Discovery of a small molecule that inhibits Bcl-3-mediated cyclin D1 expression in melanoma cells
Saamarthy, Karunakar LU ; Ahlqvist, Kristofer LU ; Daams, Renée LU ; Balagunaseelan, Navisraj ; Rinaldo-Matthis, Agnes ; Kazi, Julhash U. LU
; Sime, Wondossen
LU
and Massoumi, Ramin
LU
(2024)
In BMC Cancer
24(1).
- Abstract
Molecular targeted therapy using a drug that suppresses the growth and spread of cancer cells via inhibition of a specific protein is a foundation of precision medicine and treatment. High expression of the proto-oncogene Bcl-3 promotes the proliferation and metastasis of cancer cells originating from tissues such as the colon, prostate, breast, and skin. The development of novel drugs targeting Bcl-3 alone or in combination with other therapies can cure these patients or prolong their survival. As a proof of concept, in the present study, we focused on metastatic melanoma as a model system. High-throughput screening and in vitro experiments identified BCL3ANT as a lead molecule that could interfere with Bcl-3-mediated cyclin D1... (More)
Molecular targeted therapy using a drug that suppresses the growth and spread of cancer cells via inhibition of a specific protein is a foundation of precision medicine and treatment. High expression of the proto-oncogene Bcl-3 promotes the proliferation and metastasis of cancer cells originating from tissues such as the colon, prostate, breast, and skin. The development of novel drugs targeting Bcl-3 alone or in combination with other therapies can cure these patients or prolong their survival. As a proof of concept, in the present study, we focused on metastatic melanoma as a model system. High-throughput screening and in vitro experiments identified BCL3ANT as a lead molecule that could interfere with Bcl-3-mediated cyclin D1 expression and cell proliferation and migration in melanoma. In experimental animal models of melanoma, it was demonstrated that the use of a Bcl-3 inhibitor can influence the survival of melanoma cells. Since there are no other inhibitors against Bcl-3 in the clinical pipeline for cancer treatment, this presents a unique opportunity to develop a highly specific drug against malignant melanoma to meet an urgent clinical need.
(Less)
- author
- Saamarthy, Karunakar
LU
; Ahlqvist, Kristofer
LU
; Daams, Renée
LU
; Balagunaseelan, Navisraj
; Rinaldo-Matthis, Agnes
; Kazi, Julhash U.
LU
; Sime, Wondossen
LU
and Massoumi, Ramin
LU
- organization
- publishing date
- 2024-12
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- Bcl-3, Cyclin D1, Melanoma, Proliferation
- in
- BMC Cancer
- volume
- 24
- issue
- 1
- article number
- 103
- publisher
- BioMed Central (BMC)
- external identifiers
-
- pmid:38238702
- scopus:85182679922
- ISSN
- 1471-2407
- DOI
- 10.1186/s12885-023-11663-y
- language
- English
- LU publication?
- yes
- id
- 0dcdcafb-aff0-46f5-9274-f51dfe6f9ed1
- date added to LUP
- 2024-04-11 14:23:12
- date last changed
- 2024-04-25 17:19:55
@article{0dcdcafb-aff0-46f5-9274-f51dfe6f9ed1,
abstract = {{<p>Molecular targeted therapy using a drug that suppresses the growth and spread of cancer cells via inhibition of a specific protein is a foundation of precision medicine and treatment. High expression of the proto-oncogene Bcl-3 promotes the proliferation and metastasis of cancer cells originating from tissues such as the colon, prostate, breast, and skin. The development of novel drugs targeting Bcl-3 alone or in combination with other therapies can cure these patients or prolong their survival. As a proof of concept, in the present study, we focused on metastatic melanoma as a model system. High-throughput screening and in vitro experiments identified BCL3ANT as a lead molecule that could interfere with Bcl-3-mediated cyclin D1 expression and cell proliferation and migration in melanoma. In experimental animal models of melanoma, it was demonstrated that the use of a Bcl-3 inhibitor can influence the survival of melanoma cells. Since there are no other inhibitors against Bcl-3 in the clinical pipeline for cancer treatment, this presents a unique opportunity to develop a highly specific drug against malignant melanoma to meet an urgent clinical need.</p>}},
author = {{Saamarthy, Karunakar and Ahlqvist, Kristofer and Daams, Renée and Balagunaseelan, Navisraj and Rinaldo-Matthis, Agnes and Kazi, Julhash U. and Sime, Wondossen and Massoumi, Ramin}},
issn = {{1471-2407}},
keywords = {{Bcl-3; Cyclin D1; Melanoma; Proliferation}},
language = {{eng}},
number = {{1}},
publisher = {{BioMed Central (BMC)}},
series = {{BMC Cancer}},
title = {{Discovery of a small molecule that inhibits Bcl-3-mediated cyclin D1 expression in melanoma cells}},
url = {{http://dx.doi.org/10.1186/s12885-023-11663-y}},
doi = {{10.1186/s12885-023-11663-y}},
volume = {{24}},
year = {{2024}},
}