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Pharmaceutical Chemistry Scholarly Works: Recent submissions
Now showing items 161-180 of 358
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A small-molecule inhibitor of the aberrant transcription factor CBFβ-SMMHC delays leukemia in mice
(American Association for the Advancement of Science, 2015-02-13)Acute myeloid leukemia (AML) is the most common form of adult leukemia. The transcription factor fusion CBFβ-SMMHC (core binding factor β and the smooth-muscle myosin heavy chain), expressed in AML with the chromosome ... -
Reversible hydrogen transfer reactions of cysteine thiyl radicals in peptides: the conversion of cysteine into dehydroalanine and alanine, and of alanine into dehydroalanine
(American Chemical Society, 2011-10-27)The photodissociation of disulfide bonds in model peptides containing Ala and Ala-d3 generates a series of photoproducts following the generation of a CysS• thiyl radical pair. These photoproducts include transformations ... -
Synthesis and Antiprotozoal Activity of Dicationic 2, 6-Diphenylpyrazines and Aza-Analogues
(Elsevier, 2013-08-13)Dicationic 2,6-diphenylpyrazines, aza-analogues and prodrugs were synthesized; evaluated for DNA affinity, activity against Trypanosoma brucei rhodesiense (T. b. r.) and Plasmodium falciparum (P. f.) in vitro, efficacy in ... -
Modular Assembly of Dimeric HIV Fusion Inhibitor Peptides with Enhanced Antiviral Potency
(Elsevier, 2013-11-15)The HIV-1 envelope gp120/gp41 glycoprotein complex plays a critical role in virus-host cell membrane fusion and has been a focus for the development of HIV fusion inhibitors. In this paper, we present the synthesis of ... -
1H, 15N, 13C Resonance Assignments of the Reduced and Active Form of Human Protein Tyrosine Phosphatase, PRL-1
(Springer Verlag, 2009-06)Phosphatase of regenerating liver-1 (PRL-1) is a novel target for potentially treating cancer metastases. Although its specific biochemical role in these processes has yet to be delineated, considerable evidence suggests ... -
Controlled release of nitric oxide chemotherapy using a nanosized biodegradable multi-arm polymer
(Elsevier, 2012-04)Nitric oxide is a cell signaling molecule that can be a potent inducer of cell death in cancers at elevated concentrations. Nitric oxide molecules are short-lived in vivo; therefore, NO-donating prodrugs have been developed ... -
Rapid Identification of Fluorochrome Modification Sites in Proteins by LC ESI-Q-TOF Mass Spectrometry
(ACS, 2011-07-20)Conjugation of either a fluorescent dye or a drug molecule to the ε-amino groups of lysine residues of proteins has many applications in biology and medicine. However, this type of conjugation produces a heterogeneous ... -
I-Domain-Antigen Conjugate (IDAC) for Delivering Antigenic Peptides to APC: Synthesis, Characterization, and in vivo EAE Suppression
(ACS, 2012-03-21)The objectives of this work are to characterize the identity of I-domain-antigen conjugate (IDAC) and to evaluate the in vivo efficacy of IDAC in suppressing experimental autoimmune encephalomyelitis (EAE) in mouse model. ... -
Conjugation site heterogeneity causes variable electrostatic properties in Fc conjugates
(ACS, 2013-06-19)Immunoconjugates, including antibody-drug conjugates and Fc-conjugates, represent a rapidly growing class of therapeutics undergoing clinical development. Despite their growing popularity, the high intrinsic heterogeneity ... -
Applications and Emerging Trends of Hyaluronic Acid in Tissue Engineering, as a Dermal Filler, and in Osteoarthritis Treatment
(Elsevier, 2013-07)Hyaluronic acid (HA) is a naturally occurring biodegradable polymer with a variety of applications in medicine including scaffolding for tissue engineering, dermatological fillers, and viscosupplementation for osteoarthritis ... -
Low-Temperature NMR Characterization of Reaction of Sodium Pyruvate with Hydrogen Peroxide
(American Chemical Society, 2015-02-12)It was proposed that the reaction of sodium pyruvate and H2O2 generates the intermediate 2-hydroperoxy-2-hydroxypropanoate, which converts into acetate, CO2, and H2O (Aleksankin et al. Kernenergie 1962, 5, 362–365). These ... -
Human gut Bacteroidetes can utilize yeast mannan through a selfish mechanism
(Nature Publishing Group, 2015-01-08)Yeasts, which have been a component of the human diet for at least 7000 years, possess an elaborate cell wall α-mannan. The influence of yeast mannan on the ecology of the human microbiota is unknown. Here we show that ... -
Vorinostat with Sustained Exposure and High Solubility in Poly(ethylene glycol)-b-poly(DL-lactic acid) Micelle Nanocarriers: Characterization and Effects on Pharmacokinetics in Rat Serum and Urine
(Elsevier, 2012-10)The histone deacetylase inhibitor suberoylanilide hydroxamic acid, known as vorinostat, is a promising anti-cancer drug with a unique mode of action; however, it is plagued by low water solubility, low permeability, and ... -
Using Empirical Phase Diagrams to Understand the Role of Intramolecular Dynamics in Immunoglobulin G Stability
(Elsevier, 2009-07)Understanding the relationship between protein dynamics and stability is of paramount importance to the fields of biology and pharmaceutics. Clarifying this relationship is complicated by the large amount of experimental ... -
Use of a folding model and in situ spectroscopic techniques for rational formulation development and stability testing of Monoclonal antibody therapeutics
(Elsevier, 2010-04)Aggregation is a critical issue that hampers the development of monoclonal antibody therapeutics (Mabs). Traditionally, aggregation is considered a process in which native forms of proteins are transformed into an unstable ... -
Two Decades of Publishing Excellence in Pharmaceutical Biotechnology
(Elsevier, 2015-02)Recombinant biological products have revolutionized modern medicine by providing both remarkably effective vaccines to prevent disease and therapeutic drugs to treat a wide variety of unmet medical needs. Since the early ... -
Thiol-Disulfide Interchange in the Tocinoic Acid/Glutathione System During Freezing and Drying
(Elsevier, 2010-12)Thiol-disulfide interchange (“disulfide scrambling”) is a common mechanism of covalent aggregation for protein drugs. Using tocinoic acid (cyclo-S-Cys-Tyr-Ile-Gln-Asn-Cys-(S); TA(ox)) and glutathione (γGlu-Cys-Gly; GSH), ... -
The role of covalent dimerization on the physical and chemical stability of the EC1 domain of human E-cadherin
(Elsevier, 2009-10)The objective of this work was to evaluate the solution stability of the EC1 domain of E-cadherin under various conditions. The EC1 domain was incubated at various temperatures (4, 37, and 70 °C) and pH values (3.0, 7.0, ... -
Structural Characterization of IgG1 mAb Aggregates and Particles Generated under Various Stress Conditions
(Elsevier, 2014-03)IgG1 mAb solutions were prepared with and without sodium chloride and subjected to different environmental stresses. Formation of aggregates and particles of varying size was monitored by a combination of size exclusion ... -
Stability Analysis of an Inline Peptide-based Conjugate for Metal Delivery: Nickel(II)-claMP Tag Epidermal Growth Factor as a Model System
(Elsevier, 2015-02)Metals are a key component of many diagnostic imaging and biotechnology applications, and the majority of cancer patients receive a platinum-based drug as part of their treatment. Significant effort has been devoted to ...