Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Mauro Mileni"'
Autor:
Shinji Nakade, Hirotaka Mizuno, Christopher B. Roth, Raymond C. Stevens, Mauro Mileni, Dora Warshaviak, Guillermo Asmar-Rovira, Caroline Rodgers, Jerold Chun, Michael A. Hanson, Gye Won Han, Rie Omi, Jeffrey Velasquez, Mark T. Griffith, Haruto Kurata, Masahiko Terakado, Yasuyuki Kihara, Jill E. Chrencik
Publikováno v:
Cell. 161(7):1633-1643
SummaryLipid biology continues to emerge as an area of significant therapeutic interest, particularly as the result of an enhanced understanding of the wealth of signaling molecules with diverse physiological properties. This growth in knowledge is e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b22edcb5a06396fd07a460c9c3437433
Autor:
Richard B. Westkaemper, F. Ivy Carroll, S. Wayne Mascarella, Bryan L. Roth, Vadim Cherezov, Aaron Thompson, Eyal Vardy, Raymond C. Stevens, Wei Liu, Philip D. Mosier, Gye Won Han, Daniel Wacker, Xi Ping Huang, Huixian Wu, Mauro Mileni, Vsevolod Katritch
Publikováno v:
Nature
Opioid receptors (ORs) mediate the actions of endogenous and exogenous opioids for many essential physiological processes including regulation of pain, respiratory drive, mood, and, in the case of κ-opioid receptors (KOR), dysphoria and psychotomime
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4131ad7998a663bbd067d8f34031405
http://europepmc.org/articles/PMC3356457
http://europepmc.org/articles/PMC3356457
Autor:
Benjamin F. Cravatt, Raymond C. Stevens, Mauro Mileni, Joie Garfunkle, Cyrine Ezzili, Dale L. Boger
Publikováno v:
Journal of the American Chemical Society. 133:4092-4100
Two cocrystal X-ray structures of the exceptionally potent α-ketoheterocycle inhibitor 1 (Ki = 290 pM) bound to a humanized variant of rat fatty acid amide hydrolase (FAAH) are disclosed, representing noncovalently and covalently bound states of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f578047f7f85a6795907ba56ea965a5
https://doi.org/10.1021/ja110877y
https://doi.org/10.1021/ja110877y
Autor:
Raymond C. Stevens, F. Scott Kimball, Cyrine Ezzili, Dale L. Boger, Benjamin F. Cravatt, Joie Garfunkle, Mauro Mileni
Publikováno v:
Journal of Medicinal Chemistry. 53:230-240
Three cocrystal X-ray structures of the alpha-ketoheterocycle inhibitors 3-5 bound to a humanized variant of fatty acid amide hydrolase (FAAH) are disclosed and comparatively discussed alongside those of 1 (OL-135) and its isomer 2. These five X-ray
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbf0fff7f9f9550f715bd1a4feec20db
https://doi.org/10.1021/jm9012196
https://doi.org/10.1021/jm9012196
Autor:
Raymond C. Stevens, Mauro Mileni, Dale L. Boger, Joie Garfunkle, Benjamin F. Cravatt, Jessica K. DeMartino
Publikováno v:
Journal of the American Chemical Society. 131:10497-10506
The cocrystal X-ray structures of two isomeric alpha-ketooxazole inhibitors (1 (OL-135) and 2) bound to fatty acid amide hydrolase (FAAH), a key enzymatic regulator of endocannabinoid signaling, are disclosed. The active site catalytic Ser241 is cova
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56c6a034c6ad048bbbfdc55f96ed855e
https://doi.org/10.1021/ja902694n
https://doi.org/10.1021/ja902694n
Autor:
Mauro Mileni, Stephen Swaney, Eranthie Weerapana, Benjamin F. Cravatt, Marya Liimatta, Michele K. McKinney, Sarah E. Smith, Lazerwith Scott E, Nalini Sadagopan, David Beidler, Cory Michael Stiff, Satwik Kamtekar, Douglas S. Johnson, Keri Van Becelaere, Keshab Bhattacharya, Yanhua Zhang, Jonathan Z. Long, Kay Ahn, Raymond C. Stevens
Publikováno v:
Chemistry & Biology. 16:411-420
SummaryEndocannabinoids are lipid signaling molecules that regulate a wide range of mammalian behaviors, including pain, inflammation, and cognitive/emotional state. The endocannabinoid anandamide is principally degraded by the integral membrane enzy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::65114ff13b68954224cbf912409fee95
https://doi.org/10.1016/j.chembiol.2009.02.013
https://doi.org/10.1016/j.chembiol.2009.02.013
Autor:
Mauro Mileni, Michael H. Bracey, Raymond C. Stevens, Joie Garfunkle, Dale L. Boger, Ian Slaymaker, Benjamin F. Cravatt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5847-5850
It has been shown that the effects of ligands on an enzyme may be observed by measuring shifts in the enzyme’s thermal stability, which may in turn have implications on inhibitor potency. Indeed, a potential correlation between thermal stability an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4df88a6259eea44a44411605a3d37b7
https://doi.org/10.1016/j.bmcl.2008.06.086
https://doi.org/10.1016/j.bmcl.2008.06.086
Autor:
Michael A. Hanson, Alexander I. Alexandrov, Raymond C. Stevens, Ellen Y.T. Chien, Mauro Mileni
Publikováno v:
Structure. 16(3):351-359
SummarySystematic efforts to understand membrane protein stability under a variety of different solution conditions are not widely available for membrane proteins, mainly due to technical problems stemming from the presence of detergents necessary to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d21671fe3bb8fec7174653502afefb5
Publikováno v:
Biochemistry. 44:16718-16728
Quinol:fumarate reductase (QFR) is the terminal enzyme of anaerobic fumarate respiration. This membrane protein complex couples the oxidation of menaquinol to menaquinone to the reduction of fumarate to succinate. Although the diheme-containing QFR f
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86bf293268c266456fde57e15add088a
https://doi.org/10.1021/bi051034s
https://doi.org/10.1021/bi051034s
Autor:
Anne Baumann, Aurora Martinez, Knut Teigen, Mauro Mileni, Raymond C. Stevens, Åge A. Skjevik, Øyvind Halskau
Publikováno v:
Journal of Molecular Biology
Tyrosine hydroxylase (TH) catalyzes the rate-limiting step in the synthesis of catecholamine neurotransmitters, and a reduction in TH activity is associated with several neurological diseases. Human TH is regulated, among other mechanisms, by Ser19-p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3deee6eb61494e4be64a78781d48d22e
https://europepmc.org/articles/PMC3872242/
https://europepmc.org/articles/PMC3872242/
