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3fzl
From Proteopedia
| 3fzl, resolution 2.20Å () | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Sites: | and | ||||||||
| Ligands: | , | ||||||||
| Gene: | HSPA8, HSC70, HSP73, HSPA10 (Homo sapiens), BAG1, HAP (Homo sapiens) | ||||||||
| Related: | 3fzf, 3fzh, 3fzk, 3fzm | ||||||||
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
Contents |
Crystal Structures of Hsc70/Bag1 in Complex with Small Molecule Inhibitors
The design and synthesis of novel adenosine-derived inhibitors of HSP70, guided by modeling and X-ray crystallographic structures of these compounds in complex with HSC70/BAG-1, is described. Examples exhibited submicromolar affinity for HSP70, were highly selective over HSP90, and some displayed potency against HCT116 cells. Exposure of compound 12 to HCT116 cells caused significant reduction in cellular levels of Raf-1 and Her2 at concentrations similar to that which caused cell growth arrest.
Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design., Williamson DS, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Foloppe N, Francis GL, Graham CJ, Howes R, Macias AT, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ, J Med Chem. 2009 Mar 26;52(6):1510-3. PMID:19256508
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
3fzl is a 2 chain structure of Heat Shock Proteins with sequence from Homo sapiens. Full crystallographic information is available from OCA.
See Also
Reference
- Williamson DS, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Foloppe N, Francis GL, Graham CJ, Howes R, Macias AT, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ. Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design. J Med Chem. 2009 Mar 26;52(6):1510-3. PMID:19256508 doi:10.1021/jm801627a
Categories: Homo sapiens | Dokurno, P. | Murray, J B. | Surgenor, A E. | Williamson, D S. | Adenosine | Apoptosis | Atp-binding | Bag1 | Chaperone | Heat shock | Hsc70 | Hsp70 | Nucleotide | Nucleotide exchange factor | Nucleotide-binding | Protein folding | Small molecule inhibitor | Stress response
