Zobrazeno 1 - 10
of 34
pro vyhledávání: '"Polo C-H. Lam"'
Autor:
James M. Mutunga, Qiao-Hong Chen, Dawn M. Wong, Polo C-H. Lam, Jianyong Li, Maxim M. Totrov, Aaron D. Gross, Paul R. Carlier, Jeffrey R. Bloomquist
Publikováno v:
CHIMIA, Vol 70, Iss 10 (2016)
Widespread pyrethroid resistance has caused an urgent need to develop new insecticides for control of the malaria mosquito, Anopheles gambiae. Insecticide discovery efforts were directed towards the construction of bivalent inhibitors that occupy bot
Externí odkaz:
https://doaj.org/article/304d974ecc6945a8af3bfffb6f19d76b
Autor:
Denise Wootten, Patrick M. Sexton, Laurence J. Miller, Ingrid Mechin, Anil Nair, Andrew Orry, Ruben Abagyan, Karthigeyan Nagarajan, Polo C.-H. Lam, Aditya J. Desai, Celine Valant, Arthur Christopoulos
Publikováno v:
Molecular Pharmacology. 95:245-259
Allosteric modulation of receptors provides mechanistic safety while effectively achieving biologic endpoints otherwise difficult or impossible to obtain by other means. The theoretical case has been made for the development of a positive allosteric
Autor:
Dawn M Wong, Jianyong Li, Qiao-Hong Chen, Qian Han, James M Mutunga, Ania Wysinski, Troy D Anderson, Haizhen Ding, Tiffany L Carpenetti, Astha Verma, Rafique Islam, Sally L Paulson, Polo C-H Lam, Maxim Totrov, Jeffrey R Bloomquist, Paul R Carlier
Publikováno v:
PLoS ONE, Vol 7, Iss 10, p e46712 (2012)
Acetylcholinesterase (AChE) is a proven target for control of the malaria mosquito (Anopheles gambiae). Unfortunately, a single amino acid mutation (G119S) in An. gambiae AChE-1 (AgAChE) confers resistance to the AChE inhibitors currently approved by
Externí odkaz:
https://doaj.org/article/5787d6ace9ba45baa6e7309d3a591b29
Crystal structure of acetylcholinesterase catalytic subunits of the malaria vector Anopheles gambiae
Autor:
Paul R. Carlier, Polo C.-H. Lam, Maxim Totrov, Dawn M. Wong, Howard Robinson, Qian Han, Haizhen Ding, Jianyong Li
Publikováno v:
Insect Science. 25:721-724
Autor:
Polo C.-H. Lam, Erin E. Cawston, Ruben Abagyan, Arthur Christopoulos, Brad R. Henke, Achyut Patil, Andrew Orry, Kaleeckal G. Harikumar, Laurence J. Miller, Patrick M. Sexton
Publikováno v:
Journal of Biological Chemistry. 288:21082-21095
Understanding the molecular basis of drug action can facilitate development of more potent and selective drugs. Here, we explore the molecular basis for action of a unique small molecule ligand that is a type 1 cholecystokinin (CCK) receptor agonist
Autor:
Kevin B. Temeyer, Jeffrey R. Bloomquist, Fan Tong, Adalberto A. Pérez de León, Polo C-H. Lam, Daniel R. Swale, Paul R. Carlier, Maxim Totrov, Andrew Y. Li
Publikováno v:
Pesticide Biochemistry and Physiology. 106:85-92
The cattle tick, Rhipicephalus (Boophilus) microplus (Bm), and the sand fly, Phlebotomus papatasi (Pp), are disease vectors to cattle and humans, respectively. The purpose of this study was to characterize the inhibitor profile of acetylcholinesteras
Autor:
James M. Mutunga, Dhana Raj Boina, Jeffrey R. Bloomquist, Troy D. Anderson, Paul R. Carlier, Polo C.-H. Lam, Maxim Totrov, Dawn M. Wong
Publikováno v:
Archives of Insect Biochemistry and Physiology. 83:180-194
A series of bis(n)-tacrines were used as pharmacological probes of the acetylcholinesterase (AChE) catalytic and peripheral sites of Blattella germanica and Drosophila melanogaster, which express AChE-1 and AChE-2 isoforms, respectively. In general,
Autor:
Maxim Totrov, Dawn M. Wong, Qiao-Hong Chen, Jianyong Li, Polo C-H. Lam, Paul R. Carlier, James M. Mutunga, Jeffrey R. Bloomquist, Aaron D. Gross
Publikováno v:
CHIMIA, Vol 70, Iss 10 (2016)
Widespread pyrethroid resistance has caused an urgent need to develop new insecticides for control of the malaria mosquito, Anopheles gambiae. Insecticide discovery efforts were directed towards the construction of bivalent inhibitors that occupy bot
Autor:
Patrick M. Sexton, Andrew Orry, Laurence J. Miller, Polo C.-H. Lam, Ruben Abagyan, Maoqing Dong, Arthur Christopoulos
Publikováno v:
The Journal of biological chemistry, vol 291, iss 10
Amino-terminal regions of secretin-family peptides contain key determinants for biological activity and binding specificity, although the nature of interactions with receptors is unclear. A helix N-capping motif within this region has been postulated
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9342d62d935f94dae62ad922b0385583
https://escholarship.org/uc/item/86g3x66n
https://escholarship.org/uc/item/86g3x66n
Autor:
Polo C.-H. Lam, Jeffrey R. Bloomquist, Joshua A. Hartsel, Jianyong Li, Paul R. Carlier, Sally L. Paulson, Eric A. Wong, Rafique Islam, Ming Ma, Maxim Totrov, Dawn M. Wong, Troy D. Anderson, James M. Mutunga, Ania Wysinski
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4593-4598
To identify potential human-safe insecticides against the malaria mosquito we undertook an investigation of the structure–activity relationship of aryl methylcarbamates inhibitors of acetylcholinesterase (AChE). Compounds bearing a β-branched 2-al