Targeting MCL-1 dysregulates cell metabolism and leukemia-stroma interactions and resensitizes acute myeloid leukemia to BCL-2 inhibition

1 views | May 05 2021

Bing Z Carter et al. found that co-targeting MCL-1 and BCL-2 improved the efficacy of and overcame preexisting and acquired resistance to BCL-2 inhibition. [Read the Full Post]

Discovery of S64315, a Potent and Selective Mcl-1 Inhibitor

1 views | May 04 2021

Zoltan Szlavik et al. reported the discovery of clinical candidate S64315, a selective small molecule inhibitor of Mcl-1. [Read the Full Post]

Simultaneously Inhibiting BCL2 and MCL1 Is a Therapeutic Option for Patients with Advanced Melanoma

1 views | May 04 2021

Nabanita Mukherjee et al. suggested that several pro-apoptotic BCL2 family members, BCL2-like 11 (apoptosis facilitator) (BIM), phorbol-12-myristate-13-acetate-induced protein 1 (NOXA) or BID, played a role in the combination-induced effects. [Read the Full Post]

Albendazole-Induced SIRT3 Upregulation Protects Human Leukemia K562 Cells from the Cytotoxicity of MCL1 Suppression

12 views | Feb 12 2021

Liang-Jun Wang et al. demonstrated that ABZ-induced SIRT3 upregulation delayed the apoptosis-inducing effect of MCL1 suppression on apoptosis induction in K562 cells. [Read the Full Post]

Kinase activity-independent role of EphA2 in the regulation of M-phase progression

20 views | Jan 04 2021

Yuichiro Kaibori et al. suggested that EphA2 regulated M-phase progression in a manner independent of its kinase activity. [Read the Full Post]

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

20 views | Nov 20 2020

Zhi-Fu Tao et al. found that A-1155463 represented an excellent tool molecule for studying BCL-XL biology as well as a productive lead structure for further optimization. [Read the Full Post]

Direct Activation of BAX by BTSA1 Overcomes Apoptosis Resistance in Acute Myeloid Leukemia

0 views | Nov 19 2020

Denis E Reyna et al. provided proof-of-concept for direct BAX activation as a treatment strategy in AML. [Read the Full Post]

Mcl-1 targeting strategies unlock the proapoptotic potential of TRAIL in melanoma cells

41 views | Sep 19 2020

Zina Sarif et al. indicated a high relevance of Mcl-1 targeting also in melanoma therapy. [Read the Full Post]

Targeting BCL-2 proteins in pediatric cancer: Dual inhibition of BCL-X L and MCL-1 leads to rapid induction of intrinsic apoptosis

57 views | Aug 09 2020

Sarah Kehr et al. demonstrated the potency of A-1331852/S63845 in pediatric solid tumor cells and to describe the molecular mechanisms of A-1331852/S63845 co-treatment underlining the potential of BCL-XL and MCL-1 inhibition as treatment regime. [Read the Full Post]

The BCL-2 family protein inhibitor ABT-737 as an additional tool for the treatment of EBV-associated post-transplant lymphoproliferative disorders

97 views | Jul 14 2020

Aude Robert et al. suggested that the use of agents targeting BCL-2, either alone or in combination with other conventional drugs, represented a novel promising approach for post-transplant EBV-positive B lymphoproliferative disorders. [Read the Full Post]