Review ArticleReview Article
The Angiotensin AT2 Receptor: From a Binding Site to a Novel Therapeutic Target
U. Muscha Steckelings, Robert E. Widdop, Edward D. Sturrock, Lizelle Lubbe, Tahir Hussain, Elena Kaschina, Thomas Unger, Anders Hallberg, Robert M. Carey and Colin Sumners
Rhian Touyz, ASSOCIATE EDITOR
Pharmacological Reviews October 2022, 74 (4) 1051-1135; DOI: https://doi.org/10.1124/pharmrev.120.000281
U. Muscha Steckelings
Institute of Molecular Medicine, Department of Cardiovascular and Renal Research, University of Southern Denmark, Odense, Denmark (U.M.S.); Cardiovascular Disease Program, Biomedicine Discovery Institute, Department of Pharmacology, Monash University, Clayton, Victoria, Australia (R.E.W.); Department of Integrative Biomedical Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Republic of South Africa (E.D.S., L.L.); Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, Texas (T.H.); Charité – Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, Institute of Pharmacology, Cardiovascular–Metabolic–Renal (CMR) Research Center, DZHK (German Centre for Cardiovascular Research), Berlin, Germany (E.K.); CARIM – School for Cardiovascular Diseases, Maastricht University, The Netherlands (T.U.); Department of Medicinal Chemistry, Faculty of Pharmacy, Uppsala University, Uppsala, Sweden (A.H.); Division of Endocrinology and Metabolism, Department of Medicine, University of Virginia School of Medicine, Charlottesville, Virginia (R.M.C.); and Department of Physiology and Functional Genomics, University of Florida College of Medicine, Gainesville, Florida (C.S.)
Robert E. Widdop
Institute of Molecular Medicine, Department of Cardiovascular and Renal Research, University of Southern Denmark, Odense, Denmark (U.M.S.); Cardiovascular Disease Program, Biomedicine Discovery Institute, Department of Pharmacology, Monash University, Clayton, Victoria, Australia (R.E.W.); Department of Integrative Biomedical Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Republic of South Africa (E.D.S., L.L.); Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, Texas (T.H.); Charité – Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, Institute of Pharmacology, Cardiovascular–Metabolic–Renal (CMR) Research Center, DZHK (German Centre for Cardiovascular Research), Berlin, Germany (E.K.); CARIM – School for Cardiovascular Diseases, Maastricht University, The Netherlands (T.U.); Department of Medicinal Chemistry, Faculty of Pharmacy, Uppsala University, Uppsala, Sweden (A.H.); Division of Endocrinology and Metabolism, Department of Medicine, University of Virginia School of Medicine, Charlottesville, Virginia (R.M.C.); and Department of Physiology and Functional Genomics, University of Florida College of Medicine, Gainesville, Florida (C.S.)
Edward D. Sturrock
Institute of Molecular Medicine, Department of Cardiovascular and Renal Research, University of Southern Denmark, Odense, Denmark (U.M.S.); Cardiovascular Disease Program, Biomedicine Discovery Institute, Department of Pharmacology, Monash University, Clayton, Victoria, Australia (R.E.W.); Department of Integrative Biomedical Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Republic of South Africa (E.D.S., L.L.); Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, Texas (T.H.); Charité – Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, Institute of Pharmacology, Cardiovascular–Metabolic–Renal (CMR) Research Center, DZHK (German Centre for Cardiovascular Research), Berlin, Germany (E.K.); CARIM – School for Cardiovascular Diseases, Maastricht University, The Netherlands (T.U.); Department of Medicinal Chemistry, Faculty of Pharmacy, Uppsala University, Uppsala, Sweden (A.H.); Division of Endocrinology and Metabolism, Department of Medicine, University of Virginia School of Medicine, Charlottesville, Virginia (R.M.C.); and Department of Physiology and Functional Genomics, University of Florida College of Medicine, Gainesville, Florida (C.S.)
Lizelle Lubbe
Institute of Molecular Medicine, Department of Cardiovascular and Renal Research, University of Southern Denmark, Odense, Denmark (U.M.S.); Cardiovascular Disease Program, Biomedicine Discovery Institute, Department of Pharmacology, Monash University, Clayton, Victoria, Australia (R.E.W.); Department of Integrative Biomedical Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Republic of South Africa (E.D.S., L.L.); Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, Texas (T.H.); Charité – Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, Institute of Pharmacology, Cardiovascular–Metabolic–Renal (CMR) Research Center, DZHK (German Centre for Cardiovascular Research), Berlin, Germany (E.K.); CARIM – School for Cardiovascular Diseases, Maastricht University, The Netherlands (T.U.); Department of Medicinal Chemistry, Faculty of Pharmacy, Uppsala University, Uppsala, Sweden (A.H.); Division of Endocrinology and Metabolism, Department of Medicine, University of Virginia School of Medicine, Charlottesville, Virginia (R.M.C.); and Department of Physiology and Functional Genomics, University of Florida College of Medicine, Gainesville, Florida (C.S.)
Tahir Hussain
Institute of Molecular Medicine, Department of Cardiovascular and Renal Research, University of Southern Denmark, Odense, Denmark (U.M.S.); Cardiovascular Disease Program, Biomedicine Discovery Institute, Department of Pharmacology, Monash University, Clayton, Victoria, Australia (R.E.W.); Department of Integrative Biomedical Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Republic of South Africa (E.D.S., L.L.); Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, Texas (T.H.); Charité – Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, Institute of Pharmacology, Cardiovascular–Metabolic–Renal (CMR) Research Center, DZHK (German Centre for Cardiovascular Research), Berlin, Germany (E.K.); CARIM – School for Cardiovascular Diseases, Maastricht University, The Netherlands (T.U.); Department of Medicinal Chemistry, Faculty of Pharmacy, Uppsala University, Uppsala, Sweden (A.H.); Division of Endocrinology and Metabolism, Department of Medicine, University of Virginia School of Medicine, Charlottesville, Virginia (R.M.C.); and Department of Physiology and Functional Genomics, University of Florida College of Medicine, Gainesville, Florida (C.S.)
Elena Kaschina
Institute of Molecular Medicine, Department of Cardiovascular and Renal Research, University of Southern Denmark, Odense, Denmark (U.M.S.); Cardiovascular Disease Program, Biomedicine Discovery Institute, Department of Pharmacology, Monash University, Clayton, Victoria, Australia (R.E.W.); Department of Integrative Biomedical Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Republic of South Africa (E.D.S., L.L.); Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, Texas (T.H.); Charité – Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, Institute of Pharmacology, Cardiovascular–Metabolic–Renal (CMR) Research Center, DZHK (German Centre for Cardiovascular Research), Berlin, Germany (E.K.); CARIM – School for Cardiovascular Diseases, Maastricht University, The Netherlands (T.U.); Department of Medicinal Chemistry, Faculty of Pharmacy, Uppsala University, Uppsala, Sweden (A.H.); Division of Endocrinology and Metabolism, Department of Medicine, University of Virginia School of Medicine, Charlottesville, Virginia (R.M.C.); and Department of Physiology and Functional Genomics, University of Florida College of Medicine, Gainesville, Florida (C.S.)
Thomas Unger
Institute of Molecular Medicine, Department of Cardiovascular and Renal Research, University of Southern Denmark, Odense, Denmark (U.M.S.); Cardiovascular Disease Program, Biomedicine Discovery Institute, Department of Pharmacology, Monash University, Clayton, Victoria, Australia (R.E.W.); Department of Integrative Biomedical Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Republic of South Africa (E.D.S., L.L.); Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, Texas (T.H.); Charité – Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, Institute of Pharmacology, Cardiovascular–Metabolic–Renal (CMR) Research Center, DZHK (German Centre for Cardiovascular Research), Berlin, Germany (E.K.); CARIM – School for Cardiovascular Diseases, Maastricht University, The Netherlands (T.U.); Department of Medicinal Chemistry, Faculty of Pharmacy, Uppsala University, Uppsala, Sweden (A.H.); Division of Endocrinology and Metabolism, Department of Medicine, University of Virginia School of Medicine, Charlottesville, Virginia (R.M.C.); and Department of Physiology and Functional Genomics, University of Florida College of Medicine, Gainesville, Florida (C.S.)
Anders Hallberg
Institute of Molecular Medicine, Department of Cardiovascular and Renal Research, University of Southern Denmark, Odense, Denmark (U.M.S.); Cardiovascular Disease Program, Biomedicine Discovery Institute, Department of Pharmacology, Monash University, Clayton, Victoria, Australia (R.E.W.); Department of Integrative Biomedical Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Republic of South Africa (E.D.S., L.L.); Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, Texas (T.H.); Charité – Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, Institute of Pharmacology, Cardiovascular–Metabolic–Renal (CMR) Research Center, DZHK (German Centre for Cardiovascular Research), Berlin, Germany (E.K.); CARIM – School for Cardiovascular Diseases, Maastricht University, The Netherlands (T.U.); Department of Medicinal Chemistry, Faculty of Pharmacy, Uppsala University, Uppsala, Sweden (A.H.); Division of Endocrinology and Metabolism, Department of Medicine, University of Virginia School of Medicine, Charlottesville, Virginia (R.M.C.); and Department of Physiology and Functional Genomics, University of Florida College of Medicine, Gainesville, Florida (C.S.)
Robert M. Carey
Institute of Molecular Medicine, Department of Cardiovascular and Renal Research, University of Southern Denmark, Odense, Denmark (U.M.S.); Cardiovascular Disease Program, Biomedicine Discovery Institute, Department of Pharmacology, Monash University, Clayton, Victoria, Australia (R.E.W.); Department of Integrative Biomedical Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Republic of South Africa (E.D.S., L.L.); Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, Texas (T.H.); Charité – Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, Institute of Pharmacology, Cardiovascular–Metabolic–Renal (CMR) Research Center, DZHK (German Centre for Cardiovascular Research), Berlin, Germany (E.K.); CARIM – School for Cardiovascular Diseases, Maastricht University, The Netherlands (T.U.); Department of Medicinal Chemistry, Faculty of Pharmacy, Uppsala University, Uppsala, Sweden (A.H.); Division of Endocrinology and Metabolism, Department of Medicine, University of Virginia School of Medicine, Charlottesville, Virginia (R.M.C.); and Department of Physiology and Functional Genomics, University of Florida College of Medicine, Gainesville, Florida (C.S.)
Colin Sumners
Institute of Molecular Medicine, Department of Cardiovascular and Renal Research, University of Southern Denmark, Odense, Denmark (U.M.S.); Cardiovascular Disease Program, Biomedicine Discovery Institute, Department of Pharmacology, Monash University, Clayton, Victoria, Australia (R.E.W.); Department of Integrative Biomedical Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Republic of South Africa (E.D.S., L.L.); Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, Texas (T.H.); Charité – Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, Institute of Pharmacology, Cardiovascular–Metabolic–Renal (CMR) Research Center, DZHK (German Centre for Cardiovascular Research), Berlin, Germany (E.K.); CARIM – School for Cardiovascular Diseases, Maastricht University, The Netherlands (T.U.); Department of Medicinal Chemistry, Faculty of Pharmacy, Uppsala University, Uppsala, Sweden (A.H.); Division of Endocrinology and Metabolism, Department of Medicine, University of Virginia School of Medicine, Charlottesville, Virginia (R.M.C.); and Department of Physiology and Functional Genomics, University of Florida College of Medicine, Gainesville, Florida (C.S.)
Rhian Touyz
Roles: ASSOCIATE EDITOR
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In this issue
Review ArticleReview Article
Angiotensin AT2 Receptor: A Novel Therapeutic Target
U. Muscha Steckelings, Robert E. Widdop, Edward D. Sturrock, Lizelle Lubbe, Tahir Hussain, Elena Kaschina, Thomas Unger, Anders Hallberg, Robert M. Carey and Colin Sumners
Pharmacological Reviews October 1, 2022, 74 (4) 1051-1135; DOI: https://doi.org/10.1124/pharmrev.120.000281
Review ArticleReview Article
Angiotensin AT2 Receptor: A Novel Therapeutic Target
U. Muscha Steckelings, Robert E. Widdop, Edward D. Sturrock, Lizelle Lubbe, Tahir Hussain, Elena Kaschina, Thomas Unger, Anders Hallberg, Robert M. Carey and Colin Sumners
Pharmacological Reviews October 1, 2022, 74 (4) 1051-1135; DOI: https://doi.org/10.1124/pharmrev.120.000281
Jump to section
- Article
- Visual Overview
- Abstract
- I. Introduction
- II. The Classic and the Protective Renin-Angiotensin System
- III. The Angiotensin AT2-Receptor
- IV. AT2-Receptor Selective Ligands
- V. AT2-Receptor Physiology
- VI. AT2-Receptor in Disease
- VII. AT2-Receptor Agonists and Antagonists in Drug Development Programs
- VIII. Open Questions in AT2R Research
- IX. Conclusions and Future Perspectives
- Acknowledgments
- Authorship Contributions
- Footnotes
- Abbreviations
- References
- Figures & Data
- Info & Metrics
- eLetters
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