Structural highlights
5n5k is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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| Ligands: | , , , |
| Gene: | MMP12, HME (HUMAN) |
| Activity: | Macrophage elastase, with EC number 3.4.24.65 |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
[MMP12_HUMAN] May be involved in tissue injury and remodeling. Has significant elastolytic activity. Can accept large and small amino acids at the P1' site, but has a preference for leucine. Aromatic or hydrophobic residues are preferred at the P1 site, with small hydrophobic residues (preferably alanine) occupying P3.
Publication Abstract from PubMed
Oxaliplatin (OXA) is a valuable and largely used cancer drug which induces a serious and intractable neuropathy. The lipoyl-homotaurine derivative (ADM_12) reverts in vivo OXA-induced neuropathy, and it is an effective antagonist of the nociceptive sensor channel TRPA1. Unprecedentedly, this safe analgesic showed a synergy with OXA in vitro and proved to inhibit CA IX, a relevant therapeutic target, clearly interfering with pancreatic cancer cells' aggressiveness.
Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX).,Fragai M, Comito G, Di Cesare Mannelli L, Gualdani R, Calderone V, Louka A, Richichi B, Francesconi O, Angeli A, Nocentini A, Gratteri P, Chiarugi P, Ghelardini C, Tadini-Buoninsegni F, Supuran CT, Nativi C J Med Chem. 2017 Oct 27. doi: 10.1021/acs.jmedchem.7b01237. PMID:29048889[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Fragai M, Comito G, Di Cesare Mannelli L, Gualdani R, Calderone V, Louka A, Richichi B, Francesconi O, Angeli A, Nocentini A, Gratteri P, Chiarugi P, Ghelardini C, Tadini-Buoninsegni F, Supuran CT, Nativi C. Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX). J Med Chem. 2017 Oct 27. doi: 10.1021/acs.jmedchem.7b01237. PMID:29048889 doi:http://dx.doi.org/10.1021/acs.jmedchem.7b01237
