Search Results - "Bessire, Andrew J."
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A tag-free collisionally induced fragmentation approach to detect drug-adducted proteins by mass spectrometry
Published in Rapid communications in mass spectrometry (30-11-2015)“…Rationale The covalent modification of proteins by toxicants, new chemical entities or drug molecules, either by metabolic activation or the presence of…”
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LC/MS Methods for Studying Lysosomal ADC Catabolism
Published in Methods in molecular biology (Clifton, N.J.) (01-01-2020)“…A critical component of antibody-drug conjugate (ADC) development is identification or verification of the active released entity upon cellular uptake and…”
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Discovery of First Branched-Chain Ketoacid Dehydrogenase Kinase (BDK) Inhibitor Clinical Candidate PF-07328948
Published in Journal of medicinal chemistry (19-11-2024)“…Inhibition of branched-chain ketoacid dehydrogenase kinase (BDK or BCKDK), a negative regulator of branched-chain amino acid (BCAA) metabolism, is hypothesized…”
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Determination of Antibody–Drug Conjugate Released Payload Species Using Directed in Vitro Assays and Mass Spectrometric Interrogation
Published in Bioconjugate chemistry (20-07-2016)“…Antibody-drug conjugates (ADC) are currently an active area of research, focused primarily on oncology therapeutics, but also to a limited extent on other…”
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Development of Fluorophore-Labeled Thailanstatin Antibody-Drug Conjugates for Cellular Trafficking Studies
Published in Bioconjugate chemistry (19-04-2017)“…As the antibody-drug conjugate (ADC) field grows increasingly important for cancer treatment, it is vital for researchers to establish a firm understanding of…”
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Optimization of Tubulysin Antibody–Drug Conjugates: A Case Study in Addressing ADC Metabolism
Published in ACS medicinal chemistry letters (10-11-2016)“…As part of our efforts to develop new classes of tubulin inhibitor payloads for antibody–drug conjugate (ADC) programs, we developed a tubulysin ADC that…”
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Dirlotapide as a model substrate to refine structure-based drug design strategies on CYP3A4-catalyzed metabolism
Published in Bioorganic & medicinal chemistry letters (01-01-2012)“…Multiple crystal structures of CYP3A4 bound with various substrates or inhibitors have been used as templates for docking of new chemical entities to predict…”
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Deconstruction of Activity-Dependent Covalent Modification of Heme in Human Neutrophil Myeloperoxidase by Multistage Mass Spectrometry (MS4)
Published in Biochemistry (Easton) (13-03-2012)“…Myeloperoxidase (MPO) is known to be inactivated and covalently modified by treatment with hydrogen peroxide and agents similar to…”
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A rapid and specific derivatization procedure to identify acyl-glucuronides by mass spectrometry
Published in Rapid communications in mass spectrometry (30-07-2010)“…A simple procedure is described to identify acyl‐glucuronides by coupled liquid chromatography/mass spectrometry after derivatization to a hydroxamic acid with…”
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Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide
Published in Bioorganic & medicinal chemistry letters (15-07-2011)“…Analogues related to dirlotapide ( 1), a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) were prepared with the goal of further…”
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The use of 18O-exchange and base-catalyzed N-dealkylation with liquid chromatography/tandem mass spectrometry to identify carbinolamide metabolites
Published in Rapid communications in mass spectrometry (30-07-2010)“…Oxidation of N‐alkyl‐substituted amides is a common transformation observed in metabolism studies of drugs and other chemicals. Metabolism at the alpha carbon…”
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Transporter-Enzyme Interplay in the Pharmacokinetics of PF-06835919, A First-in-class Ketohexokinase Inhibitor for Metabolic Disorders and Non-alcoholic Fatty Liver Disease
Published in Drug metabolism and disposition (02-07-2022)“…Excess dietary fructose consumption promotes metabolic dysfunction thereby increasing the risk of obesity, type 2 diabetes, non-alcoholic steatohepatitis…”
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The use of 18 O‐exchange and base‐catalyzed N ‐dealkylation with liquid chromatography/tandem mass spectrometry to identify carbinolamide metabolites
Published in Rapid communications in mass spectrometry (30-07-2010)“…Abstract Oxidation of N ‐alkyl‐substituted amides is a common transformation observed in metabolism studies of drugs and other chemicals. Metabolism at the…”
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