ArticleACS medicinal chemistry letters2021
Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology.
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Article in ACS medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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0cells of the map it votes in
5citing papers in PubMed
1.8field-weighted citation impact, top 15% of its field
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
5 citing papers in PubMed, 25 citations in OpenAlex.
- Synthesis of Arginase Inhibitors: An Overview.Pharmaceutics · 2025Review
- Nanoengineered drug delivery in cancer immunotherapy for overcoming immunosuppressive tumor microenvironment.Drug delivery and translational research · 2023Review
- The expanding role for small molecules in immuno-oncology.Nature reviews. Drug discovery · 2022Review
- OATD-02 Validates the Benefits of Pharmacological Inhibition of Arginase 1 and 2 in Cancer.Cancers · 2022Article
- Comprehensive Strategies to Bicyclic Prolines: Applications in the Synthesis of Potent Arginase Inhibitors.ACS medicinal chemistry letters · 2021Article
Corrections and comments
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Authors and funding
25 authors at 2 institutions in 1 country.
Min LuDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.ORCID https://orcid.org/0000-0003-0378-9134
Hongjun ZhangDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.ORCID https://orcid.org/0000-0002-1136-6142
Derun LiDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.ORCID https://orcid.org/0000-0003-0512-6684
Matthew ChildersDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Qinglin PuDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.ORCID https://orcid.org/0000-0002-7853-4542
Rachel L PalteDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Symon GathiakaDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Thomas W LyonsDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Anandan PalaniDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Peter W FanDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Peter SpacciapoliDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
J Richard MillerDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Hyelim ChoDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Mangeng ChengDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Kalyan ChakravarthyDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Jennifer O'NeilDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Padmanabhan EangoorDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Adam BeardDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Hai-Young KimDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Josep SauríDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Hakan GunaydinDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.ORCID https://orcid.org/0000-0003-1093-2787
David L SlomanDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Phieng SiliphaivanhDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Jared CummingDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Christian FischerDiscovery Chemistry, Computational and Structural Chemistry, Quantitative Biosciences, Discovery Process Chemistry, Discovery Oncology, Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, and Analytical Research and Development, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Merck & Co., Inc., Rahway, NJ, USA (United States) · USQuantitative BioSciences · US
Funding
No grant is acknowledged in the PubMed record.
Abstract
Recent data suggest that the inhibition of arginase (ARG) has therapeutic potential for the treatment of a number of indications ranging from pulmonary and vascular disease to cancer. Thus, high demand exists for selective small molecule ARG inhibitors with favorable druglike properties and good oral bioavailability. In light of the significant challenges associated with the unique physicochemical properties of previously disclosed ARG inhibitors, we use structure-based drug design combined with a focused optimization strategy to discover a class of boronic acids featuring a privileged proline scaffold with superior potency and oral bioavailability. These compounds, exemplified by inhibitors
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