scholarly journals Identification of small molecule inhibitors of ERCC1-XPF that inhibit DNA repair and potentiate cisplatin efficacy in cancer cells

Oncotarget ◽  
2016 ◽  
Vol 7 (46) ◽  
pp. 75104-75117 ◽  
Author(s):  
Sanjeevani Arora ◽  
Joshua Heyza ◽  
Hao Zhang ◽  
Vivian Kalman-Maltese ◽  
Kristin Tillison ◽  
...  
Keyword(s):  
Dna Repair ◽  
Cancer Cells ◽  
Small Molecule ◽  
Small Molecule Inhibitors

A novel reporter construct for screening small molecule inhibitors that specifically target self-renewing cancer cells

2019 ◽  
Vol 383 (2) ◽  
pp. 111551
Author(s):  
Geetha Shanmugam ◽  
Amrutha Mohan ◽  
Khushbu Kumari ◽  
Jiss Maria Louis ◽  
U. Soumya Krishnan ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Reporter Construct

scholarly journals Androstano-arylpyrimidines: Novel small molecule inhibitors of MDR1 for sensitizing multidrug-resistant breast cancer cells

2021 ◽  
Vol 156 ◽  
pp. 105587
Author(s):  
Mohana Krishna Gopisetty ◽  
Dóra Izabella Adamecz ◽  
Ferenc István Nagy ◽  
Ádám Baji ◽  
Vasiliki Lathira ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Small Molecule ◽  
Breast Cancer Cells ◽  
Small Molecule Inhibitors ◽  
Multidrug Resistant

scholarly journals Small-Molecule Inhibitors of Bacterial AddAB and RecBCD Helicase-Nuclease DNA Repair Enzymes

2012 ◽  
Vol 7 (5) ◽  
pp. 879-891 ◽  
Author(s):  
Susan K. Amundsen ◽  
Timothy Spicer ◽  
Ahmet C. Karabulut ◽  
Luz Marina Londoño ◽  
Christina Eberhart ◽  
...  
Keyword(s):  
Dna Repair ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Dna Repair Enzymes ◽  
Repair Enzymes

Design and synthesis of tailored human caseinolytic protease P inhibitors

2018 ◽  
Vol 54 (70) ◽  
pp. 9833-9836 ◽  
Author(s):  
Thomas F. Gronauer ◽  
Melanie M. Mandl ◽  
Markus Lakemeyer ◽  
Mathias W. Hackl ◽  
Martina Meßner ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Target Identification ◽  
Functional Studies ◽  
Design And Synthesis ◽  
Caseinolytic Protease ◽  
Complex Target

To expedite functional studies of human ClpP we introduce tailored small molecule inhibitors. These compounds are active against the proteolytic ClpXP complex. Target identification elucidates anti-proliferative effects against cancer cells.

scholarly journals Small molecule inhibitors of a human recombination-associated ATPase, RAD54

2019 ◽  
Author(s):  
Kirk T. Ehmsen ◽  
Kenny K.H. Ang ◽  
William D. Wright ◽  
Julia L. Davies ◽  
Yassir Younis ◽  
...  
Keyword(s):  
Dna Repair ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Homology Search ◽  
Dna Breaks ◽  
Repair Synthesis ◽  
Molecular Events ◽  
Dna Strand Exchange ◽  
Dna Repair Synthesis

ABSTRACTHomologous recombination (HR) is a principal support pathway for DNA replication and for recovery from DNA breaks and interstrand crosslinks, making it a rational target for inhibition in cancer therapy. The ATPase RAD54 functions in molecular events that promote DNA sequence-preservation during HR-mediated damage repair, including homology search, DNA strand exchange, and transition to DNA repair synthesis within a displacement loop intermediate. We developed a high-throughput biochemical screen to identify small-molecule inhibitors of human RAD54, using a phosphate detection assay to monitor RAD54 ATPase activity in the presence of double-stranded DNA (dsDNA). After filtering potential DNA intercalators and ‘frequent hitters,’ we identified two chemotypes that reproducibly inhibited RAD54 ATPase in vitro. We evaluated these chemotypes for inhibition of RAD54-dsDNA binding and cancer cell survival. A halogenated carbazole/dihydroacridine scaffold inhibited a panel of SWI2/SNF2-related ATPases but not VCP/p97, an unrelated ATPase. Small molecules that interfere with key steps in HR— such as inhibitors of RAD54—may expose DNA repair-dependent vulnerabilities in cancer cells.

Structure-based Drug Design Strategies in the Development of Small Molecule Inhibitors Targeting Bcl-2 Family Proteins

2020 ◽  
Vol 17 (8) ◽  
pp. 943-953
Author(s):  
Zhe Yin ◽  
Donglin Yang ◽  
Jun Wang ◽  
Yuequan Jiang
Keyword(s):  
Clinical Trials ◽  
Drug Design ◽  
B Cell ◽  
Cancer Cells ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Cell Lymphoma ◽  
B Cell Lymphoma ◽  
Design Strategies ◽  
Structure Based Drug Design

Proteins of B-cell lymphoma (Bcl-2) family are key regulators of apoptosis and are involved in the pathogenesis of various cancers. Disrupting the interactions between the antiapoptotic and proapoptotic Bcl-2 members is an attractive strategy to reactivate the apoptosis of cancer cells. Structure-based drug design (SBDD) has been successfully applied to the discovery of small molecule inhibitors targeting Bcl-2 proteins in past decades. Up to now, many Bcl-2 inhibitors with different paralogue selectivity profiles have been developed and some were used in clinical trials. This review focused on the recent applications of SBDD strategies in the development of small molecule inhibitors targeting Bcl-2 family proteins.

Small-Molecule Inhibitors of APE1 DNA Repair Function: An Overview

2012 ◽  
Vol 5 (1) ◽  
pp. 14-35 ◽  
Author(s):  
Rasha I. Al-Safi ◽  
Srinivas Odde ◽  
Yumna Shabaik ◽  
Nouri Neamati
Keyword(s):  
Dna Repair ◽  
Small Molecule ◽  
Small Molecule Inhibitors
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