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Discovery of MDV6058 (PF-06952229), a selective and potent TGF?R1 inhibitor: Design, synthesis and optimization
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| DOI | 10.1016/J.BMCL.2022.128979 | ||||
| Año | 2022 | ||||
| Tipo | artículo de investigación |
Citas Totales
Autores Afiliación Chile
Instituciones Chile
% Participación
Internacional
Autores
Afiliación Extranjera
Instituciones
Extranjeras
Abstract
Compound 1 is a potent TGF-beta receptor type-1 (TGF beta R1 or ALK5) inhibitor but is metabolically unstable. A solvent-exposed part of this molecule was used to analogue and modulate cell activity, liver microsome stability and mouse pharmacokinetics. The evolution of SAR that led to the selection of 2 (MDV6058 / PF-06952229) as a preclinical lead compound is described.
| Ord. | Autor | Género | Institución - País |
|---|---|---|---|
| 1 | Pujala, Brahmam | - |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 2 | Ramachandran, Sreekanth A. | - |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 3 | Sonawane, Mukesh | Hombre |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 4 | Kamble, Maruti M. | - |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 5 | Panpatil, Dayanand | - |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 6 | Adhikari, Swati | Mujer |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 7 | Soni, Sanjeev | Hombre |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 8 | Subbareddy, Venkata | - |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 9 | Shinde, Bharat U. | - |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 10 | Nayak, Anjan K. | - |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 11 | Bansal, Chandni | - |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 12 | Gupta, Ashu | - |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 13 | Mukherjee, Kakoli | - |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 14 | Agarwal, Anil K. | Hombre |
Integral BioSci Pvt Ltd - India
Integral BioSciences Pvt. Ltd - India |
| 15 | GUERRERO-BUSTAMANTE, JAVIER | Hombre |
Fundación Ciencia y Vida - Chile
Fundación Ciencia para la Vida - Chile |
| 16 | Herrera, Francisco J. | Hombre |
Medivation Inc - Estados Unidos
Medivation Inc. - Estados Unidos |
| 17 | BERNALES-ODINO, SEBASTIAN | Hombre |
Medivation Inc - Estados Unidos
Medivation Inc. - Estados Unidos |
| 18 | Guha, Mausumee | - |
Medivation Inc - Estados Unidos
Pfizer Inc - Estados Unidos Medivation Inc. - Estados Unidos Pfizer Inc. - Estados Unidos |
| 19 | Chakravarty, Sarvajit | - |
Medivation Inc - Estados Unidos
Medivation Inc. - Estados Unidos |
| 20 | Pham, Son M. | Hombre |
Medivation Inc - Estados Unidos
Medivation Inc. - Estados Unidos |
| 21 | Rai, Roopa | - |
Medivation Inc - Estados Unidos
Medivation Inc. - Estados Unidos |
| Agradecimiento |
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| The authors thank Daniel L. Severance (formerly at Schrodinger, Inc.) for his input. We are grateful to the analytical and purification groups at Integral BioSciences for their support. This work was funded solely by Medivation, Inc. |
| The authors thank Daniel L. Severance (formerly at Schrödinger, Inc.) for his input. We are grateful to the analytical and purification groups at Integral BioSciences for their support. This work was funded solely by Medivation, Inc. |
