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Engineered Phosphite Dehydrogenases for Recycling Orthogonal Noncanonical Cofactors

Engineered phosphite dehydrogenases enable efficient recycling of noncanonical redox cofactors for sustainable biomanufacturing.

Immune Impact Of Cyclic STAT3 Decoy Therapy

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Inhibitors Of P90 Rsk

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CAPTaINs: Capped And Protected Targeted Immunoproteasome N-End Degrons

CAPTaINs provide a novel, selective, and stable method for selective degradation of protein targets.

Anti-Cxcr6 Treatment For Myocarditis

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1-(Benzo[1,2-b:4,5-b']Difuran-4-yl)alkyl-2-amines and 1-(2,3,6,7-Tetrahydrobenzo[1,2-b:4,5-b']Difuran-4-yl)butan-2-amines as Serotonin Receptor Modulators for Neurodegenerative Disorders

Researchers at the University of California, Davis have developed novel serotonin receptor modulators designed as mixed 5-HT2A/2C partial agonists that demonstrate promising disease-modifying potential for Parkinson’s Disease with improved safety and efficacy.

Azocino[4,5,6-cd]Indoles, Methods for Preparation and Medical Use Thereof: Simplified Synthetic Access to a New Class of 5-HT Ligands

Researchers at the University of California, Davis have developed a novel class of compounds for modulating serotonin receptors, offering potential treatment for various psychiatric and neurological disorders without inducing hallucinogenic effects.

Selection Of DNA-Encoded Libraries For Membrane-Permeable Scaffolds

Combinatorial encoded library technologies can provide a set of tools for discovering protein-targeting ligands (molecules) and for drug discovery. These techniques can accelerate ligand discovery by leveraging chemical diversity achievable through genetically encoded combinatorial libraries, for example, by combinatorial permutation of chemical building blocks. Although display technologies such as mRNA and phage display use biological translation machinery to produce peptide-based libraries, hits from these libraries often lack key drug-like properties, for example, cell permeability. This limitation can arise from the peptide backbone's inherent polarity and the tendency to select compounds with polar/charged side chains. Backbone N-methylation can increase scaffold lipophilicity in mRNA display; however, codon table constraints can necessitate longer sequences to fully utilize the available space.DNA-encoded libraries (DELs) offer an alternative approach towards discovering hits against drug targets. However, like other encoded library techniques, DELs face significant obstacles in affinity selections, which tend to enrich library members bearing polar and/or charged moieties, which can have low (poor) passive cell membrane permeability, especially in larger molecular weight libraries, resulting in hits with poor drug-like properties. This selection bias is especially problematic for larger constructs beyond the rule of 5, where fine-tuning lipophilicity can be critical. Furthermore, DNA-encoded libraries can be of low quality. Although algorithmic predictions of lipophilicity exist, these two-dimensional (2D) atomistic calculations cannot capture conformational effects exhibited by larger molecules like peptide macrocycles. Despite over a decade of DEL technology development, no method exists to measure physical properties of encoded molecules across an entire DNA-encoded library. That is, successful translation of hits from encoded library selections can be impeded by low quality libraries and enrichment of highly polar members which tend to have poor passive cell permeability, especially for larger molecular weight libraries.DELs are produced through split-pool synthesis with DNA barcoding to encode the building block of each chemical step. Although this approach can draw on a large number of building blocks and allow for the formation of non-peptidic libraries with a large number of members, synthetic challenges persist. The formation of DELs can be synthetically inefficient. Truncations multiply ( are compounded) throughout synthesis, reducing the representation of properly synthesized constructs. Although strategies to improve library purity, to enable reaction monitoring for macrocycle formation, and to identify problematic chemistry affecting DNA tag amplification may be applied, a direct method for assessing DEL quality on a library-wide basis has yet to be developed.   

Using Class I Lasso Peptides to Inhibit the Bacterial Type III Secretion System

Antibiotic resistance is a major issue in infectious disease treatment and prevention. In bacteria, the type III secretion system (T3SS) secretes effector proteins in the host cell, allowing the pathogen to infect. The T3SS is largely found on pathogens and not beneficial bacteria, so targeting the T3SS might have an advantage over using classic antibiotics, which disturb the beneficial human microbiome.

Silyl-lipid Cannabinoids with Enhanced Biological Activity

Researchers at the University of California, Davis have developed a therapeutic use of cannabinoids for the treatment of Neurodegenerative Disorders (NDDs).

Small Molecule Activators Of GTP Hydrolysis For Mutant Ras-Driven Cancer

Oncogenic mutations in the Ras family of small GTPases (like K-Ras, H-Ras, and N-Ras) are major drivers of many human cancers, yet they remain one of the most challenging targets in oncology. These mutations often trap the Ras protein in its active, GTP-bound state, leading to continuous, unchecked cell proliferation. To address this, UC Berkeley researchers have developed a novel class of Small Molecule Activators of GTP Hydrolysis for Mutant Ras-driven Cancer.These compounds accelerate the natural, but often disabled, guanosine triphosphate (GTP) hydrolysis process in mutant Ras, essentially forcing the protein back into its inactive, GDP-bound state. The compounds utilize a modular, "plug-and-play" structure. This modular platform is unique in its ability to reactivate the intrinsic GTPase function of mutant Ras, offering a promising, direct-acting therapeutic strategy against previously intractable Ras-driven cancers.

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