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PROteolysis-Targeting Chimeras (PROTACs) in leukemia: overview and future perspectives.
Vicente, André T S; Salvador, Jorge A R.
Afiliación
  • Vicente ATS; Laboratory of Pharmaceutical Chemistry Faculty of Pharmacy University of Coimbra Coimbra Portugal.
  • Salvador JAR; Center for Neuroscience and Cell Biology University of Coimbra Coimbra Portugal.
MedComm (2020) ; 5(6): e575, 2024 Jun.
Article en En | MEDLINE | ID: mdl-38845697
ABSTRACT
Leukemia is a heterogeneous group of life-threatening malignant disorders of the hematopoietic system. Immunotherapy, radiotherapy, stem cell transplantation, targeted therapy, and chemotherapy are among the approved leukemia treatments. Unfortunately, therapeutic resistance, side effects, relapses, and long-term sequelae occur in a significant proportion of patients and severely compromise the treatment efficacy. The development of novel approaches to improve outcomes is therefore an unmet need. Recently, novel leukemia drug discovery strategies, including targeted protein degradation, have shown potential to advance the field of personalized medicine for leukemia patients. Specifically, PROteolysis-TArgeting Chimeras (PROTACs) are revolutionary compounds that allow the selective degradation of a protein by the ubiquitin-proteasome system. Developed against a wide range of cancer targets, they show promising potential in overcoming many of the drawbacks associated with conventional therapies. Following the exponential growth of antileukemic PROTACs, this article reviews PROTAC-mediated degradation of leukemia-associated targets. Chemical structures, in vitro and in vivo activities, pharmacokinetics, pharmacodynamics, and clinical trials of PROTACs are critically discussed. Furthermore, advantages, challenges, and future perspectives of PROTACs in leukemia are covered, in order to understand the potential that these novel compounds may have as future drugs for leukemia treatment.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: MedComm (2020) Año: 2024 Tipo del documento: Article Pais de publicación: China

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: MedComm (2020) Año: 2024 Tipo del documento: Article Pais de publicación: China