80064-48-8Relevant articles and documents
DIPEPTIDE MIMETICS OF NGF AND BDNF NEUROTROPHINS
-
Paragraph 0055, (2019/04/16)
The invention relates to compounds having either agonist or antagonist activities for the neurotrophins NGF and BDNF and represented by monomeric or dimeric substituted dipeptides that are analogs of the exposed portions of loop 1 or loop 4 regions of these neurotrophins near or at a beta-turn of the respective loop. N-acylated substituents of these dipeptides are biostereoisomers of the amino acid residues preceding these dipeptide sequences in the neurotrophin primary structure. The dimeric structure is produced advantageously by using hexatnethylenediaanine to which dipeptides are attached via their carboxyl groups. The claimed compounds displayed neuroprotective and differentiation-inducing activities in cellular models and enhanced the amount of phosphorylated tyrosine kinase A and the heat shock proteins Hsp32 and Hsp70 in the concentration range of 10 -9 to 10 -5 M. They also displayed neuroprotective, anti-parkinsonian, anti-stroke, anti-ischemic, anti-depressant and anti-amnestic activities in animal models and were active in experimental models of Alzheimer's disease. These in vivo effects of the claimed compounds are displayed in the dose range of 0.01 to 10 mg/kg when administered intraperitoneally.
Synthesis of biologically active biotinylated muramyl dipeptides
Grimes, Catherine Leimkuhler,Podolsky, Daniel K.,O'Shea, Erin K.
supporting information; experimental part, p. 6061 - 6063 (2010/11/17)
Muramyl dipeptide (MDP) is believed to interact with an innate immune receptor, Nod2. To identify the cellular receptor for MDP, we have synthesized biotinylated MDP isomers and tested the ability of these compounds to activate Nod2 in a cell-based assay. We found that the modification of MDP does not perturb its ability to activate Nod2. These tagged versions of MDP will be useful to identify the cellular receptor of the immunostimulatory molecules.
Synthesis of some conformationally constrained analogues of muramyl dipeptide (MDP)
Kundu,Rizvi,Srivastava,Haq,Mathur
, p. 409 - 413 (2007/10/02)
Synthesis of three conformationally constrained analogues of MDP, viz AcMur-Δ-Ala-D-isoGln (1), AcMur-Aib-D-isoGln (2) and AcnorMur-Aib-D-isoGln (3) is described. Coupling of the protected carbohydrate derivatives with appropriate dipeptide amines in the