Small-molecule-induced polymerization triggers degradation of BCL6
Effective and sustained inhibition of non-enzymatic oncogenic driver proteins is a major
pharmacological challenge. The clinical success of thalidomide analogues demonstrates …
pharmacological challenge. The clinical success of thalidomide analogues demonstrates …
An inhibitor of Bcl-2 family proteins induces regression of solid tumours
T Oltersdorf, SW Elmore, AR Shoemaker… - Nature, 2005 - nature.com
Proteins in the Bcl-2 family are central regulators of programmed cell death, and members
that inhibit apoptosis, such as Bcl-XL and Bcl-2, are overexpressed in many cancers and …
that inhibit apoptosis, such as Bcl-XL and Bcl-2, are overexpressed in many cancers and …
Phthalimide conjugation as a strategy for in vivo target protein degradation
The development of effective pharmacological inhibitors of multidomain scaffold proteins,
notably transcription factors, is a particularly challenging problem. In part, this is because …
notably transcription factors, is a particularly challenging problem. In part, this is because …
[PDF][PDF] Chemically induced degradation of the oncogenic transcription factor BCL6
N Kerres, S Steurer, S Schlager, G Bader, H Berger… - Cell reports, 2017 - cell.com
The transcription factor BCL6 is a known driver of oncogenesis in lymphoid malignancies,
including diffuse large B cell lymphoma (DLBCL). Disruption of its interaction with …
including diffuse large B cell lymphoma (DLBCL). Disruption of its interaction with …
Development of a novel B-cell lymphoma 6 (BCL6) PROTAC to provide insight into small molecule targeting of BCL6
W McCoull, T Cheung, E Anderson, P Barton… - ACS Chemical …, 2018 - ACS Publications
B-cell lymphoma 6 (BCL6) inhibition is a promising mechanism for treating hematological
cancers but high quality chemical probes are necessary to evaluate its therapeutic potential …
cancers but high quality chemical probes are necessary to evaluate its therapeutic potential …
Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide
In the 1950s, the drug thalidomide, administered as a sedative to pregnant women, led to
the birth of thousands of children with multiple defects. Despite the teratogenicity of …
the birth of thousands of children with multiple defects. Despite the teratogenicity of …
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 …
Rewiring cancer drivers to activate apoptosis
S Gourisankar, A Krokhotin, W Ji, X Liu, CY Chang… - Nature, 2023 - nature.com
Genes that drive the proliferation, survival, invasion and metastasis of malignant cells have
been identified for many human cancers,,–. Independent studies have identified cell death …
been identified for many human cancers,,–. Independent studies have identified cell death …
Upgrading the BCL-2 network
HL Galonek, JM Hardwick - Nature cell biology, 2006 - nature.com
The BCL-2 oncogene promotes cancer progression by prohibiting cell death. BCL-2-related
regulators were once thought to constitute a simple, two-class system of anti-death and pro …
regulators were once thought to constitute a simple, two-class system of anti-death and pro …
Lenalidomide induces ubiquitination and degradation of CK1α in del (5q) MDS
Lenalidomide is a highly effective treatment for myelodysplastic syndrome (MDS) with
deletion of chromosome 5q (del (5q)). Here, we demonstrate that lenalidomide induces the …
deletion of chromosome 5q (del (5q)). Here, we demonstrate that lenalidomide induces the …