Выходит 4 номеров в год
ISSN Печать: 0893-9675
ISSN Онлайн: 2162-6448
Indexed in
Src Kinase Inhibitors: Promising Cancer Therapeutics?
Краткое описание
Src is the cellular counterpart of the first identified viral oncogene v-Src. It forms part of a large family of nonreceptor tyrosine kinases that have been extensively studied over the last few decades. This has led to the realization that Src can regulate a number of signaling pathways that impact on the behavior of tumor cells, including proliferation, survival, migration, invasion, and angiogenesis. There are currently four Src inhibitors (dasatinib, saracatinib, bosutinib, and KX01) in clinical development, and although there is a plethora of information on their activity in preclinical models their clinical efficacy has been disappointing. Here we review the current status of the Src inhibitors and highlight the difficulties involved in assessing these therapeutics in the clinical setting. In the future it will be important to combine our knowledge of basic Src biology with the use of appropriate preclinical models to aid the design of clinical trials. Taking this integrated approach will hopefully help to realize the true potential of Src kinase inhibitors.
-
Hebert-Chatelain Etienne, Src kinases are important regulators of mitochondrial functions, The International Journal of Biochemistry & Cell Biology, 45, 1, 2013. Crossref
-
Zámečníkova Adriana, Novel approaches to the development of tyrosine kinase inhibitors and their role in the fight against cancer, Expert Opinion on Drug Discovery, 9, 1, 2014. Crossref
-
De Luca Antonella, D'Alessio Amelia, Gallo Marianna, Maiello Monica, Bode Ann, Normanno Nicola, Src and CXCR4 are involved in the invasiveness of breast cancer cells with acquired resistance to lapatinib, Cell Cycle, 13, 1, 2014. Crossref
-
Witkowski Wojciech, Verhasselt Bruno, Contributions of HIV-1 Nef to immune dysregulation in HIV-infected patients: a therapeutic target?, Expert Opinion on Therapeutic Targets, 17, 11, 2013. Crossref
-
Karim Saadia A, Creedon Helen, Patel Hitesh, Carragher Neil O, Morton Jennifer P, Muller William J, Evans Thomas RJ, Gusterson Barry, Sansom Owen J, Brunton Valerie G, Dasatinib inhibits mammary tumour development in a genetically engineered mouse model, The Journal of Pathology, 230, 4, 2013. Crossref
-
Liu Lucy, Gaboriaud Nicolas, Vougogianopoulou Konstantina, Tian Yan, Wu Jun, Wen Wei, Skaltsounis Leandros, Jove Richard, MLS-2384, a new 6-bromoindirubin derivative with dual JAK/Src kinase inhibitory activity, suppresses growth of diverse cancer cells, Cancer Biology & Therapy, 15, 2, 2014. Crossref
-
Riemann Anne, Schneider Bettina, Gündel Daniel, Stock Christian, Thews Oliver, Gekle Michael, Acidic priming enhances metastatic potential of cancer cells, Pflügers Archiv - European Journal of Physiology, 466, 11, 2014. Crossref
-
Senis Yotis A., Mazharian Alexandra, Mori Jun, Src family kinases: at the forefront of platelet activation, Blood, 124, 13, 2014. Crossref
-
Ali Naveid A, Wu Jianmin, Hochgräfe Falko, Chan Howard, Nair Radhika, Ye Sunny, Zhang Luxi, Lyons Ruth J, Pinese Mark, Lee Hong Ching, Armstrong Nicola, Ormandy Christopher J, Clark Susan J, Swarbrick Alexander, Daly Roger J, Profiling the tyrosine phosphoproteome of different mouse mammary tumour models reveals distinct, model-specific signalling networks and conserved oncogenic pathways, Breast Cancer Research, 16, 5, 2014. Crossref
-
Yan Yanli, Ma Li, Zhou Xiaoxu, Ponnusamy Murugavel, Tang Jinhua, Zhuang Michelle A., Tolbert Evelyn, Bayliss Georgia, Bai Jianwen, Zhuang Shougang, Src inhibition blocks renal interstitial fibroblast activation and ameliorates renal fibrosis, Kidney International, 89, 1, 2016. Crossref
-
Hsu Yu-Ling, Yang Chun-Chieh, Chou Tzyy-Chao, Tai Chih-Hsuan, Chen Long-Yuan, Fu Shu-Ling, Lin Jing-Jer, Lo Lee-Chiang, Design, synthesis, and evaluation of cell permeable probes for protein kinases, Tetrahedron, 72, 1, 2016. Crossref
-
Cui Zhishan, Li Xi, Li Lulu, Zhang Bin, Gao Chunmei, Chen Yuzong, Tan Chunyan, Liu Hongxia, Xie Weiyi, Yang Ti, Jiang Yuyang, Design, synthesis and evaluation of acridine derivatives as multi-target Src and MEK kinase inhibitors for anti-tumor treatment, Bioorganic & Medicinal Chemistry, 24, 2, 2016. Crossref
-
Robak Tadeusz, Robak Ewa, Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders, Expert Opinion on Investigational Drugs, 21, 7, 2012. Crossref
-
Ismail Nasser S.M., Ali Eslam M.H., Ibrahim Diaa A., Serya Rabah A.T., Abou El Ella Dalal A., Pyrazolo[3,4-d]pyrimidine based scaffold derivatives targeting kinases as anticancer agents, Future Journal of Pharmaceutical Sciences, 2, 1, 2016. Crossref
-
Weir Marion E., Mann Jacqueline E., Corwin Thomas, Fulton Zachary W., Hao Jennifer M., Maniscalco Jeanine F., Kenney Marie C., Roman Roque Kristal M., Chapdelaine Elizabeth F., Stelzl Ulrich, Deming Paula B., Ballif Bryan A., Hinkle Karen L., Novel autophosphorylation sites of Src family kinases regulate kinase activity and SH 2 domain‐binding capacity , FEBS Letters, 590, 8, 2016. Crossref
-
CHEN QUANCHI, ZHOU ZIFEI, SHAN LIANCHENG, ZENG HUI, HUA YINGQI, CAI ZHENGDONG, The importance of Src signaling in sarcoma, Oncology Letters, 10, 1, 2015. Crossref
-
Young Adelaide I. J., Law Andrew M. K., Castillo Lesley, Chong Sabrina, Cullen Hayley D., Koehler Martin, Herzog Sebastian, Brummer Tilman, Lee Erinna F., Fairlie Walter D., Lucas Morghan C., Herrmann David, Allam Amr, Timpson Paul, Watkins D. Neil, Millar Ewan K. A., O’Toole Sandra A., Gallego-Ortega David, Ormandy Christopher J., Oakes Samantha R., MCL-1 inhibition provides a new way to suppress breast cancer metastasis and increase sensitivity to dasatinib, Breast Cancer Research, 18, 1, 2016. Crossref
-
Qin Sida, Zhang Boxiang, Xiao Guodong, Sun Xin, Li Gang, Huang Guanghong, Gao Xiao, Li Xiang, Wang Huangzhen, Yang Chengcheng, Ren Hong, Fibronectin protects lung cancer cells against docetaxel-induced apoptosis by promoting Src and caspase-8 phosphorylation, Tumor Biology, 37, 10, 2016. Crossref
-
Powley I R, Hughes M A, Cain K, MacFarlane M, Caspase-8 tyrosine-380 phosphorylation inhibits CD95 DISC function by preventing procaspase-8 maturation and cycling within the complex, Oncogene, 35, 43, 2016. Crossref
-
Padhan Narendra, Nordling Torbjörn E. M., Sundström Magnus, Åkerud Peter, Birgisson Helgi, Nygren Peter, Nelander Sven, Claesson-Welsh Lena, High sensitivity isoelectric focusing to establish a signaling biomarker for the diagnosis of human colorectal cancer, BMC Cancer, 16, 1, 2016. Crossref
-
Skhinas Joanna N., Cox Thomas R., The interplay between extracellular matrix remodelling and kinase signalling in cancer progression and metastasis, Cell Adhesion & Migration, 12, 6, 2018. Crossref
-
Wang Jun, Zhuang Shougang, Src family kinases in chronic kidney disease, American Journal of Physiology-Renal Physiology, 313, 3, 2017. Crossref
-
Duff Deirdre, Long Aideen, Roles for RACK1 in cancer cell migration and invasion, Cellular Signalling, 35, 2017. Crossref
-
Zhang Jay, Tyagi Anil Kumar, Transcriptome Analysis Reveals Novel Entry Mechanisms and a Central Role of SRC in Host Defense during High Multiplicity Mycobacterial Infection, PLoS ONE, 8, 6, 2013. Crossref
-
PENG RENJUN, JIANG BING, MA JIANRONG, MA ZHIMING, WAN XIN, LIU HONGWEI, CHEN ZIGUI, CHENG QUAN, CHEN RUI, Forced downregulation of RACK1 inhibits glioma development by suppressing Src/Akt signaling activity, Oncology Reports, 30, 5, 2013. Crossref
-
Lindauer Markus, Hochhaus Andreas, Dasatinib, in Small Molecules in Hematology, 212, 2018. Crossref
-
Ly Tony, Endo Aki, Brenes Alejandro, Gierlinski Marek, Afzal Vackar, Pawellek Andrea, Lamond Angus I., Proteome-wide analysis of protein abundance and turnover remodelling during oncogenic transformation of human breast epithelial cells, Wellcome Open Research, 3, 2018. Crossref
-
Betapudi Venkaiah, Shukla Meenal, Alluri Ravi, Merkulov Sergei, McCrae Keith R., Novel role for p56/Lck in regulation of endothelial cell survival and angiogenesis, The FASEB Journal, 30, 10, 2016. Crossref
-
Elbediwy A., Vincent-Mistiaen Z. I., Spencer-Dene B., Stone R. K., Boeing S., Wculek S. K., Cordero J., Tan E. H., Ridgway R., Brunton V. G., Sahai E., Gerhardt H., Behrens A., Malanchi I., Sansom O. J., Thompson B. J., Integrin signalling regulates YAP/TAZ to control skin homeostasis, Development, 2016. Crossref
-
Barneh Farnaz, Mirzaie Mehdi, Nickchi Payman, Tan Tuan Zea, Thiery Jean Paul, Piran Mehran, Salimi Mona, Goshadrou Fatemeh, Aref Amir R, Jafari Mohieddin, Integrated use of bioinformatic resources reveals that co-targeting of histone deacetylases, IKBK and SRC inhibits epithelial-mesenchymal transition in cancer, Briefings in Bioinformatics, 20, 2, 2019. Crossref
-
Collins Ross J., Morgan Liam D., Owen Sioned, Ruge Fiona, Jiang Wen G., Sanders Andrew J., Mechanistic insights of epithelial protein lost in neoplasm in prostate cancer metastasis, International Journal of Cancer, 143, 10, 2018. Crossref
-
Hermida-Prado Francisco, Granda-Díaz Rocío, del-Río-Ibisate Nagore, Villaronga M. Ángeles, Allonca Eva, Garmendia Irati, Montuenga Luis M., Rodríguez René, Vallina Aitana, Alvarez-Marcos César, Rodrigo Juan P., García-Pedrero Juana M., The Differential Impact of SRC Expression on the Prognosis of Patients with Head and Neck Squamous Cell Carcinoma, Cancers, 11, 11, 2019. Crossref
-
Xiao Xiang, Mruk Dolores D., Jenardhanan Pranitha, Mannu Jayakanthan, Mathur Premendu P., Lee Will M., Silvestrini Bruno, Cheng Yan-ho, Cheng C. Y., Nonreceptor Protein Kinases c-Src, c-Yes, and FAK Are Biomarkers for Male Contraceptive Research, in New Advances on Disease Biomarkers and Molecular Targets in Biomedicine, 2013. Crossref
-
Hermida-Prado Francisco, Villaronga M. Ángeles, Granda-Díaz Rocío, del-Río-Ibisate Nagore, Santos Laura, Hermosilla Maria Ana, Oro Patricia, Allonca Eva, Agorreta Jackeline, Garmendia Irati, Tornín Juan, Perez-Escuredo Jhudit, Fuente Rocío, Montuenga Luis M., Morís Francisco, Rodrigo Juan P., Rodríguez René, García-Pedrero Juana M., The SRC Inhibitor Dasatinib Induces Stem Cell-Like Properties in Head and Neck Cancer Cells that are Effectively Counteracted by the Mithralog EC-8042, Journal of Clinical Medicine, 8, 8, 2019. Crossref
-
Ma Xiuquan, Zhang Luxi, Song Jiangning, Nguyen Elizabeth, Lee Rachel S., Rodgers Samuel J., Li Fuyi, Huang Cheng, Schittenhelm Ralf B., Chan Howard, Chheang Chanly, Wu Jianmin, Brown Kristin K., Mitchell Christina A., Simpson Kaylene J., Daly Roger J., Characterization of the Src-regulated kinome identifies SGK1 as a key mediator of Src-induced transformation, Nature Communications, 10, 1, 2019. Crossref
-
Castillo Lesley, Young Adelaide I. J., Mawson Amanda, Schafranek Pia, Steinmann Angela M., Nessem Danielle, Parkin Ashleigh, Johns Amber, Chou Angela, Law Andrew M. K., Lucas Morghan C., Murphy Kendelle J., Deng Niantao, Gallego-Ortega David, Caldon Catherine E., Timpson Paul, Pajic Marina, Ormandy Christopher J., Oakes Samantha R., MCL-1 antagonism enhances the anti-invasive effects of dasatinib in pancreatic adenocarcinoma, Oncogene, 39, 8, 2020. Crossref
-
Hawkins Allegra G., Julian Claire M., Konzen Sonja, Treichel Sydney, Lawlor Elizabeth R., Bailey Kelly M., Microenvironmental Factors Drive Tenascin C and Src Cooperation to Promote Invadopodia Formation in Ewing Sarcoma, Neoplasia, 21, 10, 2019. Crossref
-
Wang Jun, Wang Li, Xu Liuqing, Shi Yingfeng, Liu Feng, Qi Hualin, Liu Na, Zhuang Shougang, Targeting Src attenuates peritoneal fibrosis and inhibits the epithelial to mesenchymal transition, Oncotarget, 8, 48, 2017. Crossref
-
Kobelt Dennis, Dahlmann Mathias, Dumbani Malti, Güllü Nazli, Kortüm Benedikt, Vílchez Miguel E. Alberto, Stein Ulrike, Walther Wolfgang, Small Ones to Fight a Big Problem—Intervention of Cancer Metastasis by Small Molecules, Cancers, 12, 6, 2020. Crossref
-
Lin Li-Fang, Wu Ming-Hsi, Pidugu Vijaya Kumar, Ho I-Ching, Su Tsann-Long, Lee Te-Chang, P-glycoprotein attenuates DNA repair activity in multidrug-resistant cells by acting through the Cbp-Csk-Src cascade, Oncotarget, 8, 28, 2017. Crossref
-
Wu Qianhui, Finley Stacey D., Mathematical Model Predicts Effective Strategies to Inhibit VEGF-eNOS Signaling, Journal of Clinical Medicine, 9, 5, 2020. Crossref
-
Wang Xin, Ren Rui, Xu Zehui, Huang Haidi, Jiang Wanglin, Ma Jinbo, Tirbanibulin Attenuates Pulmonary Fibrosis by Modulating Src/STAT3 Signaling, Frontiers in Pharmacology, 12, 2021. Crossref
-
Fraser Craig, Dawson John C., Dowling Reece, Houston Douglas R., Weiss Jason T., Munro Alison F., Muir Morwenna, Harrington Lea, Webster Scott P., Frame Margaret C., Brunton Valerie G., Patton E. Elizabeth, Carragher Neil O., Unciti-Broceta Asier, Rapid Discovery and Structure–Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase, Journal of Medicinal Chemistry, 59, 10, 2016. Crossref
-
Schepetkin Igor A., Plotnikov Mark B., Khlebnikov Andrei I., Plotnikova Tatiana M., Quinn Mark T., Oximes: Novel Therapeutics with Anticancer and Anti-Inflammatory Potential, Biomolecules, 11, 6, 2021. Crossref
-
Canel Marta, Serrels Alan, Frame Margaret C., Brunton Valerie G., E-cadherin–integrin crosstalk in cancer invasion and metastasis, Journal of Cell Science, 126, 2, 2013. Crossref
-
Hen Omri, Barkan Dalit, Dormant disseminated tumor cells and cancer stem/progenitor-like cells: Similarities and opportunities, Seminars in Cancer Biology, 60, 2020. Crossref
-
Catara Giuliana, Colanzi Antonino, Spano Daniela, Combinatorial Strategies to Target Molecular and Signaling Pathways to Disarm Cancer Stem Cells, Frontiers in Oncology, 11, 2021. Crossref
-
Polasky Daniel A., Dixit Sugyan M., Vallejo Daniel D., Kulju Kathryn D., Ruotolo Brandon T., An Algorithm for Building Multi-State Classifiers Based on Collision-Induced Unfolding Data, Analytical Chemistry, 91, 16, 2019. Crossref
-
Reynolds A B, Kanner S B, Bouton A H, Schaller M D, Weed S A, Flynn D C, Parsons J T, SRChing for the substrates of Src, Oncogene, 33, 37, 2014. Crossref
-
Su Shih-Ping, Flashner-Abramson Efrat, Klein Shoshana, Gal Mor, Lee Rachel S., Wu Jianmin, Levitzki Alexander, Daly Roger J., Impact of the Anticancer Drug NT157 on Tyrosine Kinase Signaling Networks, Molecular Cancer Therapeutics, 17, 5, 2018. Crossref
-
Gluschnaider Udi, Hertz Rachel, Ohayon Sarit, Smeir Elia, Smets Martha, Pikarsky Eli, Bar-Tana Jacob, Long-Chain Fatty Acid Analogues Suppress Breast Tumorigenesis and Progression, Cancer Research, 74, 23, 2014. Crossref
-
Chakrabarti Kristi R., Hessler Lindsay, Bhandary Lekhana, Martin Stuart S., Molecular Pathways: New Signaling Considerations When Targeting Cytoskeletal Balance to Reduce Tumor Growth, Clinical Cancer Research, 21, 23, 2015. Crossref
-
Cook D R, Rossman K L, Der C J, Rho guanine nucleotide exchange factors: regulators of Rho GTPase activity in development and disease, Oncogene, 33, 31, 2014. Crossref
-
Adan Hanad, Guy Stephanie, Arulanandam Rozanne, Geletu Mulu, Daniel Juliet, Raptis Leda, Activated Src requires Cadherin-11, Rac, and gp130 for Stat3 activation and survival of mouse Balb/c3T3 fibroblasts, Cancer Gene Therapy, 2022. Crossref
-
Toyokuni Shinya, Genotoxicity and carcinogenicity risk of carbon nanotubes, Advanced Drug Delivery Reviews, 65, 15, 2013. Crossref
-
Kegelman Timothy P., Wu Bainan, Das Swadesh K., Talukdar Sarmistha, Beckta Jason M., Hu Bin, Emdad Luni, Valerie Kristoffer, Sarkar Devanand, Furnari Frank B., Cavenee Webster K., Wei Jun, Purves Angela, De Surya K., Pellecchia Maurizio, Fisher Paul B., Inhibition of radiation-induced glioblastoma invasion by genetic and pharmacological targeting of MDA-9/Syntenin, Proceedings of the National Academy of Sciences, 114, 2, 2017. Crossref
-
Shen Pei, Wang Yezhi, Jia Xiangxiang, Xu Pengfei, Qin Lian, Feng Xi, Li Zhiyu, Qiu Zhixia, Dual-target Janus kinase (JAK) inhibitors: Comprehensive review on the JAK-based strategies for treating solid or hematological malignancies and immune-related diseases, European Journal of Medicinal Chemistry, 239, 2022. Crossref
-
Beetham Henry, Griffith Billie G.C., Murina Olga, Loftus Alexander E.P., Parry David A., Temps Carolin, Culley Jayne, Muir Morwenna, Unciti-Broceta Asier, Sims Andrew H., Byron Adam, Brunton Valerie G., Loss of Integrin-Linked Kinase Sensitizes Breast Cancer to SRC Inhibitors, Cancer Research, 82, 4, 2022. Crossref