The manipulation of apoptosis for cancer therapy using BH3-mimetic drugs

ST Diepstraten, MA Anderson, PE Czabotar… - Nature Reviews …, 2022 - nature.com
Apoptosis is a form of programmed cell death that is regulated by the balance between
prosurvival and proapoptotic BCL-2 protein family members. Evasion of apoptosis is a …

Application of fragment-based drug discovery to versatile targets

Q Li - Frontiers in molecular biosciences, 2020 - frontiersin.org
Fragment-based drug discovery (FBDD) is a powerful method to develop potent small-
molecule compounds starting from fragments binding weakly to targets. As FBDD exhibits …

Structures of p53/BCL-2 complex suggest a mechanism for p53 to antagonize BCL-2 activity

H Wei, H Wang, G Wang, L Qu, L Jiang, S Dai… - Nature …, 2023 - nature.com
Mitochondrial apoptosis is strictly controlled by BCL-2 family proteins through a subtle
network of protein interactions. The tumor suppressor protein p53 triggers transcription …

Discovering small-molecule senolytics with deep neural networks

F Wong, S Omori, NM Donghia, EJ Zheng, JJ Collins - Nature Aging, 2023 - nature.com
The accumulation of senescent cells is associated with aging, inflammation and cellular
dysfunction. Senolytic drugs can alleviate age-related comorbidities by selectively killing …

Cyclic peptides discriminate BCL-2 and its clinical mutants from BCL-XL by engaging a single-residue discrepancy

F Li, J Liu, C Liu, Z Liu, X Peng, Y Huang… - Nature …, 2024 - nature.com
Overexpressed pro-survival B-cell lymphoma-2 (BCL-2) family proteins BCL-2 and BCL-XL
can render tumor cells malignant. Leukemia drug venetoclax is currently the only approved …

Fragment-to-lead medicinal chemistry publications in 2019

W Jahnke, DA Erlanson, IJP De Esch… - Journal of medicinal …, 2020 - ACS Publications
Fragment-based drug discovery (FBDD) has grown and matured to a point where it is
valuable to keep track of its extent and details of application. This Perspective summarizes …

Discovery of S64315, a potent and selective Mcl-1 inhibitor

Z Szlavik, M Csekei, A Paczal, ZB Szabo… - Journal of Medicinal …, 2020 - ACS Publications
Myeloid cell leukemia 1 (Mcl-1) has emerged as an attractive target for cancer therapy. It is
an antiapoptotic member of the Bcl-2 family of proteins, whose upregulation in human …

Hot-spots of Mcl-1 protein: miniperspective

C Denis, J Sopková-de Oliveira Santos… - Journal of medicinal …, 2019 - ACS Publications
Protein–protein interactions (PPIs) control many important physiological processes within
human cells. Apoptosis or programmed cell death is closely regulated by pro-and …

Understanding MCL1: from cellular function and regulation to pharmacological inhibition

M Sancho, D Leiva, E Lucendo, M Orzáez - The FEBS Journal, 2022 - Wiley Online Library
Myeloid cell leukemia‐1 (MCL1), an antiapoptotic member of the BCL2 family characterized
by a short half‐life, functions as a rapid sensor that regulates cell death and other relevant …

Structure-guided discovery of a selective Mcl-1 inhibitor with cellular activity

Z Szlávik, L Ondi, M Csékei, A Paczal… - Journal of Medicinal …, 2019 - ACS Publications
Myeloid cell leukemia 1 (Mcl-1), an antiapoptotic member of the Bcl-2 family of proteins,
whose upregulation when observed in human cancers is associated with high tumor grade …