The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling.

Vecchio, Elizabeth A; Chuo, Chung Hui; Baltos, Jo-Anne; Ford, Leigh; Scammells, Peter J; Wang, Bing H; Christopoulos, Arthur; White, Paul J; May, Lauren T

Vecchio, Elizabeth A; Chuo, Chung Hui; Baltos, Jo-Anne; Ford, Leigh; Scammells, Peter J; Wang, Bing H; Christopoulos, Arthur; White, Paul J; May, Lauren T.

Afiliación

Vecchio EA; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences & Department of Pharmacology, Monash University, Parkville, VIC 3052, Australia. Electronic address: elizabeth.vecchio@monash.edu.
Chuo CH; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences & Department of Pharmacology, Monash University, Parkville, VIC 3052, Australia. Electronic address: chung.chuo@monash.edu.
Baltos JA; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences & Department of Pharmacology, Monash University, Parkville, VIC 3052, Australia. Electronic address: joanne.baltos@monash.edu.
Ford L; Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia. Electronic address: leigh.ford@monash.edu.
Scammells PJ; Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia. Electronic address: peter.scammels@monash.edu.
Wang BH; Centre of Cardiovascular Research and Education in Therapeutics, School of Public Health and Preventive Medicine, Faculty of Medicine, Nursing and Health Sciences, Monash University, Melbourne, VIC 3004, Australia. Electronic address: bing.wang@monash.edu.
Christopoulos A; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences & Department of Pharmacology, Monash University, Parkville, VIC 3052, Australia. Electronic address: arthur.christopoulos@monash.edu.
White PJ; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences & Department of Pharmacology, Monash University, Parkville, VIC 3052, Australia. Electronic address: paul.white@monash.edu.
May LT; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences & Department of Pharmacology, Monash University, Parkville, VIC 3052, Australia. Electronic address: lauren.may@monash.edu.

Biochem Pharmacol ; 117: 46-56, 2016 Oct 01.

Article en En | MEDLINE | ID: mdl-27520486

Asunto(s)

Agonistas del Receptor de Adenosina A2/farmacología; Adenosina/análogos & derivados; Colágeno/antagonistas & inhibidores; Células Mesangiales/efectos de los fármacos; Mioblastos Cardíacos/efectos de los fármacos; Sustancias Protectoras/farmacología; Receptor de Adenosina A2B/metabolismo; Transducción de Señal/efectos de los fármacos; Tiofenos/farmacología; Adenosina/farmacología; Agonistas del Receptor de Adenosina A2/metabolismo; Regulación Alostérica/efectos de los fármacos; Animales; Animales Recién Nacidos; Unión Competitiva; Células CHO; Línea Celular; Células Cultivadas; Colágeno/biosíntesis; Cricetulus; Fibrosis; Humanos; Ligandos; Células Mesangiales/citología; Células Mesangiales/metabolismo; Células Mesangiales/patología; Mioblastos Cardíacos/citología; Mioblastos Cardíacos/metabolismo; Mioblastos Cardíacos/patología; Ensayo de Unión Radioligante; Ratas; Ratas Sprague-Dawley; Receptor de Adenosina A2B/química; Receptor de Adenosina A2B/genética; Proteínas Recombinantes/química; Proteínas Recombinantes/metabolismo

Palabras clave

Adenosine; Adenosine A(2B) receptor; Angiotensin II (PubChem CID: 172198); BAY60-6583 (PubChem CID: 11717831); Bivalent agonist; Collagen; DPCPX (PubChem CID: 1329); Fibroblasts; NECA (PubChem CID: 448222); PSB-603 (PubChem CID: 44185871); SCH442416 (PubChem CID: 10668061); SLV320 (PubChem CID: 9953065); TGF-ß1 (PubChem CID: 56842206); [3H]DPCPX (PubChem CID: 53319341)

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Texto completo: 1 Colección: 01-internacional Asunto principal: Tiofenos / Transducción de Señal / Adenosina / Colágeno / Sustancias Protectoras / Mioblastos Cardíacos / Receptor de Adenosina A2B / Células Mesangiales / Agonistas del Receptor de Adenosina A2 Límite: Animals / Humans Idioma: En Revista: Biochem Pharmacol Año: 2016 Tipo del documento: Article

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