ArticleACS medicinal chemistry letters2020
Discovery and Optimization of Rationally Designed Bicyclic Inhibitors of Human Arginase to Enhance Cancer Immunotherapy.
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Article in ACS medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 30 citations in OpenAlex.
- Recent Advancements in the Diversification and Applications of Boron-Containing Compounds in Medicinal Chemistry.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Synthesis of Arginase Inhibitors: An Overview.Pharmaceutics · 2025Review
- A comprehensive review of discovery and development of drugs discovered from 2020-2022.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2024Review
- Amino acid metabolism in immune cells: essential regulators of the effector functions, and promising opportunities to enhance cancer immunotherapy.Journal of hematology & oncology · 2023Review
- In-silico studies to recognize repurposing therapeutics toward arginase-I inhibitors as a potential onco-immunomodulators.Frontiers in pharmacology · 2023Article
- Small molecule-based immunomodulators for cancer therapy.Acta pharmaceutica Sinica. B · 2022Review
- Comprehensive Strategies to Bicyclic Prolines: Applications in the Synthesis of Potent Arginase Inhibitors.ACS medicinal chemistry letters · 2021Article
- Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology.ACS medicinal chemistry letters · 2021Article
- Cryo-EM structures of inhibitory antibodies complexed with arginase 1 provide insight into mechanism of action.Communications biology · 2021Article
- Arginase as a Potential Biomarker of Disease Progression: A Molecular Imaging Perspective.International journal of molecular sciences · 2020Review
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Authors and funding
24 authors at 1 institution in 1 country.
Matthew J MitcheltreeDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Derun LiDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Abdelghani AchabDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Adam BeardDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Kalyan ChakravarthyDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Mangeng ChengDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Hyelim ChoDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Padmanabhan EangoorDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Peter FanDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Symon GathiakaDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Hai-Young KimDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Charles A LesburgDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Thomas W LyonsDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Theodore A MartinotDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
J Richard MillerDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Spencer McMinnDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Jennifer O'NeilDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Anandan PalaniDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Rachel L PalteDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Josep SauríDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
David L SlomanDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Hongjun ZhangDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Jared N CummingDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Christian FischerDiscovery Chemistry; Quantitative Biosciences; Pharmacokinetics, Pharmacodynamics, and Drug Metabolism; Computational and Structural Chemistry; Analytical Research and Development; Process Research and Development; Oncology Discovery; and External Discovery Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Merck & Co., Inc., Rahway, NJ, USA (United States) · US
Funding
No grant is acknowledged in the PubMed record.
Abstract
The action of arginase, a metalloenzyme responsible for the hydrolysis of arginine to urea and ornithine, is hypothesized to suppress immune-cell activity within the tumor microenvironment, and thus its inhibition may constitute a means by which to potentiate the efficacy of immunotherapeutics such as anti-PD-1 checkpoint inhibitors. Taking inspiration from reported enzyme-inhibitor cocrystal structures, we designed and synthesized novel inhibitors of human arginase possessing a fused 5,5-bicyclic ring system. The prototypical member of this class,
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