Search Results - "Burke, Terrence R."
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Chemically Programmable and Switchable CAR‐T Therapy
Published in Angewandte Chemie International Edition (13-07-2020)“…Although macromolecules on cell surfaces are predominantly targeted and drugged with antibodies, they harbor pockets that are only accessible to small…”
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Structure of the Rpn13-Rpn2 complex provides insights for Rpn13 and Uch37 as anticancer targets
Published in Nature communications (09-06-2017)“…Proteasome–ubiquitin receptor hRpn13/Adrm1 binds and activates deubiquitinating enzyme Uch37/UCHL5 and is targeted by bis-benzylidine piperidone RA190, which…”
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Harnessing a catalytic lysine residue for the one-step preparation of homogeneous antibody-drug conjugates
Published in Nature communications (24-10-2017)“…Current strategies to produce homogeneous antibody-drug conjugates (ADCs) rely on mutations or inefficient conjugation chemistries. Here we present a strategy…”
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Application of a Fluorescence Recovery-Based Polo-Like Kinase 1 Binding Assay to Polo-Like Kinase 2 and Polo-Like Kinase 3
Published in Biological & pharmaceutical bulletin (11-07-2024)“…Assay systems for evaluating compound protein-binding affinities are essential for developing agonists and/or antagonists. Targeting individual members of a…”
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Efficacies of Cabotegravir and Bictegravir against drug-resistant HIV-1 integrase mutants
Published in Retrovirology (16-05-2018)“…Integrase strand transfer inhibitors (INSTIs) are the class of antiretroviral (ARV) drugs most recently approved by the FDA for the treatment of HIV-1…”
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Synthetic Approaches to a Key Pyridone-carboxylic Acid Precursor Common to the HIV‑1 Integrase Strand Transfer Inhibitors Dolutegravir, Bictegravir, and Cabotegravir
Published in Organic process research & development (19-05-2023)“…Dolutegravir (DTG), Bictegravir (BIC), and Cabotegravir (CAB) are the second-generation integrase strand transfer inhibitors (INSTIs) that have been…”
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Recent Advances and New Strategies in Targeting Plk1 for Anticancer Therapy
Published in Trends in pharmacological sciences (Regular ed.) (01-12-2015)“…Polo-like kinase 1 (Plk1) plays key roles in regulating mitotic processes that are crucial for cellular proliferation. Overexpression of Plk1 is tightly…”
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Site-Specific Lysine Arylation as an Alternative Bioconjugation Strategy for Chemically Programmed Antibodies and Antibody–Drug Conjugates
Published in Bioconjugate chemistry (20-11-2019)“…By exploiting a uniquely reactive lysine residue (Lys99) for site-specific attachment of small molecules, the humanized catalytic antibody h38C2 has been used…”
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Integrase Strand Transfer Inhibitors Are Effective Anti-HIV Drugs
Published in Viruses (29-01-2021)“…Integrase strand transfer inhibitors (INSTIs) are currently recommended for the first line treatment of human immunodeficiency virus type one (HIV-1)…”
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Developing and Evaluating Inhibitors against the RNase H Active Site of HIV-1 Reverse Transcriptase
Published in Journal of virology (01-07-2018)“…We tested three compounds for their ability to inhibit the RNase H (RH) and polymerase activities of HIV-1 reverse transcriptase (RT). A high-resolution…”
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Enhancing precision in colorectal cancer surgery: development of an LGR5-targeting RSPO1 peptide mimetic as a contrast agent for intraoperative fluorescence molecular imaging
Published in Cell cycle (Georgetown, Tex.) (10-07-2024)“…Colorectal cancer (CRC) is the third most common cancer worldwide. In the United States alone, CRC was responsible for approximately 52,550 deaths in 2023,…”
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Retroviral DNA integration: reaction pathway and critical intermediates
Published in The EMBO journal (22-03-2006)“…The key DNA cutting and joining steps of retroviral DNA integration are carried out by the viral integrase protein. Structures of the individual domains of…”
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Uncoupling the Folding-Function Paradigm of Lytic Peptides to Deliver Impermeable Inhibitors of Intracellular Protein–Protein Interactions
Published in Journal of the American Chemical Society (25-11-2020)“…Here, we describe the use of peptide backbone N-methylation as a new strategy to transform membrane-lytic peptides (MLPs) into cytocompatible intracellular…”
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Structural and functional analyses of minimal phosphopeptides targeting the polo-box domain of polo-like kinase 1
Published in Nature structural & molecular biology (01-08-2009)“…The Plk1 kinase is a major regulator of mitosis that is often overexpressed in human cancers. Studies on phosphopeptide inhibitors specific to the polo-box…”
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Examination of aminophenol-containing compounds designed as antiproliferative agents and potential atypical retinoids
Published in Bioorganic & medicinal chemistry (15-03-2023)“…[Display omitted] Retinoic acid (RA, 1), an oxidized form of vitamin A, binds to retinoic acid receptors (RAR) and retinoid X receptors (RXR) to regulate gene…”
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A Practical Approach to Bicyclic Carbamoyl Pyridones with Application to the Synthesis of HIV-1 Integrase Strand Transfer Inhibitors
Published in Molecules (Basel, Switzerland) (01-02-2023)“…An efficient one-pot synthetic method has been developed for the preparation of bicyclic carbamoyl pyridones from the known common intermediate methyl…”
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Affinity enhancement of polo-like kinase 1 polo box domain-binding ligands by a bivalent approach using a covalent kinase-binding component
Published in RSC chemical biology (31-07-2024)“…The polo-like kinase 1 (Plk1) is an important cell cycle regulator that is recognized as a target molecule for development of anti-cancer agents. Plk1 consists…”
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Histidine N(τ)-cyclized macrocycles as a new genre of polo-like kinase 1 polo-box domain-binding inhibitors
Published in Bioorganic & medicinal chemistry letters (15-10-2018)“…[Display omitted] •Peptide macrocyclization is an important step in advancing peptides to peptidomimetics.•Size reduction of Plk1 PBD-binding peptides with…”
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Application of Post Solid-Phase Oxime Ligation to Fine-Tune Peptide-Protein Interactions
Published in Molecules (Basel, Switzerland) (18-06-2020)“…Protein-protein interactions (PPIs) represent an extremely attractive class of potential new targets for therapeutic intervention; however, the shallow…”
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Identification of a ligand binding hot spot and structural motifs replicating aspects of tyrosyl-DNA phosphodiesterase I (TDP1) phosphoryl recognition by crystallographic fragment cocktail screening
Published in Nucleic acids research (04-11-2019)“…Abstract Tyrosyl DNA-phosphodiesterase I (TDP1) repairs type IB topoisomerase (TOP1) cleavage complexes generated by TOP1 inhibitors commonly used as…”
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