Exploring Ramachandran and chi space: conformationally constrained amino acids and peptides in the design of bioactive polypeptide ligands

SM Cowell, YS Lee, JP Cain… - Current medicinal …, 2004 - ingentaconnect.com
Ligand binding and concomitant changes in receptor structure provide the means to target
signal transduction pathways. With appropriate refinement of the ligand's interaction with the …

SNew Trends in the Development of Opioid Peptide Analogues as Advanced Remedies for Pain Relief

L Gentilucci - Current topics in medicinal chemistry, 2004 - ingentaconnect.com
The search for new peptides to be used as analgesics in place of morphine has been mainly
directed to develop peptide analogues or peptidomimetics having higher biological stability …

Affinity, potency, efficacy, selectivity, and molecular modeling of substituted fentanyls at opioid receptors

AJ Eshleman, S Nagarajan, KM Wolfrum… - Biochemical …, 2020 - Elsevier
Substituted fentanyls are abused and cause rapid fatal overdose. As their pharmacology is
not well characterized, we examined in vitro pharmacology and structure–activity …

Crosslinked aspartic acids as helix‐nucleating templates

H Zhao, QS Liu, H Geng, Y Tian, M Cheng… - Angewandte …, 2016 - Wiley Online Library
Described is a facile helix‐nucleating template based on a tethered aspartic acid at the N‐
terminus [terminal aspartic acid (TD)]. The nucleating effect of the template is subtly …

Visualizing endogenous opioid receptors in living neurons using ligand-directed chemistry

S Arttamangkul, A Plazek, EJ Platt, H **, TF Murray… - Elife, 2019 - elifesciences.org
Identifying neurons that have functional opioid receptors is fundamental for the
understanding of the cellular, synaptic and systems actions of opioids. Current techniques …

Development of a selective peptide κ-opioid receptor antagonist by late-stage functionalization with cysteine staples

E Muratspahić, AM White, CI Ciotu… - Journal of Medicinal …, 2023 - ACS Publications
The κ-opioid receptor (KOR) is an attractive target for the development of novel drugs. KOR
agonists are potentially safer pain medications, whereas KOR antagonists are promising …

Novel opioid cyclic tetrapeptides: Trp isomers of CJ‐15,208 exhibit distinct opioid receptor agonism and short‐acting κ opioid receptor antagonism

NC Ross, KJ Reilley, TF Murray… - British Journal of …, 2012 - Wiley Online Library
BACKGROUND AND PURPOSE The κ opioid receptor antagonists demonstrate potential for
maintaining abstinence from psychostimulant abuse, but existing non‐peptide κ‐receptor …

Conformation–activity relationships of opioid peptides with selective activities at opioid receptors

VJ Hruby, RS Agnes - Peptide Science, 1999 - Wiley Online Library
The discovery of endogenous opioid peptides 25 years ago opened up a new chapter in
efforts to understand the origins and control of pain, its relationships to other biological …

[HTML][HTML] Conformation of the core sequence in melanocortin peptides directs selectivity for the melanocortin MC3 and MC4 receptors

J Oosterom, WAJ Nijenhuis, WMM Schaaper… - Journal of Biological …, 1999 - Elsevier
Melanocortin peptides regulate a variety of physiological processes. Five melanocortin
receptors (MC-R) have been cloned and the MC3R and MC4R are the main brain MC …

Melanocortins and the brain: from effects via receptors to drug targets

RAH Adan, WH Gispen - European journal of pharmacology, 2000 - Elsevier
The lack of specific receptors (and antagonists) has hampered the research on the neural
mechanism of action of adrenocorticotropic hormone (ACTH)-and melanocyte-stimulating …