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Pharmaceutical Chemistry Scholarly Works: Recent submissions
Now showing items 181-200 of 358
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Routes of Administration and Dose Optimization of Soluble Antigen Arrays in Mice with Experimental Autoimmune Encephalomyelitis
(Elsevier, 2015-02)Soluble Antigen Arrays (SAgAs) were developed for treating mice with experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis. SAgAs are composed of hyaluronan with grafted EAE antigen and LABL ... -
Reversion of Sulfenamide Prodrugs in the Presence of Free Thiol Containing Proteins
(Elsevier, 2011-07)The purpose of this work was to study the reaction kinetics between two model sulfenamide prodrugs of linezolid, N-(phenylthio)linezolid and N-((2-ethoxycarbonyl)ethylthio)linezolid, with free thiol containing proteins; ... -
Probing Residue-Specific Interactions in the Stabilization of Proteins Using High-Resolution NMR: A Study of Disulfide Bond Compensation
(Elsevier, 2010-06)It is well established that the oxidation state of cysteine residues in proteins are critical to overall physical stability. The presence of disulfide bonds most often imparts thermodynamic stability, and as such, engineered ... -
Physical characterixation and in vitro biological impact of highly aggregated antibodies separated into size-enriched populations by fluorescence-activated cell sorting
(Elsevier, 2015-05)An IgG2 monoclonal antibody (mAb) solution was subjected to stirring, generating high concentrations of nanometer and subvisible particles, which were then successfully size enriched into different size bins by low speed ... -
Pharmacokinetics and Disposition of a Localized Lymphatic Polymeric Hyaluronan Conjugate of Cisplatin in Rodents
(Elsevier, 2010-06)Cisplatin (CDDP) is an effective anticancer agent for many solid tumors but has significant systemic toxicity limiting its use in many patients. We have designed a loco-regional delivery system to increase platinum levels ... -
Overlooking Subvisible Particles in Therapeutic Protein Products: Gaps that may Compromise Product Quality
(Elsevier, 2009-04)Therapeutic protein products provide unique and effective treatments for numerous human diseases and medical conditions. In many cases, these treatments are used chronically to slow disease progression, reduce morbidity ... -
Native-like aggregates of Factor VIII (FVIII) are immunogenic von Willebrand Factor deficient and hemophilia A mice
(Elsevier, 2012-06)The administration of recombinant Factor VIII (FVIII) is the first line therapy for Hemophilia A (HA), but 25–35% of patients develop an inhibitory antibody response. In general, the presence of aggregates contributes to ... -
NanoClusters Surface Area Allows Nanoparticle Dissolution with Microparticle Properties
(Elsevier, 2014-06)Poorly water soluble drugs comprise the majority of new drug molecules. Nanoparticle agglomerates, called NanoClusters, can increase the dissolution rate of poorly soluble compounds by increasing particle surface area. ... -
Multidimensional Methods for the Formulation of Bipharmaceuticals and Vaccines
(Elsevier, 2011-10)Determining and preserving the higher order structural integrity and conformational stability of proteins, plasmid DNA and macromolecular complexes such as viruses, virus-like particles and adjuvanted antigens is often a ... -
MTX-cIBR Conjugate for Targeting Methotrexate to Leukocytes: Conjugate Stability and in vivo Efficacy in Suppressing Rheumatoid Arthritis
(Elsevier, 2012-09)Methotrexate (MTX) has been used to treat rheumatoid arthritis at low doses and leukemia at high doses; however, this drug can produce severe side effects. Our hypothesis is that MTX side effects can be attenuated by ... -
Modulation of Intercellular Junctions by Cyclic-ADT Peptides as a Method to Reversibly Increase Blood-Brain Barrier Permeability
(Elsevier, 2015-03)It is challenging to deliver molecules to the brain for diagnosis and treatment of brain diseases. This is primarily due to the presence of the blood-brain barrier (BBB), which restricts the entry of many molecules into ... -
High-Throughput Biophysical Analysis and Data Visualization of Conformational Stability of an IgG1 Monoclonal Antibody (mAb) After Deglycosylation
(Elsevier, 2013-11)The structural integrity and conformational stability of an IgG1 monoclonal antibody (mAb), after partial and complete enzymatic removal of the N-linked Fc glycan, was compared to the untreated mAb over a wide range of ... -
Glassy-State Stabilization of a Dominant Negative Inhibitor Anthrax Vaccine Containing Aluminum Hydroxide and Glycopyranoside Lipid A Adjuvants
(Elsevier, 2015-02)During transport and storage, vaccines may be exposed to temperatures outside of the range recommended for storage, potentially causing efficacy losses. To better understand and prevent such losses, Dominant Negative ... -
Formulation and Immunogencity studies of Type III Secretion System needle antigens as Vaccine Candidates
(Elsevier, 2010-11)Bacterial infections caused by Shigella flexneri, Salmonella typhimurium and Burkholderia pseudomallei are currently difficult to prevent due to the lack of a licensed vaccine. Here we present formulation and immunogenicity ... -
Do not drop: Mechanical shock in vials causes cavitation, protein aggregation and particle formation
(Elsevier, 2015-02)Industry experience suggests that g-forces sustained when vials containing protein formulations are accidentally dropped can cause aggregation and particle formation. To study this phenomenon, a shock tower was used to ... -
Development of a Stable Virus-Like Particle Vaccine Formulation against Chikungunya Virus and Investigation of the Effects of Polyanions
(Elsevier, 2013-12)Chikungunya virus (CHIKV) is an alphavirus that infects millions of people every year, especially in the developing world. The selective expression of recombinant CHIKV capsid and envelope proteins results in the formation ... -
CYP1A1 and CYP1B1-mediated biotransformation of the antitrypanosomal methamidoxime prodrug DB844 forms novel metabolites through intramolecular rearrangement
(Elsevier, 2014-01)DB844 (CPD-594-12), N-methoxy-6-{5-[4-(N-methoxyamidino)phenyl]-furan-2-yl}- nicotinamidine, is an oral prodrug that has shown promising efficacy in both mouse and monkey models of second stage human African trypanosomiasis. ... -
The N-terminus of IpaB provides a potential anchor to the Shigella type III secretion system tip complex protein IpaD
(ACS, 2013-12-10)The type III secretion system (T3SS) is an essential virulence factor for Shigella flexneri, providing a conduit through which host-altering effectors are injected directly into a host cell to promote uptake. The type III ... -
Synthesis of CJ-15,208, a novel κ-opioid receptor antagonist
(Elsevier, 2010-09-20)The tryptophan isomers of the cyclic tetrapeptide CJ-15,208, reported to be a kappa opioid receptor (KOR) antagonist [Saito, T.; Hirai, H.; Kim, Y. J.; Kojima, Y.; Matsunaga, Y.; Nishida, H.; Sakakibara, T.; Suga, O.; ... -
Controlling Ligand Surface Density Optimizes Nanoparticle Binding to ICAM-1
(Elsevier, 2011-03)During infection, pathogens utilize surface receptors to gain entry into intracellular compartments. Multiple receptor-ligand interactions that lead to pathogen internalization have been identified and the importance of ...