Spirocyclic scaffolds are incorporated in various approved drugs and drug candidates. The
increasing interest in less planar bioactive compounds has given rise to the development of …

In the search for new therapeutic agents for currently incurable diseases, attention has
turned to traditionally “undruggable” targets, and collections of drug-like small molecules …

This paper is the 28th consecutive installment of the annual review of research concerning
the endogenous opioid system, now spanning over a quarter-century of research. It …

Transient protein–protein interactions (PPIs) are essential components in cellular signaling
pathways as well as in important processes such as viral infection, replication, and immune …

The design and synthesis of a β-turn mimetic library as a key component of a small-molecule
library targeting the major recognition motifs involved in protein–protein interactions is …

The application of endomorphins as clinical available analgesic drugs has been impeded by
their relatively poor receptor selectivity compared with alkaloid analgesics, rapid …

A new class of endomorphin-1 (EM-1) analogues were synthesized by introduction of novel
unnatural α-methylene-β-amino acids (Map) at position 3 or/and position 4. Their binding …

Constraining the conformation of flexible peptides is a proven strategy to increase potency,
selectivity, and metabolic stability. The focus has mostly been on constraining the backbone …

Herein we present the expedient synthesis of endomorphin-1 analogues containing
stereoisomeric β2-homo-Freidinger lactam-like scaffolds ([Amo2] EM), and we discuss …

Recently we reported the synthesis and structure–activity study of endomorphin-1 (EM-1)
analogues containing novel, unnatural α-methylene-β-aminopropanoic acids (Map). In the …