Traditionally, drugs are monovalent, targeting only one site on the protein surface. This
includes orthosteric and allosteric drugs, which bind the protein at orthosteric and allosteric …

One of the key scientific aspects of small-molecule drug discovery and development is the
analysis of the relationship between its chemical structure and biological activity …

The cardiotoxicity associated with des-ethyl-dexfenfluramine (norDF) and related agonists of
the serotonin receptor 2B (5-HT2B) has solidified the receptor's place as an “antitarget” in …

Abstract Opioid Use Disorder (OUD) can be described as intense preoccupation with using
or obtaining opioids despite the negative consequences associated with their use. As the …

Bromodomain-selective BET inhibition has emerged as a promising strategy to improve the
safety profiles of pan-BET inhibitors. Herein, we report the discovery of potent phenoxyaryl …

The development of highly potent and selective μ opioid receptor (MOR) modulators with
favorable drug-like properties has always been a focus in the opioid domain. Our previous …

The number of opioid-related overdose deaths and individuals that have suffered from
opioid use disorders have significantly increased over the last 30 years. FDA approved …

This paper is the forty-sixth consecutive installment of the annual anthological review of
research concerning the endogenous opioid system, summarizing articles published during …