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Pharmaceutical Chemistry Scholarly Works: Recent submissions
Now showing items 341-358 of 358
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Sequence and Structure Signatures of Cancer Mutation Hotspots in Protein Kinases
(Public Library of Science, 2009-10-16)Protein kinases are the most common protein domains implicated in cancer, where somatically acquired mutations are known to be functionally linked to a variety of cancers. Resequencing studies of protein kinase coding ... -
Hierarchical Modeling of Activation Mechanisms in the ABL and EGFR Kinase Domains: Thermodynamic and Mechanistic Catalysts of Kinase Activation by Cancer Mutations
(Public Library of Science, 2009-08-28)Structural and functional studies of the ABL and EGFR kinase domains have recently suggested a common mechanism of activation by cancer-causing mutations. However, dynamics and mechanistic aspects of kinase activation by ... -
The Energy Landscape Analysis of Cancer Mutations in Protein Kinases
(Public Library of Science, 2011-10-06)The growing interest in quantifying the molecular basis of protein kinase activation and allosteric regulation by cancer mutations has fueled computational studies of allosteric signaling in protein kinases. In the present ... -
Computational Modeling of Allosteric Communication Reveals Organizing Principles of Mutation-Induced Signaling in ABL and EGFR Kinases
(Public Library of Science, 2011-10-06)The emerging structural information about allosteric kinase complexes and the growing number of allosteric inhibitors call for a systematic strategy to delineate and classify mechanisms of allosteric regulation and long-range ... -
Probing Molecular Mechanisms of the Hsp90 Chaperone: Biophysical Modeling Identifies Key Regulators of Functional Dynamics
(Public Library of Science, 2012-05-18)Deciphering functional mechanisms of the Hsp90 chaperone machinery is an important objective in cancer biology aiming to facilitate discovery of targeted anti-cancer therapies. Despite significant advances in understanding ... -
Differential expression of neuregulin-1 isoforms and downregulation of erbin are associated with Erb B2 receptor activation in diabetic peripheral neuropathy
(BioMed Central, 2013-07-17)Background Aberrant neuron/glia interactions can contribute to a variety of neurodegenerative diseases and we have previously demonstrated that enhanced activation of Erb B2, which is a member of the epidermal growth ... -
A novel scoring function for discriminating hyperthermophilic and mesophilic proteins with application to predicting relative thermostability of protein mutants
(BioMed Central, 2010-01-28)Background: The ability to design thermostable proteins is theoretically important and practically useful. Robust and accurate algorithms, however, remain elusive. One critical problem is the lack of reliable methods to ... -
Identification of Properties Important to Protein Aggregation Using Feature Selection
(BioMed Central, 2013-10-28)Background: Protein aggregation is a significant problem in the biopharmaceutical industry (protein drug stability) and is associated medically with over 40 human diseases. Although a number of computational models have ... -
Lysosomotropic Properties of Weakly Basic Anticancer Agents Promote Cancer Cell Selectivity In Vitro
(Plos One, 2012-11-07)Drug distribution in cells is a fundamentally important, yet often overlooked, variable in drug efficacy. Many weakly basic anticancer agents accumulate extensively in the acidic lysosomes of normal cells through ion ... -
Efficacy and Toxicity of Peritumoral Delivery of Nanoconjugated Cisplatin in an In Vivo Murine Model of Head and Neck Squamous Cell Carcinoma
(JAMA otolaryngology-- head & neck surgery, 2013-04-01) -
Sulfobutyl Ether b-Cyclodextrin (SBE-b-CD) in Eyedrops Improves the Tolerability of a Topically Applied Pilocarpine Prodrug in Rabbits
(Mary Ann Leibert, 1995)The effects of a novel, modified β-cyclodextrin (SBE4-β-CD; a variably substituted sulfobutyl ether with an average degree of substitution of four) on eye irritation and miotic response of an ophthalmically applied pilocarpine ... -
Prodrugs: Do They Have Advantages in Clinical Practice?
(Adis Press Limited, 1985-05)Prodrugs are pharmacologically inactive chemical derivatives of a drug molecule that require a transformation within the body in order to release the active drug. They are designed to overcome pharmaceutical and/or ... -
9,10-Anthracenedicarbaldehyde bis[(4,5-dihydro-1H-imidazol-2-yl)hydrazone] acetic acid hydrochloric acid trihydrate salt (Bisantrene)
(International Union of Crystallography, 1986) -
Antigen-specific blocking of immunological synapse formation using bifunctional peptide, Utilization of I-domain of LFA-1 to Target Drug and Marker Molecules to Leukocytes
(Ivyspring International Publisher, 2011-05-01)The long-term objective of this project is to utilize the I-domain protein for the alpha-subunit of LFA-1 to target drugs to lymphocytes by binding to ICAM receptors on the cell surface. The short-term goal is to provide ... -
Mechanism of Binding and Internalization of ICAM-1-derived Cyclic Peptides by LFA-1 on the Surface of T-cells: A Potential Method for Targeted Drug Delivery
(Springer, 2003-10)Purpose Peptides derived from the Domain 1 of the adhesion molecule ICAM-1(1-21) are being developed as targeting ligands for LFA-1 receptors expressed on activated T-cells. This work aims to elucidate the binding and ... -
Inhibition of ICAM-1/LFA-1-mediated Heterotypic T-cell Adhesion to Epithelial Cells: Design of ICAM-1 Cyclic Peptides
(Elsevier, 2004-03)In this work, we have designed cyclic peptides (cIBL, cIBR, cIBC, CH4 and CH7) derived from the parent IB peptide (ICAM-11–21) that are inhibitors of ICAM-1/LFA-1-mediated T-cell adhesion to Caco-2 cell monolayers. Cyclic ... -
Utilization of I-domain of LFA-1 to Target Drug and Marker Molecules to Leukocytes
(Theranostics, 2010-05-10)The long-term objective of this project is to utilize the I-domain protein for the -subunit of LFA-1 to target drugs to lymphocytes by binding to ICAM receptors on the cell surface. The short-term goal is to provide ... -
Prodrugs of peptides and proteins for improved formulation and delivery
(ANNUAL REVIEWS, 1993)