Robert Kargbo

• Ph.D.
• MEDICINAL CHEMIST at USONA INSTITUTE

The asymmetric intramolecular indium-mediated cyclization reaction delivers chromanes with excellent diastereoselectivity (68-91% yield, dr >99:1). The reaction was efficient for aryl substrates with both electron-withdrawing and -donating groups. Carboxylic acid additives were found to be necessary for optimal reaction.

[reaction: see text] A facile and highly selective indium-mediated allylation of hydrazones utilizing BINOL ligands is described. Chiral (R)-3,3'-bistrifluoromethylBINOL afforded homoallylic amines in up to 97% ee with stoichiometric ligand. Employing only 10 mol % ligand afforded selectivity of up to 92% ee.

Thia-Fries rearrangement of BINOL perfluoroalkylsulfonates affords readily derivatized novel mono- and disulfone ligands in just two steps from enantiomerically pure BINOL. These electron-demanding BINOLs have been successfully applied as catalysts for indium-mediated allylation of N-acylhydrazones. A general and highly enantioselective catalytic p...

The psychedelic renaissance has reignited interest in the therapeutic potential of psychedelics for mental health and well-being. An emerging area of interest is the potential modulation of psychedelic effects by the gut microbiome—the ecosystem of microorganisms in our digestive tract. This review explores the intersection of the gut microbiome an...

Cyclin-dependent kinases (CDKs) are crucial regulators of cell cycle progression and transcription. Their dysregulation has been implicated in various diseases, including cancer. This Patent Highlight focuses on recent advances in the development of CDK inhibitor-E3 ligase binding moiety conjugates for targeted CDK degradation and their potential a...

This Viewpoint discusses the intersection of targeted protein degradation (TPD) technologies and psychedelic research. The resurgence in interest in psychedelics for treating mental disorders and the known genetic variability in responses require new strategies. TPD technologies might address this variability, modulating protein expressions based o...

The KRASG12D mutation, frequently found in pancreatic cancer, is representative of various challenging cancers and is a crucial target for chemotherapy drug development. Researchers are exploring highly selective and potent small molecule inhibitors of KRASG12D to meet the needs of patients with this mutation. The Patent Highlight reveals novel com...

Depression is a widespread issue in the United States and the leading cause of disability globally, impacting people of all ages. Although selective serotonin reuptake inhibitors (SSRIs) are commonly used for treatment, they have limited effectiveness and may take weeks to show results. There is a pressing need for fast and effective solutions for...

Pancreatic carcinoma-1 (PANC-1) is a human pancreatic cancer cell line derived from a pancreatic ductal adenocarcinoma (PDAC) tumor, often used in research to study pancreatic cancer biology, molecular mechanisms, and potential therapeutic interventions. PANC-1 cells exhibit genetic alterations characteristic of pancreatic cancer, such as mutations...

Parkinson's Disease (PD) is a neurodegenerative movement disorder characterized by symptoms like resting tremor, rigidity, bradykinesia, and postural instability, mainly due to dopamine depletion and degeneration of dopaminergic neurons. Mitochondrial dysfunction plays a critical role in the disease's progression, while amyotrophic Lateral Sclerosi...

This Patent Highlight presents a method to treat inflammatory or neurological disorders in subjects needing treatment. The method involves administering a therapeutically effective amount of a composition containing a subhallucinogenic concentration of substituted phenethylamine. The substituted phenethylamine may belong to the 2C-X family, includi...

The psychedelic renaissance has reignited interest in the therapeutic potential of psychedelics for mental health and well-being. An emerging area of interest is the potential modulation of psychedelic effects by the gut microbiome - the ecosystem of microorganisms residing in our digestive tract. This review explores the intersection of the gut mi...

The B-cell lymphoma 2 (BCL-2) protein is the most extensively studied anti-apoptotic member within the BCL-2 protein family. It functions to inhibit programmed cell death by forming a heterodimer with BAX, thereby promoting cellular survival through the extension of tumor cell lifespan and facilitating malignant transformation. This Patent Highligh...

The gut-brain axis (GBA) refers to the sophisticated bidirectional communication system connecting the digestive system with the central nervous system. This interaction is enabled by a series of intricate signaling processes, encompassing various neuro-immune and hormonal pathways. The association between the gut microbiome and mental health has g...

Recent studies reveal that nearly one in seven human cancers exhibit KRAS alterations, contributing to an estimated 19.3 million new cancer cases worldwide in 2020. To date, no marketed mutant-selective and potent KRASG12D inhibitors are available. The current Patent Highlight presents compounds that directly bind to KRASG12D, selectively inhibitin...