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Peptidomimetics in Organic and Medicinal Chemistry: The Art of Transforming Peptides in Drugs
TLDR
Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery.
Low molecular weight, non-peptidic agonists of TrkA receptor with NGF-mimetic activity
Exploitation of the biologic activity of neurotrophins is desirable for medical purposes, but their protein nature intrinsically bears adverse pharmacokinetic properties. Here, we report synthesis
Low molecular weight, non-peptidic agonists of TrkA receptor with NGF-mimetic activity
Exploitation of the biologic activity of neurotrophins is desirable for medical purposes, but their protein nature intrinsically bears adverse pharmacokinetic properties. Here, we report synthesis
Selective non-steroidal inhibitors of 5α-reductase type 1
The TLR7 Ligand 9-Benzyl-2-Butoxy-8-Hydroxy Adenine Inhibits IL-17 Response by Eliciting IL-10 and IL-10–Inducing Cytokines
TLDR
The findings suggest that such TLR7 agonist downregulating Th17 (as well as Th2) response has to be considered a valid candidate for novel vaccine formulations in allergy.
2,2'-dihydroxy-3,3'-di-t-butyl-5,5'-dimethoxydiphenyl, a new metabolite of 2-t-butyl-4-methoxyphenol in the rat.
TLDR
Findings indicate that rat intestine is capable of transforming in vivo BHA into di-BHA and suggest that this organ is the major site where this transformation occurs.
Click-chemistry-derived triazole ligands of arginine-glycine-aspartate (RGD) integrins with a broad capacity to inhibit adhesion of melanoma cells and both in vitro and in vivo angiogenesis.
TLDR
The relevant biological effects exerted by compound 18 suggest its potential application as an antiangiogenic agent in the diagnosis and therapy of tumors where α(v)β(3) integrin expression is up-regulated.
New evidence of similarity between human and plant steroid metabolism: 5alpha-reductase activity in Solanum malacoxylon.
TLDR
It is demonstrated that campestenone, the natural substrate of DET2, is reduced to 5alpha-campestanone by both human 5alphaR isozymes but with different affinities.
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