Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Othman Benchama"'
Autor:
Othman Benchama, Michael S. Malamas, Kulkarni Praveen, Elizabeth C. Ethier, Mark K. Williams, Alexandros Makriyannis, Hava Karsenty Avraham
Publikováno v:
Scientific Reports, Vol 12, Iss 1, Pp 1-16 (2022)
Abstract Triple-negative breast cancer (TNBC) is associated with high mortality due to the high expression of pro-inflammatory cytokines and lack of targeted therapies. N-acylethanolamine acid amidase (NAAA) is an N-terminal cysteine hydrolase that p
Externí odkaz:
https://doaj.org/article/b03de5caa7dd4eb78cf5de132132549f
Autor:
Othman Benchama, Sergiy Tyukhtenko, Michael S. Malamas, Mark K. Williams, Alexandros Makriyannis, Hava Karsenty Avraham
Publikováno v:
Scientific Reports, Vol 12, Iss 1, Pp 1-14 (2022)
Abstract While the prevalence of breast cancer metastasis in the brain is significantly higher in triple negative breast cancers (TNBCs), there is a lack of novel and/or improved therapies for these patients. Monoacylglycerol lipase (MAGL) is a hydro
Externí odkaz:
https://doaj.org/article/bea36e2b30f7478091279c778012b3d2
Autor:
Shakiru O. Alapafuja, Spyros P. Nikas, Thanh C. Ho, Fei Tong, Othman Benchama, Alexandros Makriyannis
Publikováno v:
Molecules, Vol 24, Iss 19, p 3559 (2019)
In earlier work, we reported a novel class of CB2 selective ligands namely cannabilactones. These compounds carry a dimethylheptyl substituent at C3, which is typical for synthetic cannabinoids. In the current study with the focus on the pharmacophor
Externí odkaz:
https://doaj.org/article/b37a6c912e6e42a0961b41d3f816acb9
Autor:
Michael S. Malamas, Sergiy Tyukhtenko, Mark K. Williams, Othman Benchama, Hava Avraham, Alexandros Makriyannis
While the prevalence of breast cancer metastasis in the brain is significantly higher in triple negative breast cancers (TNBCs), there is a lack of novel and/or improved therapies for these patients. Monoacylglycerol lipase (MAGL) is a hydrolase invo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5c190a1c5f3143b253c0cb99f5f24651
https://doi.org/10.21203/rs.3.rs-1072053/v1
https://doi.org/10.21203/rs.3.rs-1072053/v1
Autor:
Xiaoyu Ma, Srikrishnan Mallipeddi, Michael S. Malamas, Han Zhou, Alexandros Makriyannis, Chandrashekhar Honrao, Othman Benchama, JodiAnne T. Wood, Jimit Girish Raghav
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:4963-4970
New oximes short-acting CB1 agonists were explored by the introduction of an internal oxime and polar groups at the C3 alkyl tail of Δ8-THC. The scope of the research was to drastically alter two important physicochemical properties hydrophobicity (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca1b6844b78d2c1075e54bc8f7133537
https://doi.org/10.1016/j.bmc.2018.08.003
https://doi.org/10.1016/j.bmc.2018.08.003
Autor:
Nikolai Zvonok, Ken Mackie, Han Zhou, Spyros P. Nikas, Demetris P. Papahatjis, Andrea G. Hohmann, JodiAnne T. Wood, Shu Xu, Simiao Wu, Lipin Ji, Patricia H. Reggio, Marsha R. Eno, Lawrence J. Marnett, Khadijah A. Mohammad, Paula Morales, Yingpeng Liu, Ai-Ling Li, Dow P. Hurst, Shalley N. Kudalkar, Alexandros Makriyannis, Chandrashekhar Honrao, Othman Benchama, Marion Schimpgen
Publikováno v:
Journal of Medicinal Chemistry. 61:8639-8657
The synthesis of potent metabolically stable endocannabinoids is challenging. Here we report a chiral arachidonoyl ethanolamide (AEA) analogue, namely, (13S,1′R)-dimethylanandamide (AMG315, 3a), a high affinity ligand for the CB1 receptor (Ki of 7.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::41a1b3b68c754e7acf2b4084786b9971
https://doi.org/10.1021/acs.jmedchem.8b00611
https://doi.org/10.1021/acs.jmedchem.8b00611
Autor:
Jimit Girish Raghav, Othman Benchama, Alexandros Makriyannis, Srikrishnan Mallipeddi, Michael Z. Leonard, Rishi Sharma, Chandrashekhar Honrao, Bin Zhang, Shashank Kulkarni, Shan Jiang, Carol A. Paronis, Jack Bergman, Spyros P. Nikas, Torbjörn U. C. Järbe
Publikováno v:
Journal of Medicinal Chemistry. 59:6903-6919
In pursuit of safer controlled-deactivation cannabinoids with high potency and short duration of action, we report the design, synthesis, and pharmacological evaluation of novel C9- and C11-hydroxy-substituted hexahydrocannabinol (HHC) and tetrahydro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ad3e3d2eb9ab2c1c2ea5f178a949a4d5
https://doi.org/10.1021/acs.jmedchem.6b00717
https://doi.org/10.1021/acs.jmedchem.6b00717
Autor:
Othman Benchama, Yiran Wu, Edward L. Stahl, Xiaoting Li, Qianqian Sun, Christos Iliopoulos-Tsoutsouvas, Shuguang Yuan, Xiyong Song, Suwen Zhao, Yuxia Wang, Nikolai Zvonok, Laura M. Bohn, Lijie Wu, Ling Shen, Christina A. Johnston, Travis W. Grim, Zhi-Jie Liu, Tian Hua, Shan Jiang, Meng Wu, Spyros P. Nikas, Alexandros Makriyannis, Feng Song
Publikováno v:
Cell. 180:655-665.e18
Human endocannabinoid systems modulate multiple physiological processes mainly through the activation of cannabinoid receptors CB1 and CB2. Their high sequence similarity, low agonist selectivity, and lack of activation and G protein-coupling knowled
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2309b56f47c33737635a53af989cf9b6
https://doi.org/10.1016/j.cell.2020.01.008
https://doi.org/10.1016/j.cell.2020.01.008
Autor:
Jay A. A. West, Nikolai Zvonok, Catherine M. Rawlins, Dimitrios N. Pelekoudas, Jeffrey N. Agar, Michael S. Malamas, Alexandros Makriyannis, Spiro Pavlopoulos, Othman Benchama
Publikováno v:
Protein expression and purification. 145
N-acylethanolamine acid amidase (NAAA) is an N-terminal nucleophile (Ntn) enzyme with a catalytic cysteine residue that has highest activity at acidic pH. The most prominent substrate hydrolyzed is palmitoylethanolamine (PEA), which regulates inflamm
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1bc31ffb47c46a9228798fb9b4e3c194
https://pubmed.ncbi.nlm.nih.gov/29253688
https://pubmed.ncbi.nlm.nih.gov/29253688