Pub. Date : 2008 Jun 1
PMID : 18468445
3 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | To overcome metabolic instability and poor membrane permeability, the N- and C-termini of Endo-1 were modified by lipoamino acids (Laa) and/or sugars, and 2",6"-dimethyltyrosine (Dmt) replacement of Tyr. | 2',6'-dimethyltyrosine | ENDO1 | Homo sapiens |
| 2 | To overcome metabolic instability and poor membrane permeability, the N- and C-termini of Endo-1 were modified by lipoamino acids (Laa) and/or sugars, and 2",6"-dimethyltyrosine (Dmt) replacement of Tyr. | 2',6'-dimethyltyrosine | ENDO1 | Homo sapiens |
| 3 | Dmt provided a promising lead compound: [C8Laa-Dmt[1]]-Endo-1 is nine times more stable (t(1/2)=43.5min), >8-fold more permeable in Caco-2 cell monolayers, and exhibits 140-fold greater mu-opioid receptor affinity (K(imu)=0.08nM). | 2',6'-dimethyltyrosine | ENDO1 | Homo sapiens |