11 Result(s)
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Rosario González-Muñiz
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Article
Constrained C-terminal hexapeptide neurotensin analogues containing a 3-oxoindolizidine skeleton
In order to enforce different spatial orientations in the C-terminal hexapeptide of neurotensin (NT8−13) and to gain information about the importance of the 10–11 peptide bond for binding to NT receptors, the Pro
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Similarity Study on Peptide γ-turn Conformation Mimetics
The ability of a series of structures to mimic the geometric and electronic properties of an ideal γ–turn has been studied. Initially, an exhaustive conformational analysis was carried out using the molecular ...
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Article
Studies on the synthesis of β-keto esters derived from dipeptides: search for a low-epimerizing method
β-Keto esters derived from dipeptides areprepared by application of common methodologiesemployed for the synthesis of amino acid-derivedβ-keto esters; however, epimerization of theC-terminal residue occurred t...
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PACAP27 Analogues Incorporating Type II/II’ β-Turn Mimetics
Pituitary adenyl cyclase-activating peptide (PACAP) is a member of the superfamily of regulatory peptides including secretin, glucagon, VIP and GRF [1]. It exists in two bioactive forms, PACAP38 and its shorte...
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Exploring solid-phase approaches for the preparation of new β-lactams from amino acids
Two solid-phase approaches, involving the base-assisted intramolecularalkylation of N-chloroacetyl-Phe derivatives anchored to appropriatesolid supports, were investigated for the preparation of novel β-lactams. ...
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Exploring the binding pocket for pyridopyrimidine ligands at the CCK1 receptor by molecular docking
Pyridopyrimidine-based analogues are among the most highly potent and selective antagonists of cholecystokinin receptor subtype-1 (CCK1R) described to date. To better understand the structural and chemical fea...
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2-Alkyl-2-carboxyazetidines as γ-turn inducers: incorporation into neurotrophin fragments
Conveniently substituted 2-alkyl-2-carboxyazetidine amino acids have been incorporated into NGF and NT3 tetrapeptide sequences to investigate their utility as reverse turn inducers (γ- vs. β-turns). Despite th...
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Pharmacology of TRP Channels
TRP channels are a family of ion channels involved in a plethora of physiological sensory processes. Since their discovery they have attracted the attention of academic and non-academic laboratories with the a...
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β-Lactams Through Single Bond Ring Closing: Methods, Transformations and Bioactivity
Because the renewed interest of β–lactams in organic and medicinal chemistry, research in this field continues producing new appealing progresses. This chapter will cover significant success in the synthesis o...
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Article
Open AccessSynthesis, high-throughput screening and pharmacological characterization of β–lactam derivatives as TRPM8 antagonists
The mammalian transient receptor potential melastatin channel 8 (TRPM8), highly expressed in trigeminal and dorsal root ganglia, mediates the cooling sensation and plays an important role in the cold hypersens...
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Open AccessHighly functionalized β-lactams and 2-ketopiperazines as TRPM8 antagonists with antiallodynic activity
The cool sensor transient receptor potential melastatin channel 8 (TRPM8) is highly expressed in trigeminal and dorsal root ganglia, playing a key role in cold hypersensitivity associated to different peripher...
