Researchers from Novartis AG recently reported on the preclinical activity of IAG-933, a first-in-class YAP1/TAZ pan-TEAD protein-protein interaction...
Researchers have identified a druggable pocket on the phosphatase Wip1, which regulates the tumor suppressor TP53 as well as DNA damage repair proteins. The work, which was published in Frontiers in Molecular Biosciences on April 18, 2023, by researchers from the University of Pennsylvania, could lead to therapeutics targeting Wip1. And the computational deep learning methods used to identify the pocket are broadly useful for identifying what the authors call “cryptic” pockets.
High levels of adenosine known to stimulate tumor immunoevasion are formed by the ecto-5’-nucleotidase enzyme (CD73) conversion of adenosine monophosphate to adenosine. CD73 is a cell surface enzyme that is overexpressed in many cancer types where this overexpression has been correlated with a poor prognosis.
Neuroblastoma is among the deadliest cancers in infants, with frequent relapse and long-term survival being <10%. Recently, it has been found that protein RD3 is constitutively expressed in healthy adult and fetal tissues beyond the retina, and it follows a gradient expression from high to low levels in ganglioneuroma and neuroblastoma.
Triple-negative breast cancer (TNBC) constitutes the most aggressive form of breast cancer and presents a high frequency of relapse. The available treatment options are limited and accompanied by resistance and significant treatment side effects.
Researchers from Jacobio Pharmaceuticals Co. Ltd. have reported preclinical data for JAB-X1800, an immunostimulatory antibody-drug conjugate (iADC) targeting CD73. JAB-X1800 was developed using an anti-CD73 monoclonal antibody (MAb) for targeted delivery of a highly potent noncyclic dinucleotide STING agonist payload, JAB-27670.
The infiltration of regulatory T cells (Tregs) into the tumor microenvironment and a low ratio of effector T cells to Tregs is usually tied to tumor progression and poor prognosis. On the other hand, interleukin-2 receptor subunit α (IL-2-RA) is highly expressed on Tregs.
Researchers from Flare Therapeutics Inc. presented the discovery of a first-in-class covalent peroxisome proliferator-activated receptor γ (PPARγ) inverse agonist, FX-909, being developed for the treatment of urothelial cancer (UC). Synthesis and optimization of covalent lead series of agonists of the PPARγ lineage transcription factor led to the discovery of FX-909 as the lead covalent PPARγ inverse agonist with powerful repressive conformational biasing activity.
The U.S. FDA’s green light April 17 for Abbvie Inc. to expand the label of Qulipta (atogepant) – the first and only oral calcitonin gene-related peptide (CGRP) receptor antagonist for migraine, with language that includes prevention of such headaches chronically in adults – provided a welcome addition to the arsenal, but sufferers are still waiting for an improved remedy. Vaxxinity Inc. just might have it. And with a vaccine, no less.
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