[PDF][PDF] Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy
S Bonazzi, E d'Hennezel, REJ Beckwith, L Xu… - Cell Chemical …, 2023 - cell.com
Malignant tumors can evade destruction by the immune system by attracting immune-
suppressive regulatory T cells (Treg) cells. The IKZF2 (Helios) transcription factor plays a …
suppressive regulatory T cells (Treg) cells. The IKZF2 (Helios) transcription factor plays a …
Homo-PROTACs for the chemical knockdown of cereblon
C Steinebach, S Lindner, ND Udeshi… - ACS chemical …, 2018 - ACS Publications
The immunomodulatory drugs (IMiDs) thalidomide, lenalidomide, and pomalidomide, all
approved for the treatment of multiple myeloma, induce targeted ubiquitination and …
approved for the treatment of multiple myeloma, induce targeted ubiquitination and …
Targeting oncoproteins with a positive selection assay for protein degraders
Most intracellular proteins lack hydrophobic pockets suitable for altering their function with
drug-like small molecules. Recent studies indicate that some undruggable proteins can be …
drug-like small molecules. Recent studies indicate that some undruggable proteins can be …
Discovery of a conditionally activated IL-2 that promotes antitumor immunity and induces tumor regression
CJ Nirschl, HR Brodkin, DJ Hicklin, N Ismail… - Cancer immunology …, 2022 - AACR
IL-2 is a cytokine clinically approved for the treatment of melanoma and renal cell
carcinoma. Unfortunately, its clinical utility is hindered by serious side effects driven by the …
carcinoma. Unfortunately, its clinical utility is hindered by serious side effects driven by the …
Development of PDE6D and CK1α degraders through chemical derivatization of FPFT-2216
Immunomodulatory drugs are a class of drugs approved for the treatment of multiple
myeloma. These compounds exert their clinical effects by inducing interactions between the …
myeloma. These compounds exert their clinical effects by inducing interactions between the …
Defining the human C2H2 zinc finger degrome targeted by thalidomide analogs through CRBN
QL Sievers, G Petzold, RD Bunker, A Renneville… - Science, 2018 - science.org
INTRODUCTION Thalidomide, lenalidomide, and pomalidomide are clinically approved
therapies for the treatment of multiple myeloma and other hematologic malignancies. These …
therapies for the treatment of multiple myeloma and other hematologic malignancies. These …
[PDF][PDF] Piperlongumine conjugates induce targeted protein degradation
Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that degrade target
proteins through recruiting E3 ligases. However, their application is limited in part because …
proteins through recruiting E3 ligases. However, their application is limited in part because …
NKTR-214, an engineered cytokine with biased IL2 receptor binding, increased tumor exposure, and marked efficacy in mouse tumor models
DH Charych, U Hoch, JL Langowski, SR Lee… - Clinical Cancer …, 2016 - AACR
Purpose: Aldesleukin, recombinant human IL2, is an effective immunotherapy for metastatic
melanoma and renal cancer, with durable responses in approximately 10% of patients; …
melanoma and renal cancer, with durable responses in approximately 10% of patients; …
A novel cereblon modulator for targeted protein degradation
SA Kim, A Go, SH Jo, SJ Park, YU Jeon, JE Kim… - European Journal of …, 2019 - Elsevier
Immunomodulatory drugs (IMiDs) exert anti-myeloma activity by binding to the protein
cereblon (CRBN) and subsequently degrading IKZF1/3. Recently, their ability to recruit E3 …
cereblon (CRBN) and subsequently degrading IKZF1/3. Recently, their ability to recruit E3 …
PI3Kα/δ inhibition promotes anti-tumor immunity through direct enhancement of effector CD8+ T-cell activity
LS Carnevalli, C Sinclair, MA Taylor… - … for immunotherapy of …, 2018 - Springer
PI3K inhibitors with differential selectivity to distinct PI3K isoforms have been tested
extensively in clinical trials, largely to target tumor epithelial cells. PI3K signaling also …
extensively in clinical trials, largely to target tumor epithelial cells. PI3K signaling also …