[HTML][HTML] Targeted protein degrader development for cancer: advances, challenges, and opportunities

Y Fang, S Wang, S Han, Y Zhao, C Yu, H Liu… - Trends in pharmacological …, 2023 - cell.com
Anticancer-targeted therapies inhibit various kinases implicated in cancer and have been
used in clinical settings for decades. However, many cancer-related targets are proteins …

Targeted protein degradation: from mechanisms to clinic

JM Tsai, RP Nowak, BL Ebert, ES Fischer - Nature Reviews Molecular …, 2024 - nature.com
Targeted protein degradation refers to the use of small molecules to induce the selective
degradation of proteins. In its most common form, this degradation is achieved through …

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 …

Targeted protein degradation: advances in drug discovery and clinical practice

G Zhong, X Chang, W Xie, X Zhou - Signal Transduction and Targeted …, 2024 - nature.com
Targeted protein degradation (TPD) represents a revolutionary therapeutic strategy in
disease management, providing a stark contrast to traditional therapeutic approaches like …

Novel agents in relapsed/refractory diffuse large B‐cell lymphoma

G Varma, J Goldstein, RH Advani - Hematological Oncology, 2023 - Wiley Online Library
Patients with relapsed or refractory (R/R) diffuse large B‐cell lymphoma (DLBCL), ineligible
for or relapsing after autologous stem‐cell transplant or chimeric antigen‐receptor T‐cell …

Targeting Ikaros and Aiolos: Reviewing novel protein degraders for the treatment of multiple myeloma, with a focus on iberdomide and mezigdomide

Y Liu, CC Mo, MA Hartley-Brown… - Expert Review of …, 2024 - Taylor & Francis
Introduction The treatment of multiple myeloma (MM) is evolving rapidly. Quadruplet
regimens incorporating proteasome inhibitors, immunomodulatory drugs (IMiDs), and CD38 …

Developing New Strategies for Relapsed/Refractory Diffuse Large B-Cell Lymphoma

E Gonzalez Barca - Journal of Clinical Medicine, 2023 - mdpi.com
Diffuse large B-cell lymphoma (DLBCL) is an aggressive and biologically heterogeneous
disease. Approximately 40% of patients with DLBCL will experience disease relapse or will …

Targeted protein degradation in hematologic malignancies: clinical progression towards novel therapeutics

Y Feng, X Hu, X Wang - Biomarker Research, 2024 - Springer
Targeted therapies, such as small molecule kinase inhibitors, have made significant
progress in the treatment of hematologic malignancies by directly modulating protein activity …

[HTML][HTML] Efficacy and Safety of Golcadomide, a Novel Cereblon E3 Ligase Modulator (CELMoD) Agent, Combined with Rituximab in a Phase 1/2 Open-Label Study of …

JC Chavez, LJ Nastoupil, F Morschhauser, G Cartron… - Blood, 2023 - Elsevier
Introduction: Golcadomide is a novel, oral, small-molecule CELMoD® agent that co-opts
cereblon to induce targeted degradation of the transcription factors Ikaros/Aiolos, which are …

CELMoDs类IKZF1/3降解剂的研究进展

吴雄, 焦宇, 吕仕铭, 陈亚东, 梅德盛 - 药学进展, 2023 - pps.cpu.edu.cn
IKZF 1 (Ikaros) 和IKZF 3 (Aiolos) 是一种锌指转录因子, 涉及多种信号通路和调节机制,
对免疫细胞发育和内环境稳定尤为关键. IKZF 1/3 过度表达与多种血液系统恶性肿瘤的发生和 …