Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.
Publication
, Journal Article
Lau, CK; Bayly, CI; Gauthier, JY; Li, CS; Therien, M; Asante-Appiah, E; Cromlish, W; Boie, Y; Forghani, F; Desmarais, S; Wang, Q; Skorey, K ...
Published in: Bioorganic & medicinal chemistry letters
February 2004
A series of benzotriazole phenyldifluoromethylphosphonic acids were found to be potent PTP-1B inhibitors. Molecular modeling on the X-ray crystal structure of the lead structure led to the design of potent PTP-1B inhibitors that show moderate selectivity against TC-PTP, a very closely related protein tyrosine phosphatase.
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Published In
Bioorganic & medicinal chemistry letters
DOI
EISSN
1464-3405
ISSN
0960-894X
Publication Date
February 2004
Volume
14
Issue
4
Start / End Page
1043 / 1048
Related Subject Headings
- Structure-Activity Relationship
- Protein Tyrosine Phosphatases
- Protein Tyrosine Phosphatase, Non-Receptor Type 1
- Organophosphorus Compounds
- Molecular Structure
- Models, Molecular
- Mice, Knockout
- Mice
- Medicinal & Biomolecular Chemistry
- Insecta
Citation
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Lau, C. K., Bayly, C. I., Gauthier, J. Y., Li, C. S., Therien, M., Asante-Appiah, E., … Scapin, G. (2004). Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors. Bioorganic & Medicinal Chemistry Letters, 14(4), 1043–1048. https://doi.org/10.1016/j.bmcl.2003.11.076
Lau, Cheuk K., Christopher I. Bayly, Jacques Yves Gauthier, Chun Sing Li, Michel Therien, Ernest Asante-Appiah, Wanda Cromlish, et al. “Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.” Bioorganic & Medicinal Chemistry Letters 14, no. 4 (February 2004): 1043–48. https://doi.org/10.1016/j.bmcl.2003.11.076.
Lau CK, Bayly CI, Gauthier JY, Li CS, Therien M, Asante-Appiah E, et al. Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors. Bioorganic & medicinal chemistry letters. 2004 Feb;14(4):1043–8.
Lau, Cheuk K., et al. “Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.” Bioorganic & Medicinal Chemistry Letters, vol. 14, no. 4, Feb. 2004, pp. 1043–48. Epmc, doi:10.1016/j.bmcl.2003.11.076.
Lau CK, Bayly CI, Gauthier JY, Li CS, Therien M, Asante-Appiah E, Cromlish W, Boie Y, Forghani F, Desmarais S, Wang Q, Skorey K, Waddleton D, Payette P, Ramachandran C, Kennedy BP, Scapin G. Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors. Bioorganic & medicinal chemistry letters. 2004 Feb;14(4):1043–1048.
Published In
Bioorganic & medicinal chemistry letters
DOI
EISSN
1464-3405
ISSN
0960-894X
Publication Date
February 2004
Volume
14
Issue
4
Start / End Page
1043 / 1048
Related Subject Headings
- Structure-Activity Relationship
- Protein Tyrosine Phosphatases
- Protein Tyrosine Phosphatase, Non-Receptor Type 1
- Organophosphorus Compounds
- Molecular Structure
- Models, Molecular
- Mice, Knockout
- Mice
- Medicinal & Biomolecular Chemistry
- Insecta