[HTML][HTML] Development and crystal structures of a potent second-generation dual degrader of BCL-2 and BCL-xL
Overexpression of BCL-xL and BCL-2 play key roles in tumorigenesis and cancer drug
resistance. Advances in PROTAC technology facilitated recent development of the first BCL …
resistance. Advances in PROTAC technology facilitated recent development of the first BCL …
[HTML][HTML] Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity
Abstract PROteolysis-TArgeting Chimeras (PROTACs) have emerged as an innovative drug
development platform. However, most PROTACs have been generated empirically because …
development platform. However, most PROTACs have been generated empirically because …
Structural insights into PROTAC-mediated degradation of Bcl-xL
C Chung, H Dai, E Fernandez, CP Tinworth… - ACS Chemical …, 2020 - ACS Publications
The Bcl-2 family of proteins, such as Bcl-xL and Bcl-2, play key roles in cancer cell survival.
Structural studies of Bcl-xL formed the foundation for the development of the first Bcl-2 family …
Structural studies of Bcl-xL formed the foundation for the development of the first Bcl-2 family …
Structure-Guided Development of Potent Benzoylurea Inhibitors of BCL-XL and BCL-2
The BCL-2 family of proteins (including the prosurvival proteins BCL-2, BCL-XL, and MCL-1)
is an important target for the development of novel anticancer therapeutics. Despite the …
is an important target for the development of novel anticancer therapeutics. Despite the …
A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity
B-cell lymphoma extra large (BCL-XL) is a well-validated cancer target. However, the on-
target and dose-limiting thrombocytopenia limits the use of BCL-XL inhibitors, such as …
target and dose-limiting thrombocytopenia limits the use of BCL-XL inhibitors, such as …
Discovery of a Novel BCL-XL PROTAC Degrader with Enhanced BCL-2 Inhibition
BCL-XL and BCL-2 are important targets for cancer treatment. BCL-XL specific proteolysis-
targeting chimeras (PROTACs) have been developed to circumvent the on-target platelet …
targeting chimeras (PROTACs) have been developed to circumvent the on-target platelet …
Discovery of IAP-recruiting BCL-XL PROTACs as potent degraders across multiple cancer cell lines
Abstract Targeting BCL-X L via PROTACs is a promising strategy in reducing BCL-X L
inhibition associated platelet toxicity. Recently, we reported potent BCL-X L PROTAC …
inhibition associated platelet toxicity. Recently, we reported potent BCL-X L PROTAC …
Design, synthesis, and evaluation of BCL‐2 targeting PROTACs
BCL‐2, a member of the BCL‐2 protein family, is an antiapoptotic factor that regulates the
intrinsic pathway of apoptosis. Due to its aberrant activity, it is frequently implicated in …
intrinsic pathway of apoptosis. Due to its aberrant activity, it is frequently implicated in …
[HTML][HTML] Thalidomide derivatives degrade BCL-2 by reprogramming the binding surface of CRBN
J Wang, M Heinz, K Han, VJ Shah… - Cell Reports Physical …, 2024 - cell.com
Recent studies demonstrate that modified thalidomide chemically alters the binding surface
of its binding E3 ligase, CRBN, leading to the degradation of new substrate proteins. In this …
of its binding E3 ligase, CRBN, leading to the degradation of new substrate proteins. In this …
Structure-Based Design of A-1293102, a Potent and Selective BCL-XL Inhibitor
ZF Tao, X Wang, J Chen, JP Ingram, S Jin… - ACS Medicinal …, 2021 - ACS Publications
BCL-XL, an antiapoptotic member of the BCL-2 family of proteins, drives tumor survival and
maintenance and thus represents a key target for cancer treatment. Herein we report the …
maintenance and thus represents a key target for cancer treatment. Herein we report the …