Drug candidate PAWI-2 fights drug-resistant pancreatic cancer stem cell tumors.
San Diego, Calif., May 27, 2024 – A collaborative team at the Human BioMolecular Research Institute (HBRI) utilized a grant award from The Conrad Prebys Foundation to continue to develop a drug candidate that potently inhibits drug resistant human pancreatic cancer stem cell proliferation and inhibits metastasis and relapse via a novel mechanism.
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Reengineering mexiletine by chemical synthesis to decrease toxicity and improve pharmacological properties with patient-derived iPSC cardiomyocytes.
In the United States, almost one million individuals are hospitalized every year for cardiac arrhythmias, making arrhythmias one of the top causes of healthcare expenditures with a direct cost of almost $50 billion annually. In the United States, almost 300,000 individuals die of sudden arrhythmic death syndrome every year.
Ventricular cardiac arrhythmia arises in acquired or congenital heart disease. Arrhythmias are very common in older adults but unfortunately, drugs to treat arrhythmias have liabilities. In addition, numerous investigational drugs have been withdrawn from the market because they induce QT prolongation and a potentially fatal ventricular tachycardia, a condition called Torsade de Pointes. For normal heart cell function, sodium channels rapidly inactivate with depolarization.
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Human-induced pluripotent stem cell-derived cardiomyocytes: Cardiovascular properties and metabolism and pharmacokinetics of deuterated mexiletine analogs
In the United States, almost one million individuals are hospitalized every year for cardiac arrhythmias, making arrhythmias one of the top causes of healthcare expenditures with a direct cost of almost $50 billion annually. Almost 300,000 individuals die of sudden arrhythmic death syndrome every year.
Ventricular cardiac arrhythmia arises in acquired or congenital heart disease. Arrhythmias are very common in older adults but unfortunately, drugs to treat arrhythmias have liabilities. In addition, numerous investigational drugs have been withdrawn from the market because they induce QT prolongation and a potentially fatal ventricular tachycardia, a condition called Torsade de Pointes.
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Anti-Arrhythmic Hit to Lead Refinement in a Dish using Patient-Derived iPSCs
In the United States, almost one million individuals are hospitalized every year for cardiac arrhythmias, making arrhythmias one of the top causes of healthcare expenditures with a direct cost of almost $50 billion annually. Almost 300,000 individuals die of sudden arrhythmic death syndrome every year.
Medicinal chemists at the Human BioMolecular Research Institute (HBRI), in San Diego, CA, and stem cell biologists at Stanford University, in Stanford, CA, and cardiovascular pharmacologists at UCLA in Los Angeles, CA and Columbia University, in New York City, NY, respectively, reported on reengineered mexiletine compounds that showed improved potency and decreased toxicity in addressing ventricular cardiac arrhythmia.
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The Conrad Prebys Foundation funds the Human BioMolecular Research Institute to research a drug candidate to fight drug-resistant pancreatic cancer.
San Diego, Calif., March 23, 2021 – A collaborative team at the Human BioMolecular Research Institute (HBRI) will utilize The Conrad Prebys Foundation award to develop a drug candidate that potently inhibits drug resistant human pancreatic cancer stem cells and inhibits metastasis and relapse via a novel mechanism. HBRI has already identified a drug candidate that shows efficacy to eradicate pancreatic cancer stem cells and HBRI scientists are eager to develop the candidate in partnership with The Conrad Prebys Foundation.
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Molecules, Stress Signaling and Wnt Responsiveness
Small molecules are important in chemical genetics exploration of intracellular pathways involved in normal and pathological processes. Wnt signaling plays a central role in tissue maintenance and cancer. This report showed a mechanism by which mitotic and genotoxic stress modulates Wnt responsiveness to control cell shape and renewal. The paper was featured in the journal Cell Chemical Biology.
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RECENT NEWS
San Diego, California – December, 2020. Medicinal chemists and biologists at the Human BioMolecular Research Institute (HBRI), in San Diego, CA, and University of California, San Diego (UCSD), in San Diego, CA, respectively, have reported on a technology to robustly produce human bone cells from stem cells. This may have importance for spinal fusion and addressing other bone cell disease drug discovery efforts.
San Diego, Calif., June 8, 2020 –Researchers at the Human BioMolecular Research Institute and ChemRegen, Inc., have reported on a small molecule p53 Activator Wnt Inhibitor-2 (PAWI-2) that potently inhibits human pancreatic cancer stem cells. Writing June 8, 2020 in the journal Scientific Reports, the team describes how they tested PAWI-2, a synthetic, drug-like compound that can be used to decrease human pancreatic cancer.
Link to read full article here
San Diego, Calif., November 15, 2019 – Researchers at the Human BioMolecular Research Institute and Pain Therapeutics, Inc., (now Cassava Sciences, Inc.,) reported that a new metabolite of oxycodone was quantified in rat and humans. Publishing November 15, 2019, in Drug Metabolism and Disposition, the team describes how they identified and characterized a new metabolite of oxycodone, oxycodone-N-oxide. Oxycodone-N-oxide is also retro-reduced by reductases to afford oxycodone in newly described metabolic pathways.
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San Diego, Calif., October 3, 2019 – Researchers at the Human BioMolecular Research Institute and ChemRegen, Inc., reported that a small molecule potently inhibited prostate cancer. Publishing October 3, 2019, in the Journal of Pharmacology and Experimental Therapeutics, the team describes how they tested PAWI-2, a man-made, drug-like chemical that can be used to inhibit prostate cancer and other cancers.
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San Diego, Calif., July 25, 2019-Researchers at the Stanford Cardiovascular Institute and the Department of Medicine, Stanford University, Sanford-Burnham-Prebys Medical Discovery Institute, Icagen, Human BioMolecular Research Institute, University Medical Center Ulm, Germany, Regencor, Sanofi, France and ChemRegen, Inc., have reported on a small molecule that potently inhibited hematologic cancer and promoted skeletal muscle differentiation. Writing July 25, 2019 in the journal Scientific Reports, the team described how they found and tested a RBPJ Inhibitor-1 (RIN1), a small molecule, drug-like compound that can be used to decrease cancer.
San Diego, Calif., February 15, 2019 – Researchers at the Human BioMolecular Research Institute, University of California San Diego School of Medicine and ChemRegen, Inc., have reported on a small molecule that potently inhibits pancreatic cancer. Writing January 18, 2019 in the journal American Journal of Cancer Research, the team describes how they tested HBRI-1, a synthetic, drug-like compound that can be used to decrease pancreatic cancer.
San Diego, Calif. (July 28, 2018) – Novel Tertiary Sulfonamides as Potent Anti-Cancer Agents.
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San Diego, Calif. (July 21, 2018) – A Novel Inhibitor Targets Both Wnt Signaling and ATM/p53 in Colorectal Cancer
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San Diego, Calif. (April 24, 2018) – Novel Inhibitor Targets both p53-Dependent Apoptotic and Autophagy Pathways as a Pancreatic Cancer Therapeutic
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San Diego, Calif. (October 2017) – Way to Safer New Drugs
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Link to Article in Frontiers in Physiology
San Diego, Calif (October 2017) – Detection of Organophosphates
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Link to Article in Chemical Research and Toxicology
Link to Article in Frontiers in Pharmacology
NEWS ARCHIVE
Novel Stereoselective Synthesis of Mexiletine Analogs (August 2015) Ryan, et. al., 2015
Small Molecule Makes Heart Cells out of Stem Cells (August 2015)
Antibodies to Detect Nerve Agents (December 21, 2012)
Scientists Use Dynamic Medicinal Chemistry to Help Cardiac Regeneration (January 2012)
Molecules To Protect The Brain From Nerve Gas (January 2012) Kalisiak, et. al., 2012
Article by Aaron A. Rowe on C&EN -“Molecules To Protect The Brain From Nerve Gas” (January 2012)
Scientists Use Chemical Biology Approach to Assist Cardiac Regeneration (July 2011)
Scientists Use Stem Cells to Heal Damaged Heart Tissue (January 2011)
Characterization of Human Flavin-Containing Monooxygenase (FMO) 3 and FMO5 Expressed as Maltose-Binding Protein Fusions (December 2010). Reddy, et. al., 2010
Scientists Develop Novel Research Tools for Detecting Organophosphates (October 2010) – View Press Release
Scientists Study New Medications for Depression (May 2010)
Scientists Study Phosphatase Enzyme and Cancer (May 2010)
Scientists Study Model Compounds that Mimic Neurodegenerative Agents (October 2009) Gilley, et al, 2009; Barakat, et al, 2009
Scientists find new potential antidote for cocaine drug abuse by studying cocaine intake in rats (September 2009) Wee, et al, 2009
Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation (August 2009)
Scientists Identify Cooperative Effects of Vitamin D and Active Chemical in Curry that Stimulates the Immune System to Clear Amyloid Plaques in Alzheimer’s Disease (July 2009) Masoumi, et al, 2009
Novel variants of the human flavin-containing monooxygenase 3 (FMO3) gene associated with trimethylaminuria (June 2009)
Research Institute Celebrates 10 years (May 2009)
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake (March 2009)
New approach to treating CNS disorders, including depression and memory(March 2009)
Hepatic flavin-containing monooxygenase gene regulation in different mouse inflammation models (March 2009)
Local 5th Grade Students Participate in Annual Science Day at HBRI (March 2009)
Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression (January 2009)
Local Non-Profit Advancing Diesease Research and Science Education (January 2009)
Click Here to View Additional Scientific Publications by HBRI