Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae
Balansa, Walter, Islam, Robiul, Fontaine, Frank, Piggott, Andrew M., Zhang, Hua, Webb, Timothy J., Gilbert, Daniel F., Lynch, Joseph W., and Capon, Robert J. (2010) Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae. Bioorganic & Medicinal Chemistry, 18 (8). pp. 2912-2919.
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Abstract
Screening an extract library of >2500 southern Australian and Antarctic marine invertebrates and algae for modulators of glycine receptor (GlyR) chloride channels identified three Irciniidae sponges that yielded new examples of a rare class of glycinyl lactam sesterterpene, ircinialactam A, 8-hydroxyircinialactam A, 8-hydroxyircinialactam B, ircinialactam C, ent-ircinialactam C and ircinialactam D. Structure–activity relationship (SAR) investigations revealed a new pharmacophore with potent and subunit selective modulatory properties against α1 and α3 GlyR isoforms. Such GlyR modulators have potential application as pharmacological tools, and as leads for the development of GlyR targeting therapeutics to treat chronic inflammatory pain, epilepsy, spasticity and hyperekplexia.
| Item ID: | 65668 |
|---|---|
| Item Type: | Article (Research - C1) |
| ISSN: | 1464-3391 |
| Copyright Information: | © 2010 Elsevier Ltd. All rights reserved. |
| Funders: | Australian Research Council (ARC) |
| Date Deposited: | 01 Aug 2024 02:56 |
| FoR Codes: | 03 CHEMICAL SCIENCES > 0304 Medicinal and Biomolecular Chemistry > 030405 Molecular Medicine @ 50% 06 BIOLOGICAL SCIENCES > 0601 Biochemistry and Cell Biology > 060110 Receptors and Membrane Biology @ 30% 11 MEDICAL AND HEALTH SCIENCES > 1109 Neurosciences > 110903 Central Nervous System @ 20% |
| SEO Codes: | 92 HEALTH > 9201 Clinical Health (Organs, Diseases and Abnormal Conditions) > 920111 Nervous System and Disorders @ 20% 97 EXPANDING KNOWLEDGE > 970111 Expanding Knowledge in the Medical and Health Sciences @ 50% 97 EXPANDING KNOWLEDGE > 970103 Expanding Knowledge in the Chemical Sciences @ 30% |
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