[HTML][HTML] Rationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma

MG Cardenas, W Yu, W Beguelin… - The Journal of …, 2016 - Am Soc Clin Investig
Diffuse large B cell lymphomas (DLBCLs) arise from proliferating B cells transiting different
stages of the germinal center reaction. In activated B cell DLBCLs (ABC-DLBCLs), a class of …

Bcl-xL–inhibitory BH3 mimetics can induce a transient thrombocytopathy that undermines the hemostatic function of platelets

SM Schoenwaelder, KE Jarman… - Blood, The Journal …, 2011 - ashpublications.org
BH3 mimetics are a new class of proapo-ptotic anticancer agents that have shown
considerable promise in preclinical animal models and early-stage human trials. These …

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy

JD Leverson, DC Phillips, MJ Mitten… - Science translational …, 2015 - science.org
The BCL-2/BCL-XL/BCL-W inhibitor ABT-263 (navitoclax) has shown promising clinical
activity in lymphoid malignancies such as chronic lymphocytic leukemia. However, its …

[HTML][HTML] The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized

MF Van Delft, AH Wei, KD Mason, CJ Vandenberg… - Cancer cell, 2006 - cell.com
Since apoptosis is impaired in malignant cells overexpressing prosurvival Bcl-2 proteins,
drugs mimicking their natural antagonists, BH3-only proteins, might overcome …

A first-in-class polymerase theta inhibitor selectively targets homologous-recombination-deficient tumors

J Zhou, C Gelot, C Pantelidou, A Li, H Yücel, RE Davis… - Nature cancer, 2021 - nature.com
DNA polymerase theta (POLθ or POLQ) is synthetic lethal with homologous recombination
(HR) deficiency and is thus a candidate target for HR-deficient cancers. Through high …

Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets

Y Xiong, Y Zhong, H Yim, X Yang, KS Park… - Journal of the …, 2022 - ACS Publications
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for
degrading disease-causing proteins. While many PROTACs have been developed for …

ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor

C Tse, AR Shoemaker, J Adickes, MG Anderson… - Cancer research, 2008 - AACR
Overexpression of the prosurvival Bcl-2 family members (Bcl-2, Bcl-xL, and Mcl-1) is
commonly associated with tumor maintenance, progression, and chemoresistance. We …

TRBC1-targeting antibody–drug conjugates for the treatment of T cell cancers

TD Nichakawade, J Ge, BJ Mog, BS Lee, AH Pearlman… - Nature, 2024 - nature.com
Antibody and chimeric antigen receptor (CAR) T cell-mediated targeted therapies have
improved survival in patients with solid and haematologic malignancies,,,,,,,–. Adults with T …

Translating cancer research into targeted therapeutics

JS de BONO, A Ashworth - Nature, 2010 - nature.com
The emphasis in cancer drug development has shifted from cytotoxic, non-specific
chemotherapies to molecularly targeted, rationally designed drugs promising greater …

Global PROTAC toolbox for degrading BCR–ABL overcomes drug-resistant mutants and adverse effects

Y Yang, H Gao, X Sun, Y Sun, Y Qiu… - Journal of medicinal …, 2020 - ACS Publications
The BCR–ABL fusion oncoprotein causes chronic myeloid leukemia or acute lymphoblastic
leukemia in Ph+ patients because the ABL kinase is constitutively activated. However …