BH3 profiling discriminates on-target small molecule BH3 mimetics from putative mimetics

Confounding off-target effects of BH3 mimetics at commonly used concentrations: MIM1, UMI-77, and A-1210477

(2019) David J. Mallick et al.   Cell Death & Disease

Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia

(2018) Adriana E. Tron et al.   Nature Communications

Epistatic mutations in PUMA BH3 drive an alternate binding mode to potently and selectively inhibit anti-apoptotic Bfl-1

(2017) Justin M Jenson et al.   eLife

iBH3: simple, fixable BH3 profiling to determine apoptotic priming in primary tissue by flow cytometry

(2016) Jeremy Ryan et al.   BIOLOGICAL CHEMISTRY

BCL2 Inhibitors as Anticancer Drugs: A Plethora of Misleading BH3 Mimetics

(2016) R. S. Soderquist et al.   MOLECULAR CANCER THERAPEUTICS

The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models

(2016) András Kotschy et al.   NATURE

Mito-priming as a method to engineer Bcl-2 addiction

(2016) Jonathan Lopez et al.   Nature Communications

Defining specificity and on-target activity of BH3-mimetics using engineered B-ALL cell lines

(2016) Brian Koss et al.   Oncotarget

Small-Molecule Bcl2 BH4 Antagonist for Lung Cancer Therapy

(2015) Bingshe Han et al.   CANCER CELL

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

(2015) Joel D. Leverson et al.   Science Translational Medicine

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax)

(2015) J D Leverson et al.   Cell Death & Disease

Maritoclax and dinaciclib inhibit MCL-1 activity and induce apoptosis in both a MCL-1-dependent and -independent manner

(2015) Shankar Varadarajan et al.   Oncotarget

Sabutoclax (BI97C1) and BI112D1, Putative Inhibitors of MCL-1, Induce Mitochondrial Fragmentation Either Upstream of or Independent of Apoptosis

(2015) Shankar Varadarajan et al.   NEOPLASIA

Designed BH3 Peptides with High Affinity and Specificity for Targeting Mcl-1 in Cells

(2014) Glenna Wink Foight et al.   ACS Chemical Biology

Gossypol Increases Expression of the Pro-apoptotic BH3-only Protein NOXA through a Novel Mechanism Involving Phospholipase A2, Cytoplasmic Calcium, and Endoplasmic Reticulum Stress

(2014) Ryan S. Soderquist et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity

(2014) Zhi-Fu Tao et al.   ACS Medicinal Chemistry Letters

The putative BH3 mimetic S1 sensitizes leukemia to ABT-737 by increasing reactive oxygen species, inducing endoplasmic reticulum stress, and upregulating the BH3-only protein NOXA

(2013) Ryan Soderquist et al.   APOPTOSIS

Evaluation and critical assessment of putative MCL-1 inhibitors

(2013) S Varadarajan et al.   CELL DEATH AND DIFFERENTIATION

A Novel Small-Molecule Inhibitor of Mcl-1 Blocks Pancreatic Cancer Growth In Vitro and In Vivo

(2013) F. Abulwerdi et al.   MOLECULAR CANCER THERAPEUTICS

Structure-guided design of a selective BCL-XL inhibitor

(2013) Guillaume Lessene et al.   Nature Chemical Biology

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

(2013) Andrew J Souers et al.   NATURE MEDICINE

Discovery of Marinopyrrole A (Maritoclax) as a Selective Mcl-1 Antagonist that Overcomes ABT-737 Resistance by Binding to and Targeting Mcl-1 for Proteasomal Degradation

(2012) Kenichiro Doi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Multiple BH3 Mimetics Antagonize Antiapoptotic MCL1 Protein by Inducing the Endoplasmic Reticulum Stress Response and Up-regulating BH3-only Protein NOXA

(2011) Tina C. Albershardt et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Apogossypol derivative BI-97C1 (Sabutoclax) targeting Mcl-1 sensitizes prostate cancer cells to mda-7/IL-24-mediated toxicity

(2011) R. Dash et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Different forms of cell death induced by putative BCL2 inhibitors

(2009) M Vogler et al.   CELL DEATH AND DIFFERENTIATION

MCL-1–dependent leukemia cells are more sensitive to chemotherapy than BCL-2–dependent counterparts

(2009) Joslyn K. Brunelle et al.   JOURNAL OF CELL BIOLOGY

Gossypol, a BH3 mimetic, induces apoptosis in chronic lymphocytic leukemia cells

(2008) K. Balakrishnan et al.   BLOOD

ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor

(2008) C. Tse et al.   CANCER RESEARCH

Expression and purification of recombinant annexin V for the detection of membrane alterations on apoptotic cells

(2008) Gabriela Brumatti et al.   METHODS