Development and evaluation of human AP endonuclease inhibitors in melanoma and glioma cell lines

M Z Mohammed; V N Vyjayanti; C A Laughton; L V Dekker; P M Fischer; D M Wilson; R Abbotts; S Shah; P M Patel; I D Hickson; S Madhusudan

doi:10.1038/sj.bjc.6606058

Development and evaluation of human AP endonuclease inhibitors in melanoma and glioma cell lines

M Z Mohammed, V N Vyjayanti, C A Laughton, L V Dekker, P M Fischer, D M Wilson, R Abbotts, S Shah, P M Patel, I D Hickson, S Madhusudan

Research output: Contribution to journal › Journal article › Research › peer-review

60 Citations (Scopus)

Abstract

Modulation of DNA base excision repair (BER) has the potential to enhance response to chemotherapy and improve outcomes in tumours such as melanoma and glioma. APE1, a critical protein in BER that processes potentially cytotoxic abasic sites (AP sites), is a promising new target in cancer. In the current study, we aimed to develop small molecule inhibitors of APE1 for cancer therapy.

Original language	English
Journal	British Journal of Cancer Management
Volume	104
Issue number	4
Pages (from-to)	653-63
Number of pages	11
ISSN	1744-3865
DOIs	https://doi.org/10.1038/sj.bjc.6606058
Publication status	Published - 15 Feb 2011

Keywords

Brain Neoplasms
Cell Line, Tumor
DNA-(Apurinic or Apyrimidinic Site) Lyase
Drug Discovery
Drug Evaluation, Preclinical
Enzyme Inhibitors
Glioma
Hela Cells
High-Throughput Screening Assays
Humans
Inhibitory Concentration 50
Melanoma
Models, Biological
Models, Molecular
Structure-Activity Relationship

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Cite this

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title = "Development and evaluation of human AP endonuclease inhibitors in melanoma and glioma cell lines",

abstract = "Modulation of DNA base excision repair (BER) has the potential to enhance response to chemotherapy and improve outcomes in tumours such as melanoma and glioma. APE1, a critical protein in BER that processes potentially cytotoxic abasic sites (AP sites), is a promising new target in cancer. In the current study, we aimed to develop small molecule inhibitors of APE1 for cancer therapy.",

keywords = "Brain Neoplasms, Cell Line, Tumor, DNA-(Apurinic or Apyrimidinic Site) Lyase, Drug Discovery, Drug Evaluation, Preclinical, Enzyme Inhibitors, Glioma, Hela Cells, High-Throughput Screening Assays, Humans, Inhibitory Concentration 50, Melanoma, Models, Biological, Models, Molecular, Structure-Activity Relationship",

author = "Mohammed, {M Z} and Vyjayanti, {V N} and Laughton, {C A} and Dekker, {L V} and Fischer, {P M} and Wilson, {D M} and R Abbotts and S Shah and Patel, {P M} and Hickson, {I D} and S Madhusudan",

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T1 - Development and evaluation of human AP endonuclease inhibitors in melanoma and glioma cell lines

AU - Mohammed, M Z

AU - Vyjayanti, V N

AU - Laughton, C A

AU - Dekker, L V

AU - Fischer, P M

AU - Wilson, D M

AU - Abbotts, R

AU - Shah, S

AU - Patel, P M

AU - Hickson, I D

AU - Madhusudan, S

PY - 2011/2/15

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N2 - Modulation of DNA base excision repair (BER) has the potential to enhance response to chemotherapy and improve outcomes in tumours such as melanoma and glioma. APE1, a critical protein in BER that processes potentially cytotoxic abasic sites (AP sites), is a promising new target in cancer. In the current study, we aimed to develop small molecule inhibitors of APE1 for cancer therapy.

AB - Modulation of DNA base excision repair (BER) has the potential to enhance response to chemotherapy and improve outcomes in tumours such as melanoma and glioma. APE1, a critical protein in BER that processes potentially cytotoxic abasic sites (AP sites), is a promising new target in cancer. In the current study, we aimed to develop small molecule inhibitors of APE1 for cancer therapy.

KW - Brain Neoplasms

KW - Cell Line, Tumor

KW - DNA-(Apurinic or Apyrimidinic Site) Lyase

KW - Drug Discovery

KW - Drug Evaluation, Preclinical

KW - Enzyme Inhibitors

KW - Glioma

KW - Hela Cells

KW - High-Throughput Screening Assays

KW - Humans

KW - Inhibitory Concentration 50

KW - Melanoma

KW - Models, Biological

KW - Models, Molecular

KW - Structure-Activity Relationship

U2 - 10.1038/sj.bjc.6606058

DO - 10.1038/sj.bjc.6606058

M3 - Journal article

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SN - 1744-3865

VL - 104

SP - 653

EP - 663

JO - British Journal of Cancer Management

JF - British Journal of Cancer Management

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