A5022178148- Cancer Treatment and Pharmacology
- RNA Interference and Gene Delivery
- Extracellular vesicles in disease
- Nanoplatforms for cancer theranostics
- Biochemical and Molecular Research
- 14-3-3 protein interactions
- Computational Drug Discovery Methods
- Interstitial Lung Diseases and Idiopathic Pulmonary Fibrosis
- Inflammatory Myopathies and Dermatomyositis
- Microbial Natural Products and Biosynthesis
- Phytochemistry and Biological Activities
- Systemic Sclerosis and Related Diseases
- Advanced biosensing and bioanalysis techniques
- Synthesis and biological activity
- Cytokine Signaling Pathways and Interactions
- Neurological Disease Mechanisms and Treatments
- Click Chemistry and Applications
- Lipid Membrane Structure and Behavior
- Natural product bioactivities and synthesis
- Antimicrobial Peptides and Activities
- Microtubule and mitosis dynamics
- Quinazolinone synthesis and applications
- Ubiquitin and proteasome pathways
University of Minnesota
2017-2022
University of Colorado Boulder
2012-2018
University of Colorado System
2013
Persistent fibrosis in multiple organs is the hallmark of systemic sclerosis (SSc). Recent genetic and genomic studies implicate TLRs their damage-associated molecular pattern (DAMP) endogenous ligands fibrosis. To test hypothesis that TLR4 its coreceptor myeloid differentiation 2 (MD2) drive persistence, we measured MD2/TLR4 signaling tissues from patients with fibrotic SSc, examined impact MD2 targeting using a potentially novel small molecule. Levels TLR4, TLR4-responsive gene signature,...
A series of novel, saccharin-based antagonists have been identified for the interferon signaling pathway. Through in vitro high-throughput screening with Colorado Center Drug Discovery (C2D2) Pilot Library, we hit compound 1, which was basis extensive structure–activity relationship studies. Our efforts produced a lead anti-inflammatory compound, tert-butyl N-(furan-2-ylmethyl)-N-{4-[(1,1,3-trioxo-2,3-dihydro-1λ6,2-benzothiazol-2-yl)methyl]benzoyl}carbamate CU-CPD103 (103), as potent...
The trimer of a bradykinin derivative displayed more than five-fold increase in binding affinity for phosphatidylserine-enriched nanovesicles as compared to its monomeric precursor. nanovesicle selection is directly correlated with multivalency, which amplifies the electrostatic attraction. This strategy may lead development novel molecular probes detecting highly curved membrane bilayers.
Pironetin, the only crystallographically confirmed natural product to target α-tubulin, displays potent cytotoxic activity against sensitive and resistant A2780 ovarian cancer cell lines but is marginally active in vivo. We now report that pironetin has a short half-life (<7 min) human liver microsomes, suggesting its limited vivo efficacy due rapid metabolism. Further, we describe discovery of epoxypironetin as pironetin's major metabolite microsomes.
ADVERTISEMENT RETURN TO ISSUEIn FocusNEXTMeeting Proceedings ICBS2016—Translating the Power of Chemical Biology to Clinical AdvancesYugo Kuriki†, Toru Komatsu*†‡, Peter D. Ycas§, Sara K. Coulup∥, Erick J. Carlson∥, and William C. Pomerantz*§∥View Author Information† Graduate School Pharmaceutical Sciences, University Tokyo, 7-3-1, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan‡ Japan Science Technology Agency (JST), 4-1-8 Honcho Kawaguchi, Saitama 332-0012, Japan§ Department Chemistry, Minnesota,...
Abstract Malignant tumor cells overexpress and release nanosized, lipid-enclosed vesicles referred to as exosomes into body fluids for the primary function of facilitating cell-to-cell communication transferring vital proteins necessary survival other parts body, resulting in metastasis. It was found that an increased secretion peripheral blood is correlated lung cancer melanoma The hallmarks are their highly curved membrane surface (d = ∼30-100 nm) enrichment anionic lipid...
Abstract Malignant tumor cells overexpress and release lipid vesicles called exosomes into the body fluids to facilitate their movement metastasis other parts of body. It was found that an increased secretion in peripheral blood is correlated with lung cancer melanoma metastasis. The hallmarks are highly curved surface (d = ∼30-100 nm) distinct from extracellular enrichment anionic phosphatidylserine (PS) outer leaflet membrane bilayer. These properties provide opportunity selectively...