Quest for novel chemical entities through incorporation of silicon in drug scaffolds
In order to optimize a lead molecule for further development, bioisosteric replacements are
generally adopted as one of the strategies. Silicon appears to be the right choice as a …
generally adopted as one of the strategies. Silicon appears to be the right choice as a …
Silicon-containing amino acids: synthetic aspects, conformational studies, and applications to bioactive peptides
E Rémond, C Martin, J Martinez, F Cavelier - Chemical Reviews, 2016 - ACS Publications
Unnatural α-amino acids form a family of essential molecules used for, among other
applications, the synthesis of modified peptides, to improve resistance to proteolytic enzyme …
applications, the synthesis of modified peptides, to improve resistance to proteolytic enzyme …
Novel approaches, drug candidates, and targets in pain drug discovery
Because of the problems associated with opioids, drug discovery efforts have been
employed to develop opioids with reduced side effects using approaches such as biased …
employed to develop opioids with reduced side effects using approaches such as biased …
Unnatural amino acids: Promising implications for the development of new antimicrobial peptides
X Wang, X Yang, Q Wang, D Meng - Critical Reviews in …, 2023 - Taylor & Francis
The increasing incidence and rapid spread of bacterial resistance to conventional antibiotics
are a serious global threat to public health, highlighting the need to develop new …
are a serious global threat to public health, highlighting the need to develop new …
New insights in the design of bioactive peptides and chelating agents for imaging and therapy in oncology
Many synthetic peptides have been developed for diagnosis and therapy of human cancers
based on their ability to target specific receptors on cancer cell surface or to penetrate the …
based on their ability to target specific receptors on cancer cell surface or to penetrate the …
Therapeutic approaches targeting the neurotensin receptors
Introduction: Neurotensin is a gut-brain peptide hormone, a 13 amino acid neuropeptide
found in the central nervous system and in the GI tract. The neurotensinergic system is …
found in the central nervous system and in the GI tract. The neurotensinergic system is …
Neurotensin (8–13) analogs as dual NTS1 and NTS2 receptor ligands with enhanced effects on a mouse model of Parkinson's disease
T Kühl, MG Georgieva, H Hübner, M Lazarova… - European Journal of …, 2023 - Elsevier
The modulatory interactions between neurotensin (NT) and the dopaminergic
neurotransmitter system in the brain suggest that NT may be associated with the progression …
neurotransmitter system in the brain suggest that NT may be associated with the progression …
Structural optimization and characterization of potent analgesic macrocyclic analogues of neurotensin (8–13)
M Sousbie, M Vivancos, RL Brouillette… - Journal of Medicinal …, 2018 - ACS Publications
The neurotensin receptors are attractive targets for the development of new analgesic
compounds. They represent potential alternatives or adjuvants to opioids. Herein, we report …
compounds. They represent potential alternatives or adjuvants to opioids. Herein, we report …
Recent progress in non-opioid analgesic peptides
MJP de Vega, A Ferrer-Montiel… - Archives of biochemistry …, 2018 - Elsevier
Pain is a prevalent complex medical problem, characterized by physically debilitating and
mentally destabilizing conditions. Current pain therapeutics mainly include non-steroidal …
mentally destabilizing conditions. Current pain therapeutics mainly include non-steroidal …
MnO2 mediated sequential oxidation/olefination of alkyl-substituted heteroarenes with alcohols
C Zhang, Z Li, Y Fang, S Jiang, M Wang, G Zhang - Tetrahedron, 2020 - Elsevier
A practical and efficient ligand-free MnO 2 mediated sequential oxidation and olefination
has been developed for the facile synthesis of a broad range of unsaturated N …
has been developed for the facile synthesis of a broad range of unsaturated N …