Search Results - "Krystek, Stanley R."
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AggScore: Prediction of aggregation‐prone regions in proteins based on the distribution of surface patches
Published in Proteins, structure, function, and bioinformatics (01-11-2018)“…Protein aggregation is a phenomenon that has attracted considerable attention within the pharmaceutical industry from both a developability standpoint (to…”
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2
Isomerization and Oxidation in the Complementarity-Determining Regions of a Monoclonal Antibody: A Study of the Modification–Structure–Function Correlations by Hydrogen–Deuterium Exchange Mass Spectrometry
Published in Analytical chemistry (Washington) (16-02-2016)“…Chemical modifications can potentially change monoclonal antibody’s (mAb) local or global conformation and therefore impact their efficacy as therapeutic…”
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3
Design for Solubility May Reveal Induction of Amide Hydrogen/Deuterium Exchange by Protein Self-Association
Published in Journal of molecular biology (30-01-2022)“…[Display omitted] •Adnectin scaffold solubility is improved by combined bioinformatic and CamSol analysis.•Adnectins differing at a single amino acid position…”
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4
Structures of Adnectin/Protein Complexes Reveal an Expanded Binding Footprint
Published in Structure (London) (08-02-2012)“…Adnectins are targeted biologics derived from the tenth type III domain of human fibronectin (10Fn3), a member of the immunoglobulin superfamily…”
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5
Development and scale-up of the recovery and purification of a domain antibody Fc fusion protein-comparison of a two and three-step approach
Published in Biotechnology and bioengineering (01-07-2015)“…ABSTRACT A robust, economical process should leverage proven technology, yet be flexible enough to adopt emerging technologies which show significant benefit…”
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Mapping the Energetic Epitope of an Antibody/Interleukin-23 Interaction with Hydrogen/Deuterium Exchange, Fast Photochemical Oxidation of Proteins Mass Spectrometry, and Alanine Shave Mutagenesis
Published in Analytical chemistry (Washington) (21-02-2017)“…Epitope mapping the specific residues of an antibody/antigen interaction can be used to support mechanistic interpretation, antibody optimization, and epitope…”
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Hydrogen/deuterium exchange mass spectrometry and computational modeling reveal a discontinuous epitope of an antibody/TL1A Interaction
Published in mAbs (01-01-2018)“…TL1A, a tumor necrosis factor-like cytokine, is a ligand for the death domain receptor DR3. TL1A, upon binding to DR3, can stimulate lymphocytes and trigger…”
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Functional Antagonism of Human CD40 Achieved by Targeting a Unique Species-Specific Epitope
Published in Journal of molecular biology (17-07-2016)“…Current clinical anti-CD40 biologic agents include both antagonist molecules for the treatment of autoimmune diseases and agonist molecules for…”
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Mapping the Binding Interface in a Noncovalent Size Variant of a Monoclonal Antibody Using Native Mass Spectrometry, Hydrogen-Deuterium Exchange Mass Spectrometry, and Computational Analysis
Published in Journal of pharmaceutical sciences (01-11-2017)“…Variants of monoclonal antibody containing an extra light chain have been reported in protein products. Due to potential impact on potency and immunogenicity,…”
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10
Loopholes and missing links in protein modeling
Published in Protein science (01-09-2007)“…This paper provides an unbiased comparison of four commercially available programs for loop sampling, Prime, Modeler, ICM, and Sybyl, each of which uses a…”
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Discovery of Potent, Orally-Active, and Muscle-Selective Androgen Receptor Modulators Based on an N-Aryl-hydroxybicyclohydantoin Scaffold
Published in Journal of medicinal chemistry (28-12-2006)“…A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered through structure-guided modifications of androgen receptor…”
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12
Pharmacological and X-Ray Structural Characterization of a Novel Selective Androgen Receptor Modulator: Potent Hyperanabolic Stimulation of Skeletal Muscle with Hypostimulation of Prostate in Rats
Published in Endocrinology (Philadelphia) (01-01-2007)“…A novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator (BMS-564929) has been identified, and this compound has…”
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13
Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications
Published in Journal of medicinal chemistry (28-06-2007)“…A novel series of imidazolin-2-ones were designed and synthesized as highly potent, orally active and muscle selective androgen receptor modulators (SARMs),…”
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14
Biotechnology Based Process for Production of a Disulfide-Bridged Peptide
Published in Bioconjugate chemistry (18-05-2016)“…A disulfide-bridged peptide drug development candidate contained two oligopeptide chains with 11 and 12 natural amino acids joined by a disulfide bond at the…”
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15
N-Aryl-oxazolidin-2-imine Muscle Selective Androgen Receptor Modulators Enhance Potency through Pharmacophore Reorientation
Published in Journal of medicinal chemistry (14-05-2009)“…A novel selective androgen receptor modulator (SARM) scaffold was discovered as a byproduct obtained during synthesis of our earlier series of…”
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Closing the side-chain gap in protein loop modeling
Published in Journal of computer-aided molecular design (01-07-2009)“…The success of structure-based drug design relies on accurate protein modeling where one of the key issues is the modeling and refinement of loops. This study…”
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17
Chemical genetics reveals an RGS/G-protein role in the action of a compound
Published in PLoS genetics (01-04-2006)“…We report here on a chemical genetic screen designed to address the mechanism of action of a small molecule. Small molecules that were active in models of…”
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18
Characterization of Aggregation Propensity of a Human Fc-Fusion Protein Therapeutic by Hydrogen/Deuterium Exchange Mass Spectrometry
Published in Journal of the American Society for Mass Spectrometry (01-05-2017)“…Aggregation of protein therapeutics has long been a concern across different stages of manufacturing processes in the biopharmaceutical industry. It is often…”
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Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators
Published in Bioorganic & medicinal chemistry letters (01-04-2007)“…SAR relating to the optimization of androgen receptor agonist activity and elimination of mutagenic potential is reported. Pharmacokinetic studies in…”
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The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists
Published in Bioorganic & medicinal chemistry letters (20-12-2004)“…A novel series of [2.2.1]-bicycloazahydantoins has been designed and synthesized in an enantiospecific manner. Several of these compounds were found to act as…”
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