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Medicinal Chemistry: Recent submissions
Now showing items 41-60 of 335
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Synthetic lethality by targeting the RUVBL1/2-TTT complex in mTORC1-hyperactive cancer cells
(American Association for the Advancement of Science, 2020-07-31)Despite considerable efforts, mTOR inhibitors have produced limited success in the clinic. To define the vulnerabilities of mTORC1-addicted cancer cells and to find previously unknown therapeutic targets, we investigated ... -
Phenylalanine Stereoisomers of CJ-15,208 and [d-Trp]CJ-15,208 Exhibit Distinctly Different Opioid Activity Profiles
(MDPI, 2020-09-02)The macrocyclic tetrapeptide cyclo[Phe-d-Pro-Phe-Trp] (CJ-15,208) and its stereoisomer cyclo[Phe-d-Pro-Phe-d-Trp] exhibit different opioid activity profiles in vivo. The present study evaluated the influence of the Phe ... -
Design of Substrate Transmembrane Mimetics as Structural Probes for γ-Secretase
(American Chemical Society, 2020-01-30)γ-Secretase is a membrane-embedded aspartyl protease complex central in biology and medicine. How this enzyme recognizes transmembrane substrates and catalyzes hydrolysis in the lipid bilayer is unclear. Inhibitors that ... -
Reactive Metabolite Target Protein Database (TPDB)
(2020-08-03)The biotransformation of drugs and xenobiotic chemicals in living cells sometimes generates chemically reactive metabolites (CRMs) that diffuse through the cell and react covalently with cellular constituents, especially ... -
The Meta-Position of Phe4 in Leu-Enkephalin Regulates Potency, Selectivity, Functional Activity, and Signaling Bias at the Delta and Mu Opioid Receptors
(MDPI, 2019-12-12)As tool compounds to study cardiac ischemia, the endogenous δ-opioid receptors (δOR) agonist Leu5-enkephalin and the more metabolically stable synthetic peptide (d-Ala2, d-Leu5)-enkephalin are frequently employed. However, ... -
STUDIES OF INTERACTIONS OF SMALL MOLECULES WITH MEMBRANES AND PROTEINS
(University of Kansas, 2019-12-31)The modern molecular understanding of biological systems relies on integration of principles, practices, and techniques from diverse fields such as molecular biology, biochemistry, and biophysics. This approach has provided ... -
Bioactivity Profiling of Plant Biodiversity of Panama by High Throughput Screening
(SAGE Publications, 2019-01-01)We report relative bioactivities of extracts prepared from a large collection of plants from three national parks in Panama. Over 181 plants were collected, taxonomically identified and their detannified dichloromethane ... -
Discovery of Novel Inhibitors of Cellular Efflux by High-Content Screening with a Fluorescent Mimic of Taxol
(University of Kansas, 2019-08-31)Fluorescence-based assays play key roles in drug discovery and development. These assays are widely used due to the widespread availability of fluorescent probes and highly sensitive detection platforms. This method is a ... -
Synthesis and Evaluation of Fluorescent Tools for Studies of Cancer Biology
(University of Kansas, 2019-08-31)A key enabling technology in biological sciences involves fluorescent probes. These probes are typically small molecules, proteins, or nucleic acids that either possess intrinsic fluorescence or are linked to a fluorophore ... -
Dysfunctional γ-Secretase in Familial Alzheimer’s Disease
(Springer Verlag, 2019-01-01)Genetics strongly implicate the amyloid β-peptide (Aβ) in the pathogenesis of Alzheimer’s disease. Dominant missense mutation in the presenilins and the amyloid precursor protein (APP) cause early-onset familial Alzheimer’s ... -
Membrane protein takes the brakes off
(American Association for the Advancement of Science, 2019-02-01) -
Structure and Function of the γ-Secretase Complex
(American Chemical Society, 2019-06-14)γ-Secretase is a membrane-embedded protease complex, with presenilin as the catalytic component containing two transmembrane aspartates in the active site. With more than 90 known substrates, the γ-secretase complex is ... -
Strategies for the Fluorine-Retentive Functionalization of Gem-Difluoroalkenes
(University of Kansas, 2019-05-31)Fluorination is an important strategy for perturbing the biophysical properties of compounds in medicinal chemistry. Specifically, fluorination modulates both the pharmacodynamic and pharmacokinetic properties of bioactive ... -
Studies of novel targeted drug delivery systems and molecular probes of cancer biology
(University of Kansas, 2019-05-31)Cancer is a complex family of diseases. As our understanding of cancer biology has improved, so has our ability to treat the pathology associated with this condition. Traditional anticancer therapeutics lack selectivity ... -
Investigation of the Phenyl Ring of Imidazoquinolines
(University of Kansas, 2018-05-31)The 1H-Imidazo-[4,5-c]quinolines are a class of compounds that are agonists towards Toll-like receptor 7 and 8 (TLR7/8). For example, Imiquimod and Resiquimod have been shown to act as vaccine adjuvants, enhancing ... -
A New Generation of Isoform Selective Hsp90 Inhibitors: Targeting the Cytosolic Hsp90 Isoforms
(University of Kansas, 2018-05-31)Heat shock protein 90 kDa (Hsp90) is a member of the molecular chaperone family of proteins that processes newly synthesized polypeptides into their three-dimensional and biologically active form. In addition, Hsp90 assists ... -
The Development of Organelle-localized Hsp90 Isoform-selective Inhibitors
(University of Kansas, 2017-12-31)Molecular chaperones are responsible for the maturation of nascent polypeptides and the re-maturation of denatured proteins. One chaperone family that has emerged as an attractive therapeutic target is the 90 kDa heat shock ... -
Exploration of Salvinorin A for the Development of Pain and Addiction Therapies
(University of Kansas, 2017-08-31)In the search for effective methods to mitigate the increasing rates of abuse and addiction of illicit substances, a variety of neurological pathways have been explored. Towards this goal of reducing drug abuse and ultimately ... -
I. Development of Bisamides as Kappa Opioid Receptor Agonists. II. Potency Enhancement of Sulfonamide-based Kappa Opioid Receptor Antagonists. III. Asymmetric Acyl Transfer Reactions Catalyzed by a Cyclic Peptide.
(University of Kansas, 2017-05-31)Development of Bisamides as Kappa Opioid Receptor Agonists. The structure-activity relationship (SAR) expansion was carried out on bisamides KOR agonists. Previous four-step linear synthetic route was replaced by Ugi ... -
Design and synthesis of cyclic analogs of the kappa opioid receptor antagonist arodyn
(University of Kansas, 2018-05-31)Opioid receptors are important therapeutic targets for mood disorders and pain. Kappa opioid receptor (KOR) antagonists have recently shown potential for treating drug addiction and depression. Arodyn (Ac[Phe1,2,3,Arg4,D-Ala8]Dyn ...