Researchers from Bristol Myers Squibb Co. presented the discovery and preclinical evaluation of a novel diacylglycerol kinases (DGK) α and ζ dual inhibitors.
Researchers from the U.S. National Institutes of Health and collaborators recently conducted a study investigating the mechanisms of HIV-1 resistance to integrase strand transfer inhibitors (INSTIs), such as the approved drug dolutegravir (DTG). They focused on understanding the mechanisms of resistance caused by mutations at positions 138, 140, and 148 and analyzed combinations of the mutations E138K, G140A/S, and Q148H/K/R, all conferring resistance to INSTIs.
The role of the enzyme γ-secretase in neuronal cholesterol metabolism could have a beneficial effect on the synapse that has not yet been explored in Alzheimer’s disease (AD). On Aug. 4, 2023, scientists at Stanford University School of Medicine and the Howard Hughes Medical Institute published a study online in Neuron that linked cholesterol levels in the brain to synaptic dysfunction in AD.
Researchers at Merck & Co. Inc. have presented the discovery of novel selective metabotropic glutamate receptor 2 (mGluR2) negative allosteric modulators (NAMs) as potential PET imaging agents. Synthesis and optimization of a series of analogues of a potent and selective mGluR2 NAM resulted in the identification of compound MK-8056 as a high-affinity mGluR2 NAM (Ki=0.19 nM) with desirable lipophilicity (logD7.0=2.46) and low P-gp susceptibility.
Genprex Inc. announced that the FDA has granted orphan drug designation to the company's lead drug candidate, Reqorsa immunogene therapy (quaratusugene ozeplasmid, GPX-001), for the treatment of small cell lung cancer (SCLC). Reqorsa contains a plasmid that expresses the tumor suppressor gene TUSC2, the expression of which is reduced or not present in SCLC.
In a study reported in the online edition of Science on Aug. 10, 2023, a group of synthetic biologists from the University of California (UC) San Diego and clinicians from Australia have engineered synthetic bacteria to detect specific DNA sequences in the genomes of colorectal cancer (CRC) cells and organoids. This living cell sensor capable of detecting cancer in the colons of mice has the potential to steer the way to new biosensors capable of identifying various infections, cancers and other diseases.
The composition of the skull bone is unique and plays a direct role in influencing brain health through small channels in the bone and immune cell expression pathways, reported researchers based at the Helmholtz Center and Ludwig-Maximilians University Munich.
Guangzhou Lupeng Pharmaceutical Co. Ltd. and Newave Pharmaceutical LLC have divulged (mutant) ligands reported to be useful for the treatment of cancer, autoimmune disease and inflammation.
Wigen Biomedicine Technology (Shanghai) Co. Ltd. has identified mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1) inhibitors reported to be useful for the treatment of cancer.
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