Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Philipp Lehr"'
Autor:
Ulrich Hommel, Konstanze Hurth, Jean-Michel Rondeau, Anna Vulpetti, Daniela Ostermeier, Andreas Boettcher, Jacob Peter Brady, Michael Hediger, Sylvie Lehmann, Elke Koch, Anke Blechschmidt, Rina Yamamoto, Valentina Tundo Dottorello, Sandra Haenni-Holzinger, Christian Kaiser, Philipp Lehr, Andreas Lingel, Luca Mureddu, Christian Schleberger, Jutta Blank, Paul Ramage, Felix Freuler, Joerg Eder, Frédéric Bornancin
Publikováno v:
Nature Communications, Vol 14, Iss 1, Pp 1-13 (2023)
Abstract Human interleukin-1β (hIL-1β) is a pro-inflammatory cytokine involved in many diseases. While hIL-1β directed antibodies have shown clinical benefit, an orally available low-molecular weight antagonist is still elusive, limiting the appli
Externí odkaz:
https://doaj.org/article/045a20bdd9464a2d8a11a51d75b0961e
Autor:
Patricia A. Horton, Daniel Baird, Philipp Lehr, Amitabh V. Nimonkar, Rose Cubbon, Flyer Alec, Timothy E. Benson, Peter Meier, Chun-Hao Chiu, John Trauger, William R. Tschantz, Chunhua Wang, Aleksandar Stojanovic, Thomas M. Smith, Rishi Arora, Stephen Craig Weldon, Pramod Pandey, Reto Brunner, Michael J. Romanowski, Susan Hanrahan, Andrei Igorevich Voznesensky, Sascha Mueller, Johannes Ottl
Lipoprotein lipase (LPL) plays a central role in triglyceride (TG) metabolism. By catalyzing the hydrolysis of TGs present in TG-rich lipoproteins (TRLs), LPL facilitates TG utilization and regulates circulating TG and TRL concentrations. Until very
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b53ee6ab3c252db213aa83a6100d0fcf
https://europepmc.org/articles/PMC6534989/
https://europepmc.org/articles/PMC6534989/
Publikováno v:
Journal of Medicinal Chemistry. 45:4310-4320
Steroid sulfatase (STS) has emerged as a highly attractive target for the therapy of a number of disorders. Starting with the known inhibitor estrone sulfamate (1) as lead compound and with the finding that steroid sulfamates containing a nonaromatic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22f962d053ca0827a7d2f0a6b80dab90
https://doi.org/10.1021/jm020878w
https://doi.org/10.1021/jm020878w
Publikováno v:
The Journal of Steroid Biochemistry and Molecular Biology. 73:225-235
Steroid sulfatase (STS) regulates the formation of active steroids from systemic precursors, such as estrone sulfate and dehydroepiandrosterone sulfate (DHEAS). In breast tissues, this pathway is a source for local production of estrogens, which supp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47d62abe2e90b2745fd01f0ad8c0ed11
https://doi.org/10.1016/s0960-0760(00)00077-7
https://doi.org/10.1016/s0960-0760(00)00077-7
Autor:
Dieter Scholz, H. Gstach, Philipp Lehr, P. Peichl, B. Rosenwirth, A. Billich, Brigitte Charpiot
Publikováno v:
Antiviral Chemistry and Chemotherapy. 6:327-336
In order to design HIV proteinase inhibitors which combine antiviral potency in HIV-infected cells with good oral bioavailability, new derivatives of 2-aminobenzylstatine containing HIV-1 proteinase inhibitors were synthesized. Compounds showing the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8479d463d91feee21096f33714ec7656
https://doi.org/10.1177/095632029500600507
https://doi.org/10.1177/095632029500600507
Autor:
Andreas Billich, Brigitte Rosenwirth, Dieter Scholz, Philipp Lehr, Brigitte Charpiot, Gert Fricker, Peter Peichl, Hubert Gstach
Publikováno v:
Antiviral Research. 25:215-233
Derivation of the 2-aminobenzylstatine containing HIV-1 proteinase (PR) inhibitor I led to a series of compounds with considerably improved antiviral activity, the most potent derivatives inhibiting HIV-1 with IC50 values below 25 nM. This was achiev
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66497f93574e81a87c79d4b794148326
https://doi.org/10.1016/0166-3542(94)90005-1
https://doi.org/10.1016/0166-3542(94)90005-1
Autor:
Brigitte Rosenwirth, Hubert Gstach, Erwin P. Schreiner, Brigitte Charpiot, Peter Ettmayer, Philipp Lehr, Dieter Scholz, Andreas Billich
Publikováno v:
Journal of Medicinal Chemistry. 37:3079-3089
A convenient procedure for the synthesis of 2-heterosubstituted statine derivatives as novel building blocks in HIV-protease inhibitors has been developed. The synthesis starts with protected L-phenylalaninols, which were converted to gamma-amino alp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6305c14abbc50167dd6355fd811c1414
https://doi.org/10.1021/jm00045a013
https://doi.org/10.1021/jm00045a013
Autor:
Andreas Billich, Philipp Lehr, Hubert Gstach, Alexander Aziz, Brigitte Charpiot, Dieter Scholz
Publikováno v:
Journal of Enzyme Inhibition. 7:213-224
Kinetic and binding studies on a novel type of potent inhibitors of HIV-1 proteinase containing a 2-aminobenzyl substituted statine moiety as dipeptide mimetic are reported. The compounds were characterized as fast-binding competitive inhibitors of t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f41883b445cfae91f7b28538d87e767b
https://doi.org/10.3109/14756369309040764
https://doi.org/10.3109/14756369309040764
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(4)
Steroid sulfatase (STS) is an attractive target for a range of oestrogen- and androgen-dependent diseases. In search of novel chemotypes of STS inhibitors, we had previously identified nortropinyl–arylsulfonylureas 1; however, while these compounds
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9367b23732519ca665e450f093a394d1
https://pubmed.ncbi.nlm.nih.gov/15686949
https://pubmed.ncbi.nlm.nih.gov/15686949
Autor:
Andreas Billich, Dieter Geyl, Peter Nussbaumer, Philipp Lehr, Amarylla Horvath, Barbara Wolff
Publikováno v:
ChemInform. 35
Steroid sulfatase (STS) has emerged as an attractive target for a range of estrogen- and androgen-dependent diseases. Searching for novel chemotypes as STS inhibitors, we identified nortropinyl-arylsulfonylurea 3 as a hit from high-throughput screeni
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::371a6d2d43a07488fa47ef648b87e2b6
https://doi.org/10.1002/chin.200405119
https://doi.org/10.1002/chin.200405119