[HTML][HTML] Venetoclax resistance: mechanistic insights and future strategies

F Ong, K Kim, MY Konopleva - Cancer Drug Resistance, 2022 - ncbi.nlm.nih.gov
Acute myeloid leukemia (AML) is historically associated with poor prognosis, especially in
older AML patients unfit for intensive chemotherapy. The development of Venetoclax, a …

[HTML][HTML] Targeting acute myeloid leukemia with venetoclax; biomarkers for sensitivity and rationale for venetoclax-based combination therapies

MS Griffioen, DC de Leeuw, JJWM Janssen, L Smit - Cancers, 2022 - mdpi.com
Simple Summary Venetoclax has proven to be a promising therapy for newly diagnosed,
relapsed and refractory AML patients ineligible for induction chemotherapy. Current ongoing …

[HTML][HTML] Activation of RAS/MAPK pathway confers MCL-1 mediated acquired resistance to BCL-2 inhibitor venetoclax in acute myeloid leukemia

Q Zhang, B Riley-Gillis, L Han, Y Jia, A Lodi… - Signal transduction and …, 2022 - nature.com
Despite high initial response rates, acute myeloid leukemia (AML) treated with the BCL-2–
selective inhibitor venetoclax (VEN) alone or in combinations commonly acquires …

[HTML][HTML] Effective Menin inhibitor-based combinations against AML with MLL rearrangement or NPM1 mutation (NPM1c)

W Fiskus, S Boettcher, N Daver, CP Mill, K Sasaki… - Blood cancer …, 2022 - nature.com
Abstract Treatment with Menin inhibitor (MI) disrupts the interaction between Menin and
MLL1 or MLL1-fusion protein (FP), inhibits HOXA9/MEIS1, induces differentiation and loss of …

Deregulation and epigenetic modification of BCL2-family genes cause resistance to venetoclax in hematologic malignancies

D Thomalla, L Beckmann, C Grimm… - Blood, The Journal …, 2022 - ashpublications.org
The BCL2 inhibitor venetoclax has been approved to treat different hematological
malignancies. Because there is no common genetic alteration causing resistance to …

Adapted to survive: targeting cancer cells with BH3 mimetics

J Montero, R Haq - Cancer discovery, 2022 - AACR
A hallmark of cancer is cell death evasion, underlying suboptimal responses to
chemotherapy, targeted agents, and immunotherapies. The approval of the antiapoptotic …

A phase II study of azacitidine, venetoclax, and trametinib in relapsed or refractory acute myeloid leukemia harboring RAS pathway-activating mutations

SP Desikan, F Ravandi, N Pemmaraju… - Acta …, 2022 - karger.com
Introduction: RAS pathway mutations are common mechanisms of resistance to acute
myeloid leukemia (AML) therapies. Trametinib, an oral MEK inhibitor, has been shown to …

Leukemic stem cell signatures in Acute myeloid leukemia-targeting the Guardians with novel approaches

D Thakral, R Gupta, A Khan - Stem Cell Reviews and Reports, 2022 - Springer
Acute myeloid leukemia is an aggressive hematopoietic stem cell malignancy with poor
outcomes despite the available treatment options including standard chemotherapy …

[HTML][HTML] Rationale for combining the BCL2 inhibitor venetoclax with the PI3K inhibitor bimiralisib in the treatment of IDH2-and FLT3-mutated acute myeloid leukemia

K Seipel, Y Brügger, H Mandhair, U Bacher… - International journal of …, 2022 - mdpi.com
In October 2020, the FDA granted regular approval to venetoclax (ABT-199) in combination
with hypomethylating agents for newly-diagnosed acute myeloid leukemia (AML) in adults …

[HTML][HTML] Proteomic and phosphoproteomic measurements enhance ability to predict ex vivo drug response in AML

SJC Gosline, C Tognon, M Nestor, S Joshi, R Modak… - Clinical proteomics, 2022 - Springer
Abstract Acute Myeloid Leukemia (AML) affects 20,000 patients in the US annually with a
five-year survival rate of approximately 25%. One reason for the low survival rate is the high …