Protein degraders enter the clinic—a new approach to cancer therapy

D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X Xie, T Yu, X Li, N Zhang, LJ Foster, C Peng… - Signal transduction and …, 2023 - nature.com
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

[HTML][HTML] Emerging pharmacotherapeutic strategies to overcome undruggable proteins in cancer

Y Lu, Y Yang, G Zhu, H Zeng, Y Fan, F Guo… - … Journal of Biological …, 2023 - ncbi.nlm.nih.gov
Targeted therapies in cancer treatment can improve in vivo efficacy and reduce adverse
effects by altering the tissue exposure of specific biomolecules. However, there are still large …

Digesting the role of JAK-STAT and cytokine signaling in oral and gastric cancers

Y Ni, JT Low, J Silke, LA O'Reilly - Frontiers in Immunology, 2022 - frontiersin.org
When small proteins such as cytokines bind to their associated receptors on the plasma
membrane, they can activate multiple internal signaling cascades allowing information from …

Targeting cereblon in hematologic malignancies

O Fuchs - Blood Reviews, 2023 - Elsevier
The protein cereblon (CRBN) is a substrate receptor of the cullin 4-really interesting new
gene (RING) E3 ubiquitin ligase complex CRL4 CRBN. Targeting CRBN mediates selective …

Degraders upgraded: the rise of PROTACs in hematological malignancies

JML Casan, JF Seymour - Blood, 2024 - ashpublications.org
Targeted protein degradation (TPD) is a revolutionary approach to targeted therapy in
hematological malignancies that potentially circumvents many constraints of existing small …

Molecular glue-mediated targeted protein degradation: A novel strategy in small-molecule drug development

X Tan, Z Huang, H Pei, Z Jia, J Zheng - Iscience, 2024 - cell.com
Small-molecule drugs are effective and thus most widely used. However, their applications
are limited by their reliance on active high-affinity binding sites, restricting their target …

[HTML][HTML] Exploiting the ubiquitin system in myeloid malignancies. From basic research to drug discovery in MDS and AML

R Drula, S Iluta, D Gulei, C Iuga, D Dima, G Ghiaur… - Blood Reviews, 2022 - Elsevier
The ubiquitin-proteasome system is the crucial homeostatic mechanism responsible for the
degradation and turnover of proteins. As such, alterations at this level are often associated …

Research progress of PROTACs for neurodegenerative diseases therapy

Z Cai, Z Yang, H Li, Y Fang - Bioorganic Chemistry, 2024 - Elsevier
Neurodegenerative diseases (NDD) are characterized by the gradual deterioration of
neuronal function and integrity, resulting in an overall decline in brain function. The existing …

Emerging synthetic drugs for the treatment of diffuse large B-cell lymphoma

N Dong, L Perez-Lamas, JC Chavez - Expert Opinion on Emerging …, 2023 - Taylor & Francis
Introduction Diffuse large B-cell lymphoma (DLBCL) is the most common aggressive
lymphoma. Recent advances in immunotherapy such as chimeric antigen receptor T-cell …