K-Ras4B/calmodulin/PI3Kα: A promising new adenocarcinoma-specific drug target?

Gursoy, Attila; Muratcioglu, Serena; Keskin, Ozlem; Nussinov, Ruth; Tsai, Chung-Jung; Jang, Hyunbum

doi:10.1517/14728222.2016.1135131

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K-Ras4B/calmodulin/PI3Kα: A promising new adenocarcinoma-specific drug target?

Author(s): Ruth Nussinov ¹ ^, ² , Serena Muratcioglu ³ , Chung-Jung Tsai ¹ , Hyunbum Jang ¹ , Attila Gursoy ⁴ , Ozlem Keskin ³

Publication date (Electronic): Jul 2016

Journal: Expert opinion on therapeutic targets

Publisher: Informa Healthcare

Keywords: K-Ras dimers, KRAS, KRAS4A, KRAS4B, allosteric drugs, calcium, calmodulin, colorectal cancer, lung cancer, orthosteric drugs, pancreatic cancer, pancreatic ductal adenocarcinomas (PDAC), small molecule drug

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Abstract

Decades of efforts have yet to yield a safe and effective drug to target KRAS-driven pancreatic, colorectal and lung cancers; particularly those driven by the highly oncogenic splice variant KRAS4B. K-Ras4B's fairly smooth surface, cancer tissue/cell heterogeneity, tolerated lipid post-translational modification exchange, as well as drug-elicited toxicity present a daunting challenge.

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Journal ID (iso-abbrev): Expert Opin. Ther. Targets

Title: Expert opinion on therapeutic targets

Publisher: Informa Healthcare

ISSN (Electronic): 1744-7631

ISSN (Print): 1472-8222

Publication date (Electronic): Jul 2016

Volume: 20

Issue: 7

Affiliations

[1 ] a Cancer and Inflammation Program, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research , National Cancer Institute at Frederick , Frederick , MD , USA.

[2 ] b Department of Human Molecular Genetics and Biochemistry, Sackler School of Medicine , Tel Aviv University , Tel Aviv , Israel.

[3 ] c Department of Chemical and Biological Engineering , Koc University , Istanbul , Turkey.

[4 ] d Department of Computer Engineering , Koc University , Istanbul , Turkey.

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DOI: 10.1517/14728222.2016.1135131

PubMed ID: 26873344

SO-VID: c2c802de-0c91-4d50-bad8-622e940aea19

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Keywords: KRAS4B,pancreatic ductal adenocarcinomas (PDAC),pancreatic cancer,KRAS,lung cancer,calcium,small molecule drug,K-Ras dimers,orthosteric drugs,colorectal cancer,calmodulin,KRAS4A,allosteric drugs

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Keywords: KRAS4B, pancreatic ductal adenocarcinomas (PDAC), pancreatic cancer, KRAS, lung cancer, calcium, small molecule drug, K-Ras dimers, orthosteric drugs, colorectal cancer, calmodulin, KRAS4A, allosteric drugs

K-Ras4B/calmodulin/PI3Kα: A promising new adenocarcinoma-specific drug target?

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