Structural insight into the catalytic mechanism and inhibitor binding of aminopeptidase A

Autor: Vincent Leroux, Catherine Llorens-Cortes, Xavier Iturrioz, Hugo De Almeida, Bernard P. Roques, Bernard Maigret, Pierre Couvineau

Publikováno v: Biochemical Journal
Biochemical Journal, Portland Press, 2020, 477 (21), pp.4133-4148. ⟨10.1042/BCJ20200307⟩
Biochemical Journal, 2020, 477 (21), pp.4133-4148. ⟨10.1042/BCJ20200307⟩

Aminopeptidase A (APA) is a membrane-bound monozinc aminopeptidase. In the brain, APA generates angiotensin III which exerts a tonic stimulatory effect on the control of blood pressure (BP) in hypertensive animals. The oral administration of RB150 re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::007af7fe0da704792b5f0f22fab28bc6
https://doi.org/10.1042/bcj20200307

Positive allosteric modulation of the mu-opioid receptor produces analgesia with reduced side effects

Autor: Kathryn E. Livingston, Shainnel O. Eans, Andrew D. White, Neil T. Burford, Jay P. McLaughlin, Bernard P. Roques, Andrew Alt, Todd M. Hillhouse, Ram Kandasamy, Minghua Li, Susan L. Ingram, Claire Meurice, Kelsey E Kochan, John R. Traynor

Publikováno v: Proc Natl Acad Sci U S A
Proceedings of the National Academy of Sciences of the United States of America
Proceedings of the National Academy of Sciences of the United States of America, National Academy of Sciences, 2021, 118 (16), pp.e2000017118. ⟨10.1073/pnas.2000017118⟩

International audience; Positive allosteric modulators (PAMs) of the mu-opioid receptor (MOR) have been hypothesized as potentially safer analgesics than traditional opioid drugs. This is based on the idea that PAMs will promote the action of endogen

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::592cc679812be187baac01d7115fa3bf
https://europepmc.org/articles/PMC8072371/

P4481NI956/QGC006, a potent orally active, brain-penetrating aminopeptidase A inhibitor prodrug for treating hypertension

Autor: Delphine Compere, Mathilde Keck, Fabrice Balavoine, Bernard P. Roques, Catherine Llorens-Cortes, Adrien Flahault, Nicolas Inguimbert, H De Almeida

Publikováno v: European Heart Journal. 40

Background Brain renin-angiotensin system hyperactivity has been implicated in the development and maintenance of hypertension. We previously showed that aminopeptidase A (APA) generates in the brain, angiotensin III, which exerts a tonic stimulatory

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::893d9d320838eb0a86561be3bd830ef2
https://doi.org/10.1093/eurheartj/ehz745.0875

NI956/QGC006, a Potent Orally Active, Brain-Penetrating Aminopeptidase A Inhibitor for Treating Hypertension

Autor: Catherine Llorens-Cortes, Mathilde Keck, Adrien Flahault, Fabrice Balavoine, Nicolas Inguimbert, Bernard P. Roques, Hugo De Almeida, Delphine Compere

Publikováno v: Hypertension
Hypertension, American Heart Association, 2019, 73 (6), pp.1300-1307. ⟨10.1161/HYPERTENSIONAHA.118.12499⟩

Brain renin-angiotensin system hyperactivity has been implicated in the development and maintenance of hypertension. We have shown that aminopeptidase A is involved in the formation of brain angiotensin III, which exerts tonic stimulatory control ove

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38c31fdc20118fa9e2aec051729422c7
https://hal.archives-ouvertes.fr/hal-02265480

Obligatory Metabolism of Angiotensin II to Angiotensin III for Zona Glomerulosa Cell-Mediated Relaxations of Bovine Adrenal Cortical Arteries

Autor: Phillip G. Kopf, Anja Herrnreiter, Christian Krause, Bernard P. Roques, William B. Campbell, Sang-Kyu Park

Publikováno v: Endocrinology
Endocrinology, 2018, 159 (1), pp.238-247. ⟨10.1210/en.2017-00759⟩
Endocrinology, Oxford University Press, 2018, 159 (1), pp.238-247. ⟨10.1210/en.2017-00759⟩

International audience; Hyperaldosteronism is associated with hypertension, cardiac hypertrophy, and congestive heart failure. Steroidogenic factors facilitate aldosterone secretion by increasing adrenal blood flow. Angiotensin (Ang) II decreases adr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b55fc5a3e860e73f0893ae8030cbbdf
https://hal-cnrs.archives-ouvertes.fr/hal-03292703