MCL-1 inhibitors, fast-lane development of a new class of anti-cancer agents

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http://hdl.handle.net/10138/322848

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Journal of Hematology & Oncology. 2020 Dec 11;13(1):173

Title: MCL-1 inhibitors, fast-lane development of a new class of anti-cancer agents
Author: Bolomsky, Arnold; Vogler, Meike; Köse, Murat C; Heckman, Caroline A; Ehx, Grégory; Ludwig, Heinz; Caers, Jo
Publisher: BioMed Central
Date: 2020-12-11
URI: http://hdl.handle.net/10138/322848
Abstract: Abstract Cell death escape is one of the most prominent features of tumor cells and closely linked to the dysregulation of members of the Bcl-2 family of proteins. Among those, the anti-apoptotic family member myeloid cell leukemia-1 (MCL-1) acts as a master regulator of apoptosis in various human malignancies. Irrespective of its unfavorable structure profile, independent research efforts recently led to the generation of highly potent MCL-1 inhibitors that are currently evaluated in clinical trials. This offers new perspectives to target a so far undruggable cancer cell dependency. However, a detailed understanding about the tumor and tissue type specific implications of MCL-1 are a prerequisite for the optimal (i.e., precision medicine guided) use of this novel drug class. In this review, we summarize the major functions of MCL-1 with a special focus on cancer, provide insights into its different roles in solid vs. hematological tumors and give an update about the (pre)clinical development program of state-of-the-art MCL-1 targeting compounds. We aim to raise the awareness about the heterogeneous role of MCL-1 as drug target between, but also within tumor entities and to highlight the importance of rationale treatment decisions on a case by case basis.
Subject: Myeloid cell leukemia 1
MCL-1
BCL-2
Dependency
Inhibitor
Apoptosis
Cancer
Leukemia
Myeloma
Lymphoma
Melanoma
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