Selective degradation of CDK6 by a palbociclib based PROTAC.

Rana, Sandeep; Bendjennat, Mourad; Kour, Smit; King, Hannah M; Kizhake, Smitha; Zahid, Muhammad; Natarajan, Amarnath

Rana, Sandeep; Bendjennat, Mourad; Kour, Smit; King, Hannah M; Kizhake, Smitha; Zahid, Muhammad; Natarajan, Amarnath.

Afiliación

Rana S; Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, Nebraska 68022, USA. Electronic address: sandeep.rana@unmc.edu.
Bendjennat M; Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, Nebraska 68022, USA.
Kour S; Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, Nebraska 68022, USA.
King HM; Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, Nebraska 68022, USA.
Kizhake S; Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, Nebraska 68022, USA.
Zahid M; Department of Environmental, Agricultural and Occupational Health, College of Public Health, University of Nebraska Medical Center, Omaha, Nebraska 68022, USA.
Natarajan A; Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, Nebraska 68022, USA; Fred & Pamela Buffett Cancer Center, University of Nebraska Medical Center, Omaha, Nebraska 68022, USA; Department of Pharmaceutical Sciences, University of Nebraska Me

Bioorg Med Chem Lett ; 29(11): 1375-1379, 2019 06 01.

Article en En | MEDLINE | ID: mdl-30935795

Asunto(s)

Quinasa 6 Dependiente de la Ciclina/antagonistas & inhibidores; Piperazinas/farmacología; Inhibidores de Proteínas Quinasas/farmacología; Proteolisis/efectos de los fármacos; Piridinas/farmacología; Quinasa 6 Dependiente de la Ciclina/metabolismo; Relación Dosis-Respuesta a Droga; Humanos; Modelos Moleculares; Estructura Molecular; Piperazinas/síntesis química; Piperazinas/química; Inhibidores de Proteínas Quinasas/síntesis química; Inhibidores de Proteínas Quinasas/química; Piridinas/síntesis química; Piridinas/química; Relación Estructura-Actividad

Palabras clave

CDK6; CDK6 degrader; PROTAC; Palbociclib

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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piperazinas / Piridinas / Inhibidores de Proteínas Quinasas / Quinasa 6 Dependiente de la Ciclina / Proteolisis Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article

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