Targeting BCR-ABL1 in chronic myeloid leukemia by PROTAC-mediated targeted protein degradation
Although the use of ATP-competitive tyrosine kinase inhibitors of oncoprotein BCR-ABL1
has enabled durable responses in patients with chronic myeloid leukemia (CML), issues of …
has enabled durable responses in patients with chronic myeloid leukemia (CML), issues of …
Orally bioavailable BTK PROTAC active against wild-type and C481 mutant BTKs in human lymphoma CDX mouse models
YS Lim, SM Yoo, V Patil, HW Kim, HH Kim… - Blood …, 2023 - ashpublications.org
Bruton tyrosine kinase (BTK) is an important signaling hub that activates the B-cell receptor
(BCR) signaling cascade. BCR activation can contribute to the growth and survival of B-cell …
(BCR) signaling cascade. BCR activation can contribute to the growth and survival of B-cell …
[HTML][HTML] S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth
P Casara, J Davidson, A Claperon… - Oncotarget, 2018 - ncbi.nlm.nih.gov
Escape from apoptosis is one of the major hallmarks of cancer cells. The B-cell Lymphoma 2
(BCL-2) gene family encodes pro-apoptotic and anti-apoptotic proteins that are key …
(BCL-2) gene family encodes pro-apoptotic and anti-apoptotic proteins that are key …
Targeting BCL2 with BH3 mimetics: basic science and clinical application of venetoclax in chronic lymphocytic leukemia and related B cell malignancies
AW Roberts, DCS Huang - Clinical Pharmacology & …, 2017 - Wiley Online Library
The intracellular protein B‐cell‐lymphoma‐2 (BCL2) has been considered an attractive
target for cancer therapy since the discovery of its function as a major promoter of cell …
target for cancer therapy since the discovery of its function as a major promoter of cell …
Radiotherapy-triggered proteolysis targeting chimera prodrug activation in tumors
C Yang, Y Yang, Y Li, Q Ni, J Li - Journal of the American …, 2022 - ACS Publications
Proteolysis targeting chimera (PROTAC) is an emerging protein degradation strategy, which
shows excellent advantages in targeting those so-called “undruggable” proteins. However …
shows excellent advantages in targeting those so-called “undruggable” proteins. However …
High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell–like diffuse large B-cell lymphoma cells
LA Mathews Griner, R Guha, P Shinn… - Proceedings of the …, 2014 - National Acad Sciences
The clinical development of drug combinations is typically achieved through trial-and-error
or via insight gained through a detailed molecular understanding of dysregulated signaling …
or via insight gained through a detailed molecular understanding of dysregulated signaling …
Targeted therapy: an elusive cancer target
C Brown - Nature, 2016 - nature.com
Targeted therapy: An elusive cancer target | Nature Skip to main content Thank you for visiting
nature.com. You are using a browser version with limited support for CSS. To obtain the best …
nature.com. You are using a browser version with limited support for CSS. To obtain the best …
Bcl-2, Bcl-xL, and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells
Abstract The BH3-mimetic ABT-737 and an orally bioavailable compound of the same class,
navitoclax (ABT-263), have shown promising antitumor efficacy in preclinical and early …
navitoclax (ABT-263), have shown promising antitumor efficacy in preclinical and early …
Target and tissue selectivity of PROTAC degraders
RG Guenette, SW Yang, J Min, B Pei… - Chemical Society …, 2022 - pubs.rsc.org
Targeted protein degradation (TPD) strategies have revolutionized how scientists tackle
challenging protein targets deemed undruggable with traditional small molecule inhibitors …
challenging protein targets deemed undruggable with traditional small molecule inhibitors …
Strategies to Reduce the On‐Target Platelet Toxicity of Bcl‐xL Inhibitors: PROTACs, SNIPERs and Prodrug‐Based Approaches
A Negi, AS Voisin‐Chiret - ChemBioChem, 2022 - Wiley Online Library
Apoptosis is a highly regulated cellular process. Aberration in apoptosis is a common
characteristic of various disorders. Therefore, proteins involved in apoptosis are prime …
characteristic of various disorders. Therefore, proteins involved in apoptosis are prime …