Gilead recently conducted a clinical trial for GS-3583, an FMS-like tyrosine kinase 3 (FLT3) agonist Fc fusion protein. Gilead collaborated with NuProbe to develop a qBDA panel that targeted multiple AML hotspot mutations. This qBDA panel significantly helped in the accurate and sensitive detection of drug-induced mutation emergence down to 0.06% variants allele frequency with minimal sequencing depth, offering more information for the trial’s efficacy evaluation. Gilead discovered that other NGS methods were unable to detect what NuProbe's innovative qBDA technology detected. NuProbe’s qBDA technology enhances the precision and effectiveness of cancer therapy research and development. Learn more about Gilead’s clinical trial published in the AACR Editor’s Picks here: https://lnkd.in/gngWUVVX
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ESR1 mutation detection from liquid biopsy or FFPET– order your CE-IVD dPCR test from BIOTYPE! 🔬Exciting news: Orserdu (Elacestrant), the innovative anti-oestrogen, is now available in Germany after EMA approval in September. Patients are eligible for treatment with Orserdu if their cancer cells exhibit oestrogen receptors on their surface (ER-positive), lack significant quantities of the HER2 receptor (HER2-negative), and have a confirmed mutation in the ESR1 gene. For accurate ESR1 testing, liquid biopsy on blood is mandated. 🧬Blood-based ctDNA liquid biopsy or FFPET-DNA testing by digital PCR, in line with several medical guidelines in oncology, offers superior sensitivity in detecting ESR1 mutations. 🧪BIOTYPE will support the nationwide supply of ESR1 testing. If you are interested in learning more about ESR1 testing, klick the link below or contact us for more information: https://lnkd.in/eNQxvuYa #ESR1 #HER2 #liquidbiopsy #breastcancer #oncology
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Predicting response to checkpoint inhibitor therapy is challenging. What if there was a way to identify individuals who would respond favorably to checkpoint inhibitor therapy based on biomarkers found in blood? Read our latest blog “Biomarker discovery leading the way in PD-L1 expression and PD-1 checkpoint inhibitor therapy” to learn more about complex cancer pathways and to investigate the potential of targeting PD-L1 expression & the PD-1 checkpoint pathway in cancer. https://lnkd.in/g6pffxEC #CancerResearch #Proteomics
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Predicting response to checkpoint inhibitor therapy is challenging. What if there was a way to identify individuals who would respond favorably to checkpoint inhibitor therapy based on biomarkers found in blood? Read our latest blog "Biomarker discovery leading the way in PD-L1 expression and PD-1 checkpoint inhibitor therapy" to learn more about complex cancer pathways and to investigate the potential of targeting PD-L1 expression & the PD-1 checkpoint pathway in cancer. https://lnkd.in/g6pffxEC #CancerResearch #Proteomics
Advancing immunotherapy: PD-1 checkpoint focus - SomaLogic
https://somalogic.com
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Predicting response to checkpoint inhibitor therapy is challenging. What if there was a way to identify individuals who would respond favorably to checkpoint inhibitor therapy based on biomarkers found in blood? Read our latest blog "Biomarker discovery leading the way in PD-L1 expression and PD-1 checkpoint inhibitor therapy" to learn more about complex cancer pathways and to investigate the potential of targeting PD-L1 expression & the PD-1 checkpoint pathway in cancer. https://lnkd.in/g6pffxEC #CancerResearch #Proteomics
Advancing immunotherapy: PD-1 checkpoint focus - SomaLogic
https://somalogic.com
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Predicting response to checkpoint inhibitor therapy is challenging. What if there was a way to identify individuals who would respond favorably to checkpoint inhibitor therapy based on biomarkers found in blood? Read our latest blog "Biomarker discovery leading the way in PD-L1 expression and PD-1 checkpoint inhibitor therapy" to learn more about complex cancer pathways and to investigate the potential of targeting PD-L1 expression & the PD-1 checkpoint pathway in cancer. https://lnkd.in/g6pffxEC #CancerResearch #Proteomics
Advancing immunotherapy: PD-1 checkpoint focus - SomaLogic
https://somalogic.com
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They say good things come in threes so here's out third preprint of the month! In collaboration with the Witze lab in Cancer Biology, we developed the first selective small molecule inhibitors of a palmitoyl transferase! Our lead compound phenocopies genetic ablation of DHHC20, reducing EGFR palmitoylation, Akt phosphorylation and Myc expression. Excitingly it's also orally bioavailable and significantly improves survival in KRas mutant lung cancer xenografts. Finally, we were able to use our recently published proximity ligation imaging approach to demonstrate on-target activity in vivo! https://lnkd.in/ekQHXdqj https://lnkd.in/e235KXNt
A selective S-acyltransferase inhibitor suppresses tumor growth
biorxiv.org
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Medicinal Chemistry - Project Leader; Technology Innovation & External Platforms presso Alfasigma - parla di #scienze #farmaci #farmaceutico #ricerca #innovazione #sociale
HETEROCYCLIC-CONTAINING HDAC INHIBITORS ACTIVE IN CANCER Cancer is a leading cause of mortality worldwide. A biological target validated in recent years in the pharmacological armamentarium are histone deacetylases (HDACs), epigenetic enzymes that remove acetyl groups from lysines present on histone tails, and overexpressed in various types of cancer. The first HDA inhibitor in history to be approved by the FDA (October 2006) was Zolinza (vorinostat), used to treat Cutaneous T-cell Lymphoma. To date, there are several HDA inhibitors approved by regulatory bodies: vorinostat (SAHA), romidepsin (FK-228), panobinostat (LBH589), and belinostat (PDX-101) are approved by the Food and Drug Administration. In 2021, China and Japan have approved the use of chidamide (epidaza/tucidinostat; HBI-8000), a new subtype-selective HDACi that inhibits class 1 HDAC1, HDAC2, HDAC3, as well as class 2b HDAC10. Many of these inhibitors are based on a heterocyclic structure, a structural element that has been particularly interesting in the design of this class of compounds. An updated review, just published in ChemMedChem, summarizes all major studies conducted so far on HDAC inhibitors, with heterocyclic rings, as their therapeutic potential is well known and has gained increasing interest in recent years. Therefore, the insertion of heterocyclic moieties into the scaffold that inhibits HDAC may be a valuable strategy to deliver potent and/or selective compounds. Here, in addition to summarizing the properties of new heterocyclic HDAC-inhibiting compounds, ideas are provided for the development of novel, more potent and selective compounds for the treatment of cancer. #heterocyclic #HDAC #cancer
Full professor of Medicinal Chemistry & Chemical Biology at the University of Salerno; Secretary of the EFMC Executive Committee; Chair of the Editorial Board of ChemMedChem
Histone Deacetylases (HDACs), epigenetic enzymes that remove acetyl groups from lysines on histone’s tails, are overexpressed in various types of cancer, and their inhibition represents a valid therapeutic strategy to fight tumor progression. To date, some HDAC inhibitors have achieved FDA approval. Nevertheless, several other potential drug candidates have been developed. A review article just accepted in ChemMedChem (Chemistry Europe) provides a comprehensive overview of the studies done so far regarding HDAC inhibitors bearing heterocyclic rings, the therapeutic potential of which has gained increasing interest in recent years. In addition to summarizing the properties of novel heterocyclic HDAC inhibiting compounds, the article also provides ideas for developing new, more potent, and selective compounds for treating cancer. Heterocycles-Containing HDAC Inhibitors Active in Cancer: An Overview of the Last Fifteen Years Alessia Raucci, Carola Castiello, Antonello Mai, Clemens Zwergel, sergio valente (Sapienza Università di Roma) https://lnkd.in/dauUdAVb
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Acquired resistance to first to third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) is a significant challenge in the treatment of cancers, particularly non-small cell lung cancer (NSCLC). The triple mutant forms of EGFR, either 19Del/T790M/C797S or L858R/T790M/C797S, are known to confer resistance to these inhibitors. Development of fourth-generation EGFR TKIs is currently undergoing, designed to overcome the resistance mechanisms that limit the efficacy of earlier generations. Carna’s EGFR protein products & services will help accelerate your research and development of novel next-gen EGFR inhibitors!! Please check our lineups on our website at Protein products https://lnkd.in/dhGWHExD Mobility Shift Assay Services https://lnkd.in/gfts7Rdg NanoBRET TE Intracellular Kinase Assays https://lnkd.in/gxjza7JD We are always pleased to receive your feedback or comments^^ Please contact us at [email protected] #kinases #EGFR #MobilityShiftAssay #NanoBRET™ #Drugdiscovery #kinaseinhibitor #EGFRmutants [Image: IC50s of three 4th generation EGFR inhibitors (Mobility Shift Assay platform using Carna’s GST-tagged EGFRs, ATP=~Km) Note: d746-750 is one of the major deletions within exon 19 (del19)]
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Predicting response to checkpoint inhibitor therapy is challenging. What if there was a way to identify individuals who would respond favorably to checkpoint inhibitor therapy based on biomarkers found in blood? Read our latest blog "Biomarker discovery leading the way in PD-L1 expression and PD-1 checkpoint inhibitor therapy" to learn more about complex cancer pathways and to investigate the potential of targeting PD-L1 expression & the PD-1 checkpoint pathway in cancer. https://lnkd.in/g6pffxEC #CancerResearch #Proteomics
Advancing immunotherapy: PD-1 checkpoint focus - SomaLogic
https://somalogic.com
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Coinhibition of topoisomerase 1 (TOP1) and bromodomain-containing protein 4 (BRD4) synergistically induces tumor regression. This synergistic effect of TOP1 + BRD4 inhibition is specific to cancer cells leaving normal cells unaffected, which is very interesting from safety and quality-of-life perspective. We have a strong interest from our research on chemotherapy induced mucositis. https://lnkd.in/dMweZ2QU
Coinhibition of topoisomerase 1 and BRD4-mediated pause release selectively kills pancreatic cancer via readthrough transcription - PubMed
pubmed.ncbi.nlm.nih.gov
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