Sonoshita M, Scopton AP, Ung PMU, Murray MA, Silber L, Maldonado AY, Real A, Schlessinger A, Cagan RL, Dar AC. A whole-animal platform to advance a clinical kinase inhibitor into new disease space. Nat Chem Biol. 2018 Jan 22. PMID: 29355849.
From the abstract: "Synthetic tailoring of approved drugs for new indications is often difficult ... Here, we report a multidisciplinary approach for accessing novel target and chemical space starting from an FDA-approved kinase inhibitor. By combining chemical and genetic modifier screening with computational modeling, we identify distinct kinases that strongly enhance ('pro-targets') or limit ('anti-targets') whole-animal activity of the clinical kinase inhibitor sorafenib in a Drosophila medullary thyroid carcinoma (MTC) model. ... Through progressive synthetic refinement, we report a new class of 'tumor calibrated inhibitors' with unique polypharmacology and strongly improved therapeutic index in fly and human MTC xenograft models. This platform provides a rational approach to creating new high-efficacy and low-toxicity drugs."
Showing posts with label Thyroid cancer. Show all posts
Showing posts with label Thyroid cancer. Show all posts
Tuesday, January 23, 2018
Monday, June 2, 2014
Recent fly studies and reviews related to cancer
Sechi S, Colotti G, Belloni G, Mattei V, Frappaolo A, Raffa GD, Fuller MT, Giansanti MG. GOLPH3 Is Essential for Contractile Ring Formation and Rab11 Localization to the Cleavage Site during Cytokinesis in Drosophila melanogaster. PLoS Genet. 2014 May 1;10(5):e1004305. PMID: 24786584; PubMed Central PMCID: PMC4006750.
Huo G, Lu J, Qu Z, Lin Z, Zhang D, Yang Y, Li B. [The applications and advantages of Drosophila melanogaster in cancer research]. Yi Chuan. 2014 Jan;36(1):30-40. Chinese. PubMed PMID: 24846916.
Reddy BA, van der Knaap JA, Bot AG, Mohd-Sarip A, Dekkers DH, Timmermans MA, Martens JW, Demmers JA, Verrijzer CP. Nucleotide biosynthetic enzyme GMP synthase is a TRIM21-controlled relay of p53 stabilization. Mol Cell. 2014 Feb 6;53(3):458-70. PMID: 24462112. From the abstract: "... Here, we show that guanosine 5'-monophosphate synthase (GMPS) is required for USP7-mediated stabilization of p53. ... Intriguingly, cytoplasmic sequestration of GMPS requires ubiquitylation by TRIM21, a ubiquitin ligase associated with autoimmune disease. These results implicate a classic nucleotide biosynthetic enzyme and a ubiquitin ligase, better known for its role in autoimmune disease, in p53 control."
Markstein M. Modeling colorectal cancer as a 3-dimensional disease in a dish: the case for drug screening using organoids, zebrafish, and fruit flies. Drug Discov Today Technol. 2013 Spring;10(1):e73-81. PMID: 24050233. From the abstract: "This review discusses recent shifts in the understanding of colorectal cancer ... recent advances in the culturing of colorectal stem cells using mammalian organoids, zebrafish, and Drosophila offer promising avenues for anti-CSC drug discovery."
Das TK, Cagan RL. A Drosophila approach to thyroid cancer therapeutics. Drug Discov Today Technol. 2013 Spring;10(1):e65-71. doi: 10.1016/j.ddtec.2012.09.004. PMID: 24050232; PubMed Central PMCID: PMC3779345. From the abstract: "Thyroid neoplasias represent among the fastest growing cancers. ... recent Drosophila models have proven useful both for understanding disease mechanism as well as helping identify new generation therapeutics"
Lourenço FC, Munro J, Brown J, Cordero J, Stefanatos R, Strathdee K, Orange C, Feller SM, Sansom OJ, Vidal M, Murray GI, Olson MF. Reduced LIMK2 expression in colorectal cancer reflects its role in limiting stem cell proliferation. Gut. 2014 Mar;63(3):480-93. PMID: 23585469; PubMed Central PMCID: PMC3932979.
Huo G, Lu J, Qu Z, Lin Z, Zhang D, Yang Y, Li B. [The applications and advantages of Drosophila melanogaster in cancer research]. Yi Chuan. 2014 Jan;36(1):30-40. Chinese. PubMed PMID: 24846916.
Reddy BA, van der Knaap JA, Bot AG, Mohd-Sarip A, Dekkers DH, Timmermans MA, Martens JW, Demmers JA, Verrijzer CP. Nucleotide biosynthetic enzyme GMP synthase is a TRIM21-controlled relay of p53 stabilization. Mol Cell. 2014 Feb 6;53(3):458-70. PMID: 24462112. From the abstract: "... Here, we show that guanosine 5'-monophosphate synthase (GMPS) is required for USP7-mediated stabilization of p53. ... Intriguingly, cytoplasmic sequestration of GMPS requires ubiquitylation by TRIM21, a ubiquitin ligase associated with autoimmune disease. These results implicate a classic nucleotide biosynthetic enzyme and a ubiquitin ligase, better known for its role in autoimmune disease, in p53 control."
Markstein M. Modeling colorectal cancer as a 3-dimensional disease in a dish: the case for drug screening using organoids, zebrafish, and fruit flies. Drug Discov Today Technol. 2013 Spring;10(1):e73-81. PMID: 24050233. From the abstract: "This review discusses recent shifts in the understanding of colorectal cancer ... recent advances in the culturing of colorectal stem cells using mammalian organoids, zebrafish, and Drosophila offer promising avenues for anti-CSC drug discovery."
Das TK, Cagan RL. A Drosophila approach to thyroid cancer therapeutics. Drug Discov Today Technol. 2013 Spring;10(1):e65-71. doi: 10.1016/j.ddtec.2012.09.004. PMID: 24050232; PubMed Central PMCID: PMC3779345. From the abstract: "Thyroid neoplasias represent among the fastest growing cancers. ... recent Drosophila models have proven useful both for understanding disease mechanism as well as helping identify new generation therapeutics"
Lourenço FC, Munro J, Brown J, Cordero J, Stefanatos R, Strathdee K, Orange C, Feller SM, Sansom OJ, Vidal M, Murray GI, Olson MF. Reduced LIMK2 expression in colorectal cancer reflects its role in limiting stem cell proliferation. Gut. 2014 Mar;63(3):480-93. PMID: 23585469; PubMed Central PMCID: PMC3932979.
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