Hallmark tumor metabolism becomes a validated therapeutic target

Lartigue, Jane De

doi:10.12788/jcso.0389

Cited by 5 publications

(8 citation statements)

References 24 publications

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“…Indeed, virtually every step of glycolysis has been targeted during drug discovery efforts at this point. Although to our knowledge there is not yet an approved glycolysis inhibitor in the clinic [10,11], progress in this area is ongoing.…”

Section: Glycolysismentioning

confidence: 99%

“…It is then unsurprising that well over 2000 small-molecule inhibitors having been reported to date [4]. As was the case for glycolysis inhibitors, no GLS inhibitors are yet approved for use in the clinic [10,11], but research is ongoing. The vast majority of GLS inhibitors have been derived from compound 14, first reported in 2002 [35].…”

Section: Anaplerosismentioning

confidence: 99%

“…These transporters are thus attractive targets for drug development. As yet no LAT1 or ASCT2 inhibitor has entered clinical trials, or been approved for clinical use [10,11], but a number of studies have made progress toward changing that.…”

Section: Nutrient Importmentioning

confidence: 99%

“…Notably, GLUT expression is one of the driving forces that allows positron emission tomography scans to reveal tumor locations [9,102]. Despite their obvious importance to cancer, no inhibitors of the GLUTs have yet advanced to clinical approval, but at least one molecule (ritonavir) is currently undergoing clinical trials for prostate cancer and multiple myeloma [10,11].…”

Section: Executive Summarymentioning

confidence: 99%

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Inhibition of Cancer Metabolism: a Patent Landscape

Katt

Cerione

2019

Pharm. Pat. Anal.

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Cancer metabolism is currently a hot topic. Since it was first realized that cancer cells rely upon an altered metabolic program to sustain their rapid proliferation, the enzymes that support those metabolic changes have appeared to be good targets for pharmacological intervention. Here, we discuss efforts pertaining to targets in cancer metabolism, focusing upon the tricarboxylic acid cycle and the mechanisms which feed nutrients into it. We describe a broad landscape of small-molecule inhibitors, targeting a dozen different proteins, each implicated in cancer progression. We hope that this will serve as a reference both to the areas being most highly examined today and, relatedly, the areas that are still ripe for novel intervention.

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Section: Glycolysismentioning

confidence: 99%

Section: Anaplerosismentioning

confidence: 99%

Section: Nutrient Importmentioning

confidence: 99%

Section: Executive Summarymentioning

confidence: 99%

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Inhibition of Cancer Metabolism: a Patent Landscape

Katt

Cerione

2019

Pharm. Pat. Anal.

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“…Instead of converting glucose to pyruvate to produce adenosine triphosphate (ATP) like normal cells, cancer cells have been known to utilize glutamine, an amino acid contained abundantly in plasma, as a nitrogen and carbon source to synthesize ATP and nucleotides [ 14 ]. During glutaminolysis, glutamine is hydrolyzed to glutamate and ammonia by the mitochondrial enzyme glutaminase1 (GLS1), a process needed to produce substrates for the citric acid cycle and subsequently supply the cells with vital proteins and other important metabolites [ 15 ]. Thus, by inhibiting the function of glutaminases, cell apoptosis and a slower tumor growth is expected and has already been observed in a variety of cases [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

Augmented Therapeutic Potential of Glutaminase Inhibitor CB839 in Glioblastoma Stem Cells Using Gold Nanoparticle Delivery

et al. 2021

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Gold nanoparticles (Au NPs) are studied as delivery systems to enhance the effect of the glutaminase1 inhibitor CB839, a promising drug candidate already in clinical trials for tumor treatments. Au NPs were synthesized using a bottom-up approach and covered with polymers able to bind CB839 as a Au-polymer-CB839 conjugate. The drug loading efficiency (DLE) was determined using high-performance liquid chromatography and characterization of the CB839-loaded NPs was done with various microscopic and spectroscopic methods. Despite the chemical inertness of CB839, Au NPs were efficient carriers with a DLE of up to 12%, depending on the polymer used. The therapeutic effect of CB839 with and without Au was assessed in vitro in 2D and 3D glioblastoma (GBM) cell models using different assays based on the colony formation ability of GBM stem cells (GSCs). To avoid readout disturbances from the Au metal, viability methods which do not require optical detection were hereby optimized. These showed that Au NP delivery increased the efficacy of CB839 in GSCs, compared to CB839 alone. Fluorescent microscopy proved successful NP penetration into the GSCs. With this first attempt to combine CB839 with Au nanotechnology, we hope to overcome delivery hurdles of this pharmacotherapy and increase bioavailability in target sites.

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Emerging Targets and Therapeutics in Immuno-Oncology: Insights from Landscape Analysis

Iyer,

Ivanov,

Tenchov

et al. 2024

J. Med. Chem.

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In the ever-evolving landscape of cancer research, immuno-oncology stands as a beacon of hope, offering novel avenues for treatment. This study capitalizes on the vast repository of immuno-oncology-related scientific documents within the CAS Content Collection, totaling over 350,000, encompassing journals and patents. Through a pioneering approach melding natural language processing with the CAS indexing system, we unveil over 300 emerging concepts, depicted in a comprehensive "Trend Landscape Map". These concepts, spanning therapeutic targets, biomarkers, and types of cancers among others, are hierarchically organized into eight major categories. Delving deeper, our analysis furnishes detailed quantitative metrics showcasing growth trends over the past three years. Our findings not only provide valuable insights for guiding future research endeavors but also underscore the merit of tapping the vast and unparalleled breadth of existing scientific information to derive profound insights. ■ SIGNIFICANCEA "Trend Landscape Map" of emerging concepts in immunooncology has been crafted based on a comprehensive analysis of the extensive CAS Content Collection. The map has been constructed by utilizing a novel Natural Language Processing algorithm in combination with extensive curation by subject matter experts, resulting in identification of >300 emergent topics across eight main areas of interest. The map acts as a visual aid, with detailed quantitative metrics of recent growth illustrating the spread of emerging ideas in immuno-oncology.

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Hallmark tumor metabolism becomes a validated therapeutic target

Cited by 5 publications

References 24 publications

Inhibition of Cancer Metabolism: a Patent Landscape

Inhibition of Cancer Metabolism: a Patent Landscape

Augmented Therapeutic Potential of Glutaminase Inhibitor CB839 in Glioblastoma Stem Cells Using Gold Nanoparticle Delivery

Emerging Targets and Therapeutics in Immuno-Oncology: Insights from Landscape Analysis

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