Small Molecule CD38 Inhibitors: Synthesis of 8-Amino-N1-inosine 5′-monophosphate, Analogues and Early Structure-Activity Relationship

Autor: Joanna M. Watt, Richard Graeff, Barry V. L. Potter

Publikováno v: Molecules, Vol 26, Iss 23, p 7165 (2021)

Although a monoclonal antibody targeting the multifunctional ectoenzyme CD38 is an FDA-approved drug, few small molecule inhibitors exist for this enzyme that catalyzes inter alia the formation and metabolism of the N1-ribosylated, Ca2+-mobilizing, s

Externí odkaz: https://doaj.org/article/a4b277117732405ca369cdbf4afde384

Small Molecule CD38 Inhibitors: Synthesis of 8-Amino-N1-inosine 5′-monophosphate, Analogues and Early Structure-Activity Relationship

Autor: Richard M. Graeff, Joanna M. Watt, Barry V. L. Potter

Publikováno v: Molecules; Volume 26; Issue 23; Pages: 7165
Watt, J M, Graeff, R & Potter, B V L 2021, ' Small Molecule CD38 Inhibitors: Synthesis of 8-Amino-N1-Inosine 5'-Monophosphate, Analogues and Early Structure-Activity Relationship ', Molecules, vol. 26, no. 23, 7165 . https://doi.org/10.3390/molecules26237165
Molecules, Vol 26, Iss 7165, p 7165 (2021)

Although a monoclonal antibody targeting the multifunctional ectoenzyme CD38 is an FDA-approved drug, few small molecule inhibitors exist for this enzyme that catalyzes inter alia the formation and metabolism of the N1-ribosylated, Ca2+-mobilizing, s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a73339c8c5d1340c4e586553c81a16e

Ligand-induced activation of human TRPM2 requires the terminal ribose of ADPR and involves Arg1433 and Tyr1349

Autor: Wiebke Sick, Angelika Harneit, Andrea C. Araujo, Ralf Fliegert, Monika D. Rozewitz, Anja Schöbel, Tanja Kirchberger, Joanna M. Watt, Mark P. Thomas, Andreas H. Guse, Barry V. L. Potter, Christelle Moreau

Publikováno v: Biochemical Journal

TRPM2 (transient receptor potential channel, subfamily melastatin, member 2) is a Ca2+-permeable non-selective cation channel activated by the binding of adenosine 5′-diphosphoribose (ADPR) to its cytoplasmic NUDT9H domain (NUDT9 homology domain).

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e149b107746fd09de4ed57b19cf45fbb
https://doi.org/10.1042/bcj20170091

Different substrate specificities of the two ADPR binding sites in TRPM2 channels of Nematostella vectensis and the role of IDPR

Autor: Frank J. P. Kühn, Andreas Lückhoff, Barry V. L. Potter, Joanna M. Watt

Publikováno v: Scientific Reports
Scientific Reports, Vol 9, Iss 1, Pp 1-12 (2019)

NvTRPM2 (Nematostella vectensis Transient Receptor Potential Melastatin 2), the species variant of the human apoptosis-related cation channel hTRPM2, is gated by ADP-ribose (ADPR) independently of the C-terminal NUDT9H domain that mediates ADPR-direc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3cdec66ae6c4b5b59275bd9092aa83c
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Context-dependent calcium signaling in encephalitogenic T cells – an in vivo two-photon imaging study

Autor: Stephanie Everts, Nikolaos I. Kyratsous, Ingo Bartholomäus, Guokun Zhang, Marija Pesic, Joanna M. Watt, Naoto Kawakami, Miriam Wörner, Ping Fang, Reinhard Hohlfeld, H. Wekerle, Marsilius Mues, Joachim W. Ellwart, Isabel J. Bauer, Barry V. L. Potter

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America
Proc. Natl. Acad. Sci. U.S.A. 114, E6381-E6389 (2017)

In experimental autoimmune encephalitis (EAE), autoimmune T cells are activated in the periphery before they home to the CNS. On their way, the T cells pass through a series of different cellular milieus where they receive signals that instruct them

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3b476f2bc673a22acb3cea6e6db102b
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