Zobrazeno 1 - 10
of 25
pro vyhledávání: '"David Madge"'
Autor:
Alan S. Futran, Tao Lu, Katherine Amberg-Johnson, Jiayi Xu, Xiaoxiao Yang, Saidi He, Sarah Boyce, Jeffrey A. Bell, Robert Pelletier, Takao Suzuki, Xianhai Huang, Heng Qian, Liping Fang, Li Xing, Zhaowu Xu, Stephen E. Kurtz, Jeffrey W. Tyner, Wayne Tang, Tao Guo, Karen Akinsanya, David Madge, Kristian K. Jensen
Publikováno v:
iScience, Vol 27, Iss 5, Pp 109693- (2024)
Summary: The USP7 deubiquitinase regulates proteins involved in the cell cycle, DNA repair, and epigenetics and has been implicated in cancer progression. USP7 inhibition has been pursued for the development of anti-cancer therapies. Here, we describ
Externí odkaz:
https://doaj.org/article/ad0bc59a163a477bae0474b6a3ff6a2d
Autor:
Steve Peigneur, Aleš Žula, Nace Zidar, Fiona Chan-Porter, Robert Kirby, David Madge, Janez Ilaš, Danijel Kikelj, Jan Tytgat
Publikováno v:
Marine Drugs, Vol 12, Iss 4, Pp 2132-2143 (2014)
Clathrodin is a marine alkaloid and believed to be a modulator of voltage-gated sodium (NaV) channels. Since there is an urgent need for small molecule NaV channel ligands as novel therapeutics, clathrodin could represent an interesting lead compound
Externí odkaz:
https://doaj.org/article/ae4d9687a1d8427f8427040fc63d88ca
Autor:
Yan A. Ivanenkov, Alex Zhavoronkov, Mark S. Veselov, Rim Shayakhmetov, Anastasiya V Aladinskaya, Daniil Polykovskiy, Victor A Terentiev, Vladimir A. Aladinskiy, Bogdan A Zagribelnyy, Tao Guo, Artem Zholus, Yury Volkov, Alexander Zhebrak, Lennart H Lee, Li Xing, Lidiya I Minaeva, Richard Soll, Alán Aspuru-Guzik, Alexander Aliper, David Madge, Maksim Kuznetsov, Arip Asadulaev
Publikováno v:
Nature Biotechnology. 37:1038-1040
We have developed a deep generative model, generative tensorial reinforcement learning (GENTRL), for de novo small-molecule design. GENTRL optimizes synthetic feasibility, novelty, and biological activity. We used GENTRL to discover potent inhibitors
Autor:
Liping Fang, Takao Suzuki, Kristian Jensen, Mats A. Svensson, Robert Pelleltier, Jeffrey A. Bell, Zef Konst, Hamish Wright, Wayne Tang, Katherine Amberg-Johnson, Shuping Xu, Xianhai Huang, Karen Dingley, Yan Zhang, Heng Qian, Markus K. Dahlgren, Michael Trzoss, Alan Futran, Karen Akinsanya, Xiaoxiao Yang, Sarah Boyce, Saidi He, Li Xing, Jiayi Xu, Tao Guo, David Madge, Tao Lu, Heidi Koldsoe, Fang-Yu Lin, Zhaowu Xu, Jie Xu, Engin Yapici
Publikováno v:
Cancer Research. 81:1338-1338
Introduction: Ubiquitin-specific protease 7 (USP7) is a deubiquitinase that regulates several proteins involved in cell cycle, DNA repair, genomic stability, and epigenetics and has been implicated in cancer progression. A key substrate of USP7 is MD
Autor:
Fiona Chan, Steve Peigneur, Robert W. Kirby, David Madge, Marko Jukič, Rok Frlan, Jan Tytgat, Marko Anderluh, Danijel Kikelj
Publikováno v:
Medicinal Chemistry Research. 24:2366-2380
Sponges of the genus Agelas produce compounds that modulate the activity of voltage-gated sodium ion channels and contribute novel scaffolds for the development of compounds with activity against a plethora of biological targets. In particular, clath
Autor:
Muneto Mogi, Yuka Ikegami, Klaus Urbahns, Masaomi Tajimi, Takeshi Yura, Marumo Makiko, David Madge, Noriyuki Yamamoto, Kayo Yasoshima, Tsutomu Masuda, Jang Bahadur Gupta, Nagahiro Yoshida, Fiona Chan, Hiroshi Fujishima, Toshiya Moriwaki
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3408-3411
Starting from a naphthol-based lead series with low oral bioavailability, we have identified potent TRPV1 antagonists with oral bioavailability in rats. These compounds emerged from SAR studies aimed at replacing the lead's phenol structure whilst ma
Autor:
Toshiya Moriwaki, Heinrich Meier, Muneto Mogi, Klaus Urbahns, Takeshi Yura, Nagahiro Yoshida, Timothy B. Lowinger, Hiroshi Fujishima, Masaomi Tajimi, Fiona Chan, Jang Bahadur Gupta, Tsutomu Masuda, David Madge
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3354-3357
We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has re
Publikováno v:
International Journal of Impotence Research. 16:479-485
We compared the effects of a nitric oxide (NO)-releasing sildenafil (NCX-911), NO-independent soluble guanylate cyclase activator (BAY41-2272) and sildenafil on the anococcygeus muscle from streptozotocin-induced 16-weeks diabetic rats. NCX-911, BAY4
Autor:
Zoltan Kaposzta, Paul A. Baskerville, David Madge, Simon Fraser, John F. Martin, Hugh S. Markus
Publikováno v:
Circulation. 103:2371-2375
Background — l -Arginine reduces platelet aggregation and adhesion in ex vivo studies, but there is no evidence as yet that it has a therapeutic effect on clinical end points. Doppler ultrasound can detect cerebral emboli noninvasively. Such emboli
Publikováno v:
Bioorganic & Medicinal Chemistry. 9:1337-1343
There is currently interest in the metabolism of the various compounds which make up the vitamin E family, especially with regards to the possible use of vitamin E metabolites as markers of oxidative stress and adequate vitamin E supply. A number of