Cargando…

Phenylalanine-Derived β-Lactam TRPM8 Modulators. Configuration Effect on the Antagonist Activity

Transient receptor potential cation channel subfamily M member 8 (TRPM8) is a Ca(2+) non-selective ion channel implicated in a variety of pathological conditions, including cancer, inflammatory and neuropathic pain. In previous works we identified a family of chiral, highly hydrophobic β–lactam deri...

Descripción completa

Detalles Bibliográficos
Autores principales:	Bonache, María Ángeles, Llabrés, Pedro Juan, Martín-Escura, Cristina, De la Torre-Martínez, Roberto, Medina-Peris, Alicia, Butrón, Laura, Gómez-Monterrey, Isabel, Roa, Ana María, Fernández-Ballester, Gregorio, Ferrer-Montiel, Antonio, Fernández-Carvajal, Asia, González-Muñiz, Rosario
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	MDPI 2021
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7956626/ https://www.ncbi.nlm.nih.gov/pubmed/33673444 http://dx.doi.org/10.3390/ijms22052370

Ejemplares similares

Highly functionalized β-lactams and 2-ketopiperazines as TRPM8 antagonists with antiallodynic activity
por: Bonache, M.Ángeles, et al.
Publicado: (2020)

Synthesis, high-throughput screening and pharmacological characterization of β–lactam derivatives as TRPM8 antagonists
por: de la Torre-Martínez, Roberto, et al.
Publicado: (2017)

β-Lactam TRPM8 Antagonists Derived from Phe-Phenylalaninol Conjugates: Structure–Activity Relationships and Antiallodynic Activity
por: Martín-Escura, Cristina, et al.
Publicado: (2023)

Recent Progress in TRPM8 Modulation: An Update
por: González-Muñiz, Rosario, et al.
Publicado: (2019)

β–Lactam TRPM8 Antagonist RGM8-51 Displays Antinociceptive Activity in Different Animal Models
por: Martín-Escura, Cristina, et al.
Publicado: (2022)

TRPM8 contributes to sex dimorphism by promoting recovery of normal sensitivity in a mouse model of chronic migraine
por: Alarcón-Alarcón, David, et al.
Publicado: (2022)

TRPV1 in chronic pruritus and pain: Soft modulation as a therapeutic strategy
por: Fernández-Carvajal, Asia, et al.
Publicado: (2022)

Progress in the Structural Basis of thermoTRP Channel Polymodal Gating
por: Fernández-Ballester, Gregorio, et al.
Publicado: (2023)

Differential role of the menthol-binding residue Y745 in the antagonism of thermally gated TRPM8 channels
por: Malkia, Annika, et al.
Publicado: (2009)

In Vitro and In Vivo Pharmacological Characterization of a Novel TRPM8 Inhibitor Chemotype Identified by Small-Scale Preclinical Screening
por: Iraci, Nunzio, et al.
Publicado: (2022)

Ionic Channels as Targets for Drug Design: A Review on Computational Methods
por: Fernández-Ballester, Gregorio, et al.
Publicado: (2011)

New Strategies to Develop Novel Pain Therapies: Addressing Thermoreceptors from Different Points of View
por: Fernández-Carvajal, Asia, et al.
Publicado: (2011)

A capsaicinoid-based soft drug, AG1529, for attenuating TRPV1-mediated histaminergic and inflammatory sensory neuron excitability
por: Nikolaeva-Koleva, Magdalena, et al.
Publicado: (2021)

TRPM8 Channels: Advances in Structural Studies and Pharmacological Modulation
por: Izquierdo, Carolina, et al.
Publicado: (2021)

On the modulation of TRPM channels: Current perspectives and anticancer therapeutic implications
por: Ciaglia, Tania, et al.
Publicado: (2023)

Comprehensive Survey of Consensus Docking for High-Throughput Virtual Screening
por: Blanes-Mira, Clara, et al.
Publicado: (2022)

Role of the transient receptor potential vanilloid 1 in inflammation and sepsis
por: Devesa, Isabel, et al.
Publicado: (2011)

Exploration of TRPM8 Binding Sites by β-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities
por: Bertamino, Alessia, et al.
Publicado: (2020)

Compartmentalized primary cultures of dorsal root ganglion neurons to model peripheral pathophysiological conditions
por: Giorgi, Simona, et al.
Publicado: (2023)

Paclitaxel in vitro reversibly sensitizes the excitability of IB4(−) and IB4(+) sensory neurons from male and female rats
por: Villalba‐Riquelme, Eva, et al.
Publicado: (2022)

Modulating Protein–Protein Interactions by Cyclic and Macrocyclic Peptides. Prominent Strategies and Examples
por: González-Muñiz, Rosario, et al.
Publicado: (2021)

Therapeutic potential of TRPM8 antagonists in prostate cancer
por: Di Donato, Marzia, et al.
Publicado: (2021)

Characterization of New TRPM8 Modulators in Pain Perception
por: De Caro, Carmen, et al.
Publicado: (2019)

Targeting protein–protein interactions to rescue Δf508-cftr: a novel corrector approach to treat cystic fibrosis
por: Devesa, Isabel, et al.
Publicado: (2013)

Biosynthesis and Metabolic Fate of Phenylalanine in Conifers
por: Pascual, María B., et al.
Publicado: (2016)

Clinical Relevance of Antibiotic Susceptibility Profiles for Screening Gram-negative Microorganisms Resistant to Beta-Lactam Antibiotics
por: Montiel-Riquelme, Francisco, et al.
Publicado: (2020)

Solid-Phase Synthesis of New Trp(Nps)-Containing Dipeptide Derivatives as TRPV1 Channel Blockers
por: de Vega, Mª Jesús Pérez, et al.
Publicado: (2010)

Elucidation of the Relationship between CD Cotton Effects and the Absolute Configuration of Sixteen Stereoisomers of Spiroheterocyclic-Lactams
por: Yamada, Takeshi, et al.
Publicado: (2018)

Phenylalanine Binding Is Linked to Dimerization of the Regulatory Domain of Phenylalanine Hydroxylase
por: Zhang, Shengnan, et al.
Publicado: (2014)

Highly Functionalized 1,2–Diamino Compounds through Reductive Amination of Amino Acid-Derived β–Keto Esters
por: Pérez-Faginas, Paula, et al.
Publicado: (2013)

Mutation of I696 and W697 in the TRP box of vanilloid receptor subtype I modulates allosteric channel activation
por: Gregorio-Teruel, Lucia, et al.
Publicado: (2014)

Enantiomeric Resolution and Absolute Configuration of a Chiral δ-Lactam, Useful Intermediate for the Synthesis of Bioactive Compounds
por: Listro, Roberta, et al.
Publicado: (2020)

Activation of Phenylalanine Hydroxylase by Phenylalanine Does Not Require Binding in the Active Site
por: Roberts, Kenneth M., et al.
Publicado: (2014)

Deregulation of phenylalanine biosynthesis evolved with the emergence of vascular plants
por: El-Azaz, Jorge, et al.
Publicado: (2021)

Adamantyl Analogues of Paracetamol as Potent Analgesic Drugs via Inhibition of TRPA1
por: Fresno, Nieves, et al.
Publicado: (2014)

Expression of TRPM6 and TRPM7 in the preterm piglet heart
por: Forbes, Elizabeth M., et al.
Publicado: (2022)

(13)C-phenylalanine breath test detects altered phenylalanine kinetics in schizophrenia patients
por: Teraishi, T, et al.
Publicado: (2012)

Therapeutic implication of L-phenylalanine aggregation mechanism and its modulation by D-phenylalanine in phenylketonuria
por: Singh, Virender, et al.
Publicado: (2014)

Mutations of TRPM8 channels: Unraveling the molecular basis of activation by cold and ligands
por: Plaza‐Cayón, Alejandro, et al.
Publicado: (2022)

High-resolution experimental and computational electrophysiology reveals weak β-lactam binding events in the porin PorB
por: Bartsch, Annika, et al.
Publicado: (2019)

Cannot write session to /tmp/vufind_sessions/sess_1ki1cbtesejg0pkk0a1h8ravaa