Allosteric Modulators of Dopamine D2 Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects …

AA Kaczor, TM Wróbel, D Bartuzi - Molecules, 2022 - mdpi.com
Allosteric modulation of G protein-coupled receptors (GPCRs) is nowadays a hot topic in
medicinal chemistry. Allosteric modulators, ie, compounds which bind in a receptor site …

Wandering beyond small molecules: Peptides as allosteric protein modulators

M Mannes, C Martin, C Menet, S Ballet - Trends in Pharmacological …, 2022 - cell.com
Recent years have seen the rise of allosteric modulation as an innovative approach for drug
design and discovery, efforts which culminated in the development of several clinical …

Stapling Amantadine to Melanostatin Neuropeptide: Discovery of Potent Positive Allosteric Modulators of the D2 Receptors

SC Silva-Reis, XC Correia… - ACS Medicinal …, 2023 - ACS Publications
This work describes the synthesis and pharmacological and toxicological evaluation of
melanostatin (MIF-1) bioconjugates with amantadine (Am) via a peptide linkage. The data …

Synthesis, pharmacological, and biological evaluation of 2-furoyl-based MIF-1 peptidomimetics and the development of a general-purpose model for allosteric …

IE Sampaio-Dias, JE Rodriguez-Borges… - ACS Chemical …, 2020 - ACS Publications
This work describes the synthesis and pharmacological evaluation of 2-furoyl-based
Melanostatin (MIF-1) peptidomimetics as dopamine D2 modulating agents. Eight novel …

Discovery of New Potent Positive Allosteric Modulators of Dopamine D2 Receptors: Insights into the Bioisosteric Replacement of Proline to 3-Furoic Acid in the …

IE Sampaio-Dias, A Reis-Mendes… - Journal of Medicinal …, 2021 - ACS Publications
The control of Parkinson's disease (PD) is challenged by the motor and non-motor
fluctuations as well as dyskinesias associated with levodopa long-term therapy. As such …

Design, synthesis, and biological evaluation of hybrid glypromate analogues using 2-azanorbornane as a prolyl and pipecolyl surrogate

IE Sampaio-Dias, M Santejo… - ACS Chemical …, 2021 - ACS Publications
Neurodegenerative disorders of the central nervous system are a class of heterogeneous
pathologies affecting millions of people worldwide and represent a global health burden in …

A convenient on-site oxidation strategy for the N-hydroxylation of Melanostatin neuropeptide using Cope elimination

IE Sampaio-Dias, SC Silva-Reis, BL Pires-Lima… - …, 2022 - thieme-connect.com
A convenient synthetic protocol for the unprecedented N-hydroxylation of proline residue in
Melanostatin (MIF-1) neuropeptide is reported. This methodology is grounded on the …

[PDF][PDF] Discovery, Design and Synthesis of G Protein Peptidomimetics

M Mannes - 2022 - researchportal.vub.be
The present thesis manuscript concludes my semi-industrial PhD fellowship in both the
fields of peptide synthesis in the Research Group of Organic Chemistry (ORGC), Faculty of …

Síntese de novos péptidos antioxidantes de penetração celular com alvo na mitocôndria

D Brandão - 2020 - search.proquest.com
A mitocôndria desempenha um papel vital na regulação do metabolismo de energia celular.
A sua capacidade de regular o equilíbrio redox é fundamental no controlo da vida e da …

[CITATION][C] Synthesis, Pharmacological and Biological Evaluation of 2-Furoyl-based MIF-1 Peptidomimetics, and the Development of a General-Purpose Model for …

I Dias, JE Rodríguez Borges, V Yáñez, S Arrasate… - American Chemical Society