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BioWorld - Sunday, February 5, 2023
Home » Topics » Science » New compound

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Microscope
Cancer

Superior immune protection demonstrated by ENPP1 inhibitor GBD-09259 in cancer

Nov. 2, 2022
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Activation of the STING pathway is a strategy to promote antitumor immunity.
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Cancer

Bridgene Biosciences reports discovery of BGI-9004, a potent and efficacious covalent pan-TEAD inhibitor for Hippo-altered cancers

Oct. 31, 2022
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Targeting TEAD with small-molecule inhibitors is an emerging therapeutic strategy for YAP/TAZ-dependent human cancers with Hippo pathway alterations. Bridgene Biosciences Inc. identified three hits with the Isobaric Mass Tagged Affinity Characterization (IMTAC) screening platform that covalently bound to TEAD1 with the binding site being cysteine 359, which led to the BGI-9004 compound.
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Cancer

I-0436650, a potent and selective SHP2 allosteric inhibitor for solid tumor treatment

Oct. 28, 2022
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Src homology region 2-containing protein tyrosine phosphatase 2 (SHP2) is a target for cancer...
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Microscopic view of of high grade urothelial carcinoma of the ureter in a man.
Cancer

FTX-6746, a new PPARG inverse agonist with efficacy in urothelial cancer animal models

Oct. 28, 2022
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Luminal molecular subtype represents most advanced urothelial cancer (UC) cases. It is...
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3D rendering conceptualizing theranostics
Diagnostics

[67Cu]EB-TATE demonstrates efficacy in cellular GP-NET models

Oct. 27, 2022
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Researchers from the University of Saskatchewan have developed a novel theranostic candidate, [67Cu]EB-TATE, as an alternative to [177Lu]DOTATATE, for the imaging of gastroenteropancreatic neuroendocrine tumors (GEP-NET). EB-TATE, which is a derivative of octreotate with evans blue (EB), was radiolabeled with electron linear accelerator-produced 67CuCl2.
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Cancer cell and target
Cancer

F3-8-60, pan-RAS inhibitor with efficacy in malignant peripheral nerve sheath tumors and pancreatic cancer

Oct. 26, 2022
No Comments
Researchers from Qualigen Therapeutics Inc. and University of Louisville presented the discovery and preclinical evaluation of a novel pan-RAS inhibitor...
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Antibodies attacking SARS-CoV-2 virus
Infection

Discovery of novel broadly neutralizing MAb against SARS-CoV-2

Oct. 25, 2022
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Researchers from Emory University have discovered a novel broadly neutralizing SARS-CoV-2 antibody, 002-S21F2, being developed as a potential anti-coronavirus therapeutic.
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Prostate cancer cells
Diagnostics

Peptide substitution stabilizes GRPR antagonist while maintaining its biological features

Oct. 21, 2022
No Comments
The suboptimal metabolic stability of radiolabeled gastrin-releasing peptide receptor (GRPR) antagonists has been a hindering factor of these promising theranostic candidates for prostate cancer. Uppsala University researchers have recently reported the development of [111In]DOTAGA-PEG-2-SAR11-RM-26, after replacement of Gly11 by Sar11 in the peptidic chain.
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Neurology/Psychiatric

Novel mPGES-1 inhibitor demonstrates neuroprotective effects in models of PD

Oct. 21, 2022
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mPGES-1 is overexpressed in the dopaminergic neurons of the substantia nigra pars compacta of post-mortem brain tissue from patients with Parkinson’s disease (PD) as well as in 6-hydroxydopamine (6-OHDA)-injected PD mice.
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PET imaging
Diagnostics

Development of heterobivalent radiotracer targeting PSMA and GRPR

Oct. 21, 2022
No Comments
Researchers have detailed the development and preclinical characterization of a novel heterobivalent radiotracer targeting prostate-specific membrane antigen (PSMA) and the gastrin-releasing peptide receptor (GRPR).
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