-the inhibition of a human drug target-into a microbial host and using it to guide the discovery and biosynthesis of targeted, biologically active natural products. This approach identi ed two previously unknown terpenoid inhibitors of protein tyrosine phosphatase 1B (PTP1B), an elusive therapeutic target for the treatment of diabetes and cancer. Both inhibitors target an allosteric site, which confers unusual selectivity, and can inhibit PTP1B in living cells. A screen of 24 uncharacterized terpene synthases from a pool of 4,464 genes uncovered additional hits, demonstrating a scalable discovery approach, and the incorporation of different PTPs into the microbial host yielded alternative PTP-speci c detection systems. Findings illustrate the potential for using microbes to discover and build natural products that exhibit precisely de ned biochemical activities yet possess unanticipated structures and/or binding sites.

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Section: Design Of Alternative Ptp-speci C Objectivesmentioning

confidence: 99%

Microbially Guided Discovery and Biosynthesis of Biologically Active Natural Products

et al. 2021

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“…We explored the versatility of our B2H system by assessing its ability to detect the inactivation of several other disease-relevant PTPs. In short, we swapped out the gene for PTP1B with genes for PTPN2, PTPN6, or PTPN12; these enzymes are targets for immunotherapeutic enhancement 59 , the treatment of ovarian cancer 60 , and acute myocardial infarction 61 , respectively.…”

Section: Design Of Alternative Ptp-speci C Objectivesmentioning

confidence: 99%

Microbially guided discovery and biosynthesis of biologically active natural products

Sarkar

Kim

Jang

et al. 2021

Preprint

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The design of small molecules that inhibit disease-relevant proteins represents a longstanding challenge of medicinal chemistry. Here, we describe an approach for encoding this challenge—the inhibition of a human drug target—into a microbial host and using it to guide the discovery and biosynthesis of targeted, biologically active natural products. This approach identified two previously unknown terpenoid inhibitors of protein tyrosine phosphatase 1B (PTP1B), an elusive therapeutic target for the treatment of diabetes and cancer. Both inhibitors appear to target an allosteric site, which confers selectivity, and can inhibit PTP1B in living cells. A screen of 24 uncharacterized terpene synthases from a pool of 4,464 genes uncovered additional hits, demonstrating a scalable discovery approach, and the incorporation of different PTPs into the microbial host yielded alternative PTP-specific detection systems. Findings illustrate the potential for using microbes to discover and build natural products that exhibit precisely defined biochemical activities yet possess unanticipated structures and/or binding sites.

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“…SHP-1 is one of tyrosine phosphate protein, which is considered as a unique tumor suppressor gene that involved in different hallmarks of glioblastoma and other types of cancer. The key mechanism by which SHP-1 limits cancer progression and development is the capability to weaken signaling pathways, which control cell proliferation, migration, survival and invasion [35]. SHP-1 activities can be inhibited by small interfering RNA (siRNA) [36].…”

Section: Brain Cancermentioning

confidence: 99%

Verbascoside—A Review of Its Antitumor Activities

Khalaf¹,

Jasim²,

Ibrahim³

2021

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Cancer is a set of diseases including abnormal growth of cells that can spread to another tissue. Verbascoside (or acteoside) is a naturally occurring, water-soluble secondary metabolite with significant biological properties, which is distributed widely in plant kingdom. Verbascoside is pharmacologically active compounds with many recent evidences that support its biological activities and safety. This review focuses on the recent studies that concerned with the antitumor activities of verbascoside alone and as a synergistic agent as well as nanoproduct. It also shows the latest advances in its antitumor effects, cytotoxic selectivity and its efficiencies in treating cancer, in vitro and/or vivo.

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Shp1 in Solid Cancers and Their Therapy

Cited by 38 publications

References 104 publications

Microbially Guided Discovery and Biosynthesis of Biologically Active Natural Products

Microbially Guided Discovery and Biosynthesis of Biologically Active Natural Products

Microbially guided discovery and biosynthesis of biologically active natural products

Verbascoside—A Review of Its Antitumor Activities

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