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| 001 | 179694 | ||
| 005 | 20240229145551.0 | ||
| 024 | 7 | _ | |a 10.1371/journal.pcbi.1009962 |2 doi |
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| 037 | _ | _ | |a DKFZ-2022-00843 |
| 041 | _ | _ | |a English |
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| 100 | 1 | _ | |a Poorebrahim, Mansour |0 P:(DE-He78)081f0df0551762b7dbb2faabe23023b5 |b 0 |e First author |u dkfz |
| 245 | _ | _ | |a Multi-targeting of K-Ras domains and mutations by peptide and small molecule inhibitors. |
| 260 | _ | _ | |a San Francisco, Calif. |c 2022 |b Public Library of Science |
| 336 | 7 | _ | |a article |2 DRIVER |
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| 336 | 7 | _ | |a Journal Article |0 0 |2 EndNote |
| 500 | _ | _ | |a #EA:D122# |
| 520 | _ | _ | |a K-Ras activating mutations are significantly associated with tumor progression and aggressive metastatic behavior in various human cancers including pancreatic cancer. So far, despite a large number of concerted efforts, targeting of mutant-type K-Ras has not been successful. In this regard, we aimed to target this oncogene by a combinational approach consisting of small peptide and small molecule inhibitors. Based on a comprehensive analysis of structural and physicochemical properties of predominantly K-Ras mutants, an anti-cancer peptide library and a small molecule library were screened to simultaneously target oncogenic mutations and functional domains of mutant-type K-Ras located in the P-loop, switch I, and switch II regions. The selected peptide and small molecule showed notable binding affinities to their corresponding binding sites, and hindered the growth of tumor cells carrying K-RasG12D and K-RasG12C mutations. Of note, the expression of K-Ras downstream genes (i.e., CTNNB1, CCND1) was diminished in the treated Kras-positive cells. In conclusion, our combinational platform signifies a new potential for blockade of oncogenic K-Ras and thereby prevention of tumor progression and metastasis. However, further validations are still required regarding the in vitro and in vivo efficacy and safety of this approach. |
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| 700 | 1 | _ | |a Abazari, Mohammad Foad |b 1 |
| 700 | 1 | _ | |a Moradi, Leila |b 2 |
| 700 | 1 | _ | |a Shahbazi, Behzad |b 3 |
| 700 | 1 | _ | |a Mahmoudi, Reza |b 4 |
| 700 | 1 | _ | |a Kalhor, Hourieh |0 0000-0003-0715-294X |b 5 |
| 700 | 1 | _ | |a Askari, Hassan |0 0000-0002-2285-2592 |b 6 |
| 700 | 1 | _ | |a Teimoori-Toolabi, Ladan |0 0000-0002-6588-9774 |b 7 |
| 773 | _ | _ | |a 10.1371/journal.pcbi.1009962 |g Vol. 18, no. 4, p. e1009962 - |0 PERI:(DE-600)2193340-6 |n 4 |p e1009962 - |t PLoS Computational Biology |v 18 |y 2022 |x 1553-734X |
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| 910 | 1 | _ | |a Deutsches Krebsforschungszentrum |0 I:(DE-588b)2036810-0 |k DKFZ |b 0 |6 P:(DE-He78)081f0df0551762b7dbb2faabe23023b5 |
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| 914 | 1 | _ | |y 2022 |
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