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Use Of Viral Il-6 To Modulate Monocyte Differentiation To Boost Anti-Tumor Immunity

Researchers at the University of California, Davis have developed a virally derived homolog to increase the inflammatory response desirable in cancer immunotherapy.

Transcription Active Complex Targeting Cancer Drug From Viral Protein Sequence

Researchers at the University of California, Davis have developed a viral peptide therapeutic that targets MYC-based cancerous tumors.

Novel molecular target and approach(es) for the bidirectional modulation of T-cell function

Researchers at UC Irvine have identified and tested a molecular target that regulates T cell function during chronic viral infection and cancer. The molecular target is one of the high mobility group proteins (HMGB2). HMGB2 is a DNA binding protein that regulates transcriptional processes, meaning that its modulation will have profound effects on T cell differentiation and ultimate function by altering the expression of many genes.

15LOX1 Inhibitor Formulation Determination For IV Administration

Lipoxygenases catalyze the peroxidation of fatty acids which contain bisallylic hydrogens between two cis double bonds, such as in linoleic acid (LA) and arachidonic acid (AA). Lipoxygenases are named according to their product specificity with AA as the substrate because AA is the precursor of many active lipid metabolites that are involved in a number of significant disease states. The human genome contains six functional human lipoxygenases (LOX) genes (ALOX5, ALOX12, ALOX12B, ALOX15, ALOX15B, eLOX3) encoding for six different human LOX isoforms (h5-LOX, h12S-LOX, h12R-LOX, h15-LOX-1, h15-LOX-2, eLOX3, respectively). The biological role in health and disease for each LOX isozyme varies dramatically, ranging from asthma to diabetes or stroke. The nomenclature of the LOX isozymes is loosely based on the carbon position (e.g., 5, 12, or 15) at which they oxidize arachidonic acid to form the corresponding hydroperoxyeicosatetraenoic acid (HpETE), which is reduced to the hydroxyeicosatetraenoic acid (HETE) by intracellular glutathione peroxidases. Lipoxygenase inhibitors are difficult to formulate due to challenges with solubility and other factors, therefore new formulations are needed.

Small molecule drug leads for p53 mutant cancers

Researchers at UC Irvine have used a computationally powered method to identify small molecule drug leads that exhibited anti-cancer activity in a human-cell-based assay. These small molecules and the approach used to find them will accelerate the research and development of anti-cancer therapeutics.

Cell Perneable Cyclic Peptide Scaffolds

For the growing list of "undruggable" targets that lack well defined binding pockets  a consensus is emerging that successful inhibìtors will necessarily be larger and more complex than typical small molecule drugs. The targets of existing small molecule drugs make up only a small fraction of the protein encoding genome, and it is estimated that the total "druggable" genome (accessible to inhibition by classic small molecules) represents a small fraction of the total number of potential targets. The number of therapeutic targets that have been unexploited due to poor druggability, such as transcription factors and non-coding RNAs, therefore represent a vast opportunity to make therapeutic advances in virtually every disease category. Macrocycles - in particular, cyclic peptides - have shown remarkable versatility as ligands against challenging therapeutic targets such as protein-protein interactions (PPls). Cyclization is an established method for improving potency in peptides, and cyclization can dramatically improve proteolytic stability. Importantly, the synthesis of cyclic peptides is much more modular and straightforward than the synthesis of organic molecules of similar size and complexity. Large combinatorial lìbraries of cyclic peptides, derived from methods such as DNA-encoded synthesis, phage display and mRNA-d¡splay, have yielded potent inhibitors against a variety of undruggable or challenging targets.

Mitochondria Targeting Photosensitizer for Photodynamic Therapy

Researchers at the University of California, Davis have developed a self-assembling, fibrous photosensitizer that targets mitochondria in tumor cells for destruction via photodynamic therapy with enhanced localization and potency.

Soluble Epoxide Hydrolase Inhibitors For The Treatment Of Arrhythmogenic Cardiomyopathy And Related Diseases

Researchers at the University of California, Davis have developed an effective drug therapy, utilizing Soluble Epoxide Hydrolase (sEH) inhibitors, to prevent sudden death and treat the progression of myocardial dysfunction in patients with Arrhythmogenic Cardiomyopathy (“ACM”).

Novel EphA4 Agonists for the Treatment of ALS

Researchers at the University of California, Riverside (UCR) in collaboration Nationwide Children’s Hospital  have developed and characterized small peptidomimetics that act as EphA4 agonists. Given ALS is a heterogeneous disease, astrocytes reprogrammed from the fibroblasts of patients with sporadic and SOD1-linked ALS (iAstrocytes) were cultured with MNs and the UCR/Nationwide EphA4 agonists.  As seen in Fig. 1, these small agonistic peptidomimetics decrease MN death in iAstrocytes derived from sporadic ALS (sALS) cells.     

Pharmacological fortification and/or restoration of protective nerve coverings via a novel therapeutic target

Researchers at UC Irvine have discovered a novel mechanism by which restoration of protective nerve coverings fails in degenerative disease like multiple sclerosis. While therapeutics to slow disease progression exist, there are currently none aimed at preventing or restoring damage to nerve coverings.

Small Molecule Modulators Of Kir7.1 To Improve Female Reproductive Health

Preterm birth affects more than 10% of pregnancies in the US, and accounts for 85% of perinatal morbidity and mortality. Additionally, conditions such as preeclampsia which are associated with preterm labor can be fatal to both mother and child if left untreated, and chronic conditions such as PCOS result in anovulation in 10% of reproductive-age women. While the administration of progesterone and related compounds has been used to treat these conditions, their mechanism of action remained elusive, severely limiting the effectiveness of drug development and treatment.To address these issues, researchers at UC Berkeley have discovered that through modulation of the Kir7.1 receptor more effective treatments can be sought and existing treatments administered more effectively for these disorders.

Optimized Non-Addictive Biologics Targeting Sodium Channels Involved In Pain Signaling

Researchers at the University of California, Davis have developed high potency and selective peptide inhibitors that act as a non-addictive analgesic for relief of chronic and/or severe pain in humans.

(SD2022-092) Cannabinoid production

Brief description not available

Cannabigerol (CBG) In The Treatment Of Seizures And Epilepsy

Researchers at the University of California, Davis have developed a method of treating or mitigating seizure, treating epilepsy, as well as a method of reducing the frequency of seizures, using cannabigerol or dihydrocannabigerol and analogs thereof.

Small Molecules for Restoring Activity of p53 Mutants found in Human Cancer

This invention consists of novel small molecule compounds that bind to mutant variants of p53 and induce conformational changes to restore p53 function for treatment of human cancers.

Generalizable and Non-genetic Approach to Create Metabolically-active-but-non-replicating Bacteria

Researchers at the University of California, Davis have developed a method to stop bacterial growth while maintaining desirable metabolic functions for therapeutic and biotechnological applications.

Teixobactin O-Acyl Isopeptide Prodrugs

Recently, teixobactin was investigated to treat antibiotic-resistant pathogens, but the drug has yet to reach clinical trial due to its tendency to form gels which prevents accurate dosing. To address this, researchers at the University of California, Irvine have invented a new library of teixobactin related prodrugs which show improved solubility and efficacy versus teixobactin.

(SD2022-270) Algorithm for de novo drug discovery

Generation of drug-like molecules with high binding affinity to target proteins remains a difficult and resource-intensive task in drug discovery. Existing approaches primarily employ reinforcement learning, Markov sampling, or deep generative models guided by Gaussian processes, which can be prohibitively slow when generating molecules with high binding affinity calculated by computationally-expensive physicsbased methods. Researchers a UC San Diego have developed a new approach, named Latent Inceptionism on Molecules (LIMO), which significantly accelerates molecule generation with an inceptionism-like technique. LIMO employs a variational autoencoder-generated latent space and property prediction by two neural networks in sequence to enable faster gradient-based reverse-optimization of molecular properties.

Functionalized Sila-Adamantane

Brief description not available

Integrin Binding to P-Selectin as a Treatment for Cancer and Inflammation

Researchers at the University of California, Davis have developed a potential drug target for cancer and inflammation by studying the binding of integrins to P-selectin.

Modulating MD-2-Integrin Interaction for Sepsis Treatment

Researchers at the University of California, Davis have developed a potential therapeutic treatment for sepsis by modulating the interaction between integrins and Myeloid Differentiation factor 2 (MD-2).

Deep Learning-Based Approach to Accelerate T cell Receptor Design

Researchers at the University of California, Davis have developed a deep learning simulation model to predict mutated T-cell receptor affinity and avidity for immunotherapy applications.

Peptide Inhibitors of Human Voltage Gated Proton Channel hHv1 Activity to Reduce Inflammation

Human voltage-gated proton channels (hHv1) are implicated in a wide range of biological responses, including capacitation of sperm and stimulation of the innate immune response. Human sperm undergo a process called capacitation in the female reproductive tract, whereby intracellular pH rises and stimulates a progesterone-induced Ca2+ influx.  Researchers at the University of California, Irvine have discovered that this calcium influx is controlled by albumin activation of Hv1 voltage-gated proton channels.  Albumin activation of hHV1 in neutrophils also supports production and release of reactive oxygen species and protease during the immune respiratory burst.  These findings demonstrating a stimulatory role of albumin in both sperm and neutrophils has led to new therapeutic approaches to fertility and the treatment of inflammatory diseases.

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