[HTML][HTML] PROTACs: great opportunities for academia and industry

X Sun, H Gao, Y Yang, M He, Y Wu, Y Song… - Signal transduction and …, 2019 - nature.com
Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …

[HTML][HTML] Targeting transcription factors for cancer treatment

M Lambert, S Jambon, S Depauw… - Molecules, 2018 - mdpi.com
Transcription factors are involved in a large number of human diseases such as cancers for
which they account for about 20% of all oncogenes identified so far. For long time, with the …

Small-molecule-induced polymerization triggers degradation of BCL6

M Słabicki, H Yoon, J Koeppel, L Nitsch… - Nature, 2020 - nature.com
Effective and sustained inhibition of non-enzymatic oncogenic driver proteins is a major
pharmacological challenge. The clinical success of thalidomide analogues demonstrates …

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 …

Germinal center‐derived lymphomas: The darkest side of humoral immunity

C Mlynarczyk, L Fontán, A Melnick - Immunological reviews, 2019 - Wiley Online Library
One of the unusual features of germinal center (GC) B cells is that they manifest many
hallmarks of cancer cells. Accordingly, most B‐cell neoplasms originate from the GC …

[HTML][HTML] Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies

Y He, S Khan, Z Huo, D Lv, X Zhang, X Liu… - Journal of Hematology & …, 2020 - Springer
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that
utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI) …

[HTML][HTML] 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 …

[HTML][HTML] TBL1XR1 mutations drive extranodal lymphoma by inducing a pro-tumorigenic memory fate

L Venturutti, M Teater, A Zhai, A Chadburn, L Babiker… - Cell, 2020 - cell.com
The most aggressive B cell lymphomas frequently manifest extranodal distribution and carry
somatic mutations in the poorly characterized gene TBL1XR1. Here, we show that TBL1XR1 …

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 …

The expanding role of the BCL6 oncoprotein as a cancer therapeutic target

MG Cardenas, E Oswald, W Yu, F Xue… - Clinical Cancer …, 2017 - AACR
BCL6 was initially discovered as an oncogene in B-cell lymphomas, where it drives the
malignant phenotype by repressing proliferation and DNA damage checkpoints and …