Identification of phenothiazine derivatives as UHM-binding inhibitors of early spliceosome assembly

Autor: Pravin Kumar Ankush Jagtap, Tomáš Kubelka, Komal Soni, Cindy L. Will, Divita Garg, Claudia Sippel, Tobias G. Kapp, Harish Kumar Potukuchi, Kenji Schorpp, Kamyar Hadian, Horst Kessler, Reinhard Lührmann, Felix Hausch, Thorsten Bach, Michael Sattler

Publikováno v: Nature Communications, Vol 11, Iss 1, Pp 1-11 (2020)

So far only a few compounds have been reported as splicing modulators. Here, the authors combine high-throughput screening, chemical synthesis, NMR, X-ray crystallography with functional studies and develop phenothiazines as inhibitors for the U2AF H

Externí odkaz: https://doaj.org/article/816cddccf4d4425e993bdca998fb63bd

Selective Targeting of Integrin αvβ8 by a Highly Active Cyclic Peptide

Autor: Markus Schwaiger, Katja Steiger, Luciana Marinelli, Markus Nieberler, Johannes Notni, Horst Kessler, Salvatore Di Maro, Michael Weinmüller, Francesco Saverio Di Leva, Oleg V. Maltsev, Hans-Jürgen Wester, Ute Reuning, Alexander Wurzer, Udaya Kiran Marelli, Roswitha Beck, Andreas F. B. Räder, Florian Reichart, Tobias G. Kapp

Publikováno v: Journal of Medicinal Chemistry. 62:2024-2037

Integrins play important roles in physiological and pathophysiological processes. Among the RGD-recognizing integrin subtypes, the αvβ8 receptor is emerging as an attractive target because of its involvement in various illnesses, such as autoimmune

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57f17db6403be53764217b3bb753a783
https://doi.org/10.1021/acs.jmedchem.8b01588

In Vivo PET Imaging of the Cancer Integrin αvβ6 Using 68Ga-Labeled Cyclic RGD Nonapeptides

Autor: Johannes Notni, Frauke Hoffmann, Irene Esposito, Tobias G. Kapp, Hans-Jürgen Wester, Dominik Reich, Wilko Weichert, Horst Kessler, Oleg V. Maltsev, Katja Steiger

Publikováno v: Journal of Nuclear Medicine. 58:671-677

Expression of the cellular transmembrane receptor αvβ6 integrin is essentially restricted to malignant epithelial cells in carcinomas of a broad variety of lineages, whereas it is virtually absent in normal adult tissues. Thus, it is a highly attra

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::087389bdd47f0ae34a85afa102362f7f
https://doi.org/10.2967/jnumed.116.182824

Identification of phenothiazine derivatives as UHM-binding inhibitors of early spliceosome assembly

Autor: Felix Hausch, Tobias G. Kapp, Komal Soni, Michael Sattler, Horst Kessler, Kenji Schorpp, Cindy L. Will, Divita Garg, Reinhard Lührmann, Thorsten Bach, Claudia Sippel, Kamyar Hadian, Pravin Kumar Ankush Jagtap, Harish K. Potukuchi, Tomáš Kubelka

Publikováno v: Nature Communications, Vol 11, Iss 1, Pp 1-11 (2020)
Nature Communications
'Nature Communications ', vol: 11, pages: 5621-1-5621-11 (2020)
Nat. Commun. 11:5621 (2020)

Interactions between U2AF homology motifs (UHMs) and U2AF ligand motifs (ULMs) play a crucial role in early spliceosome assembly in eukaryotic gene regulation. UHM-ULM interactions mediate heterodimerization of the constitutive splicing factors U2AF6

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b7c7bf8fe0cab2d397f14b562196e6e
https://mediatum.ub.tum.de/doc/1601975/document.pdf

Rational Design of Cyclic Peptide Inhibitors of U2AF Homology Motif (UHM) Domains To Modulate Pre-mRNA Splicing

Autor: Oliver Demmer, Michael Sattler, Cindy L. Will, Tobias G. Kapp, Reinhard Lührmann, Divita Garg, Horst Kessler, Pravin Kumar Ankush Jagtap

Publikováno v: Europe PubMed Central
Journal of Medicinal Chemistry
J. Med. Chem. 59, 10190-10197 (2016)

U2AF homology motifs (UHMs) are atypical RNA recognition motif domains that mediate critical protein-protein interactions during the regulation of alternative pre-mRNA splicing and other processes. The recognition of UHM domains by UHM ligand motif (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::268e7cef31b0415bcd95c01155eded1f
https://doi.org/10.1021/acs.jmedchem.6b01118