Publications

Protectan Technology: Entolimod (CBLB502) & CBLB612

1. Brackett CM, Koiouharov B, Veith J, Greene KF, Burdelya LG, Gollnick SO, Abrams SI, Gudkov AV. 2015 Toll-like receptor-5 agonist, entolimod, suppresses metastasis and induces immunity by stimulating an NK-dendritic-CD8+ T-cell axis. PNAS 2016 Feb 1. pii: 201521359. (PMID: 26831100)

2. Yang H, Brackett C, Morales-Tirado V, Li Z, Zhang Q, Wilson M, Benjamin C, Harris W, Waller V, Gudkov AV, Burdelya L, Grossniklaus H. 2015 The toll-like receptor 5 agonist entolimod suppresses hepatic metastases in a murine model of ocular melanoma via an NK cell-dependent mechanism. Oncotarget 2015 Dec 8. doi: 10.18632/oncotarget.6500

3. Krivokrysenko V, Toshkov I, Gleiberman A, Krasnov P, Shyshynova I, Bespalov I, Maitra R, Narizhneva N, Singh V, Whitnall M, Purmal A, Shakhov A, Gudkov AV, Feinstein E. 2015. The Toll-Like Receptor 5 Agonist Entolimod Mitigates Lethal Acute Radiation Syndrome in Non-Human Primates. PLoS One Sep 15;10(9):e0135388. doi: 10.1371/journal.pone.0135388 (PMCID: PMC4569586)

4. Leigh ND, Bian G, Ding X, Liu H, Aygun-Sunar S, Burdelya LG, Gudkov AV, Cao X. 2014. A Flagellin-Derived Toll-Like Receptor 5 Agonist Stimulates Cytotoxic Lymphocyte-Mediated Tumor Immunity. PLoS One Jan 14;9(1):e85587. doi: 10.1371/journal.pone.0085587. eCollection 2014. (PMID: 24454895)

5. Kojouharov BM, Brackett CM, Veith JM, Johnson CP, Gitlin II, Toshkov IA, Gleiberman AS,Gudkov AV, Burdelya LG. 2014. Toll-like receptor-5 agonist Entolimod broadens the therapeutic window of 5-fluorouracil by reducing its toxicity to normal tissues in mice. Oncotarget. Feb 15;5(3):802-14.. (PMID:24583651)

6. Chow CP, Faqi AS. Developmental toxicity study of CBLB502 in Wistar rats. Reprod Toxicol. 2014 Jul;46:12-9. doi: 10.1016/j.reprotox.2014.02.007. Epub 2014 Mar 3. (PMID: 24602561)

7. Burdelya LG, Brackett CM, Kojouharov B, Gitlin II, Leonova KI, Gleiberman AS, Aygun-Sunar S, Veith J, Johnson C, Haderski GJ, Stanhope-Baker P, Allamaneni S, Skitzki J, Zeng M, Martsen E, Medvedev A, Scheblyakov D, Artemicheva NM, Logunov DY, Gintsburg AL, Naroditsky BS, Makarov SS, Gudkov AV. 2013.Central role of liver in anticancer and radioprotective activities of Toll-like receptor 5 agonist. Proceedings of the National Academy of Science. 2013 May 14;110(20):E1857-66. doi: 10.1073/pnas.1222805110. Epub 2013 Apr 29. (PMID: 23630282)

8. Ding X, Bian G, Leigh ND, Qiu J, McCarthy PL, Liu H, Aygun-Sunar S, Burdelya LG, Gudkov AV, Cao X., 2012.A TLR5 Agonist Enhances CD8+ T Cell-Mediated Graft-versus-Tumor Effect without Exacerbating Graft-versus-Host Disease. J Immunol 189(10):4719-4727. doi: 10.4049/jimmunol.1201206. Epub 2012 Oct 8 (PMID: 23045613)

9. Krivokrysenko V, Shakhov A, Singh V, Bone F, Kononov Y, Shyshynova I, Cheney A, Maitra R, Purmal A, Whitnall M, Gudkov AV, Feinstein E., 2012. Identification of G-CSF and IL-6 as Candidate Biomarkers of CBLB502 Efficacy as a Medical Radiation Countermeasure. Journal Pharmacology and Experimental Therapeutics July 26 (e-pub ahead of print) (PMID: 22837010)

10. Yoon SI, Kurnasov O, Natarajan V, Hong M, Gudkov AV, Osterman AL, Wilson IA., 2012. Structural Basis of TLR5-Flagellin Recognition and Signaling. Science 335:859-864 (PMID: 22344444)

• Mueller, K., 2012. Flagellin Takes Its Toll. Science. Editor’s Choice 5:212 p ec62

11. Singh VK, Ducey EJ, Fatanmi OO, Singh PK, Brown DS, Purmal A, Shakhova VV, Gudkov AV, Feinstein E, Shakhov A., 2012. CBLB613: A TLR2/6 agonist, natural lipopeptide of Mycoplasma arginini, as a novel radiation countermeasure. Radiation Research 177, 628-642 (PMID: 22175300)

12. Shakhov AN, Singh VK, Bone F, Cheney A, Kononov Y, Krasnov P, Bratanova-Toshkova TK, Shakhova VV, Young J, Weil MM, Panoskaltsis-Mortari A, Orschell CM, Baker PS, Gudkov A, Feinstein E.,2012. Prevention and mitigation of acute radiation syndrome in mice by synthetic lipopeptide agonists of Toll-like receptor 2 (TLR2). PLoS One, 7(3):e33044. Epub 2012 Mar 27(PMID: 22479357)

13. Burdelya LG, Gleiberman AS, Toshkov I, Aygun-Sunar S, Bapardekar M, Manderscheid-Kern P, Bellnier D, Krivokrysenko VI, Feinstein E, Gudkov AV., 2011. Toll-like Receptor 5 Agonist Protects Mice from Dermatitis and Oral Mucositis Caused by Local Radiation: Implications for Head-and-Neck Cancer Radiotherapy. International Journal of Radiation Oncology, Biology and Physics, Oct.14 (e-pub ahead of print) (PMID: 22000579)

14. Fukuzawa N, Petro M, Baldwin WM 3rd, Gudkov AV, Fairchild RL., 2011. A TLR5 agonist inhibits acute renal ischemic failure. Journal of Immunology 187: 3831-3839 (PMID: 21890657)

15. Burdelya LG, Krivokrysenko VI, Tallant TC, Strom E, Gleiberman AS, Gupta D, Kurnasov OV, Fort FL, Osterman AL, Didonato JA, Feinstein E, Gudkov AV., 2008. An agonist of Toll-like receptor 5 has radioprotective activity in mouse and primate models. Science 320:226-230 (PMID: 18403709)

Other Supporting Publications

16. Howell BA, Siler SQ, Shoda LK, Yang Y, Woodhead JL, Watkins PB. A mechanistic model of drug-induced liver injury AIDS the interpretation of elevated liver transaminase levels in a phase I clinical trial. CPT Pharmacometrics Syst Pharmacol. 2014 Feb 5;3:e98. doi: 10.1038/psp.2013.74. (PMID: 24500662)

17. Chen H, Wang ZD, Chen MS, Zhang XQ, Shen LP, Zhang JX, Chen Y. Activation of Toll-like receptors by intestinal microflora reduces radiation-induced DNA damage in mice. Mutat Res Genet Toxicol Environ Mutagen. 2014 Nov 1;774:22-8. doi:10.1016/j.mrgentox.2014.09.001. Epub 2014 Sep 16. (PMID: 25440907)

18. Hossain MS, Ramachandiran S, Gewirtz AT, Waller EK. Recombinant TLR5 agonist CBLB502 promotes NK cell-mediated anti-CMV immunity in mice. PLoS One. 2014 May 30;9(5):e96165. doi: 10.1371/journal.pone.0096165. eCollection 2014. (PMID: 24879439)

19. Lu J., Sun PD. 2012. The Structure of the TLR5-Flagellin Complex: A New Mode of Pathogen Detection, Conserved Receptor Dimerization for Signaling. Science Signaling 5, (pe 11) (PMID: 22434932)

20. Cai Z, Sanchez A, Shi Z, Zhang T, Liu M, Zhang D., 2011. Activation of Toll-like Receptor 5 on Breast Cancer Cells by Flagellin Suppresses Cell Proliferation and Tumor Growth. Cancer Research DOI:10.1158/0008-5472.CAN-10-1993 (PMID: 21427357)

21, Gudkov AV, Komarova EA. 2010. Pathologies associated with the p53 response. Cold Spring Harb Perspect Biol. 2(7):a001180. 2(7):a001180. Epub 2010 Apr 7 (PMID: 20595398)

22. Bhattacharjee, Y. 2008. Medicine. Drug bestows radiation resistance on mice and monkeys. Science 320:163 (PMID: 18403680)

23. Strom E, Sathe S, Komarov PG, Chernova OB, Pavlovska I, Shyshynova I, Bosykh DA, Burdelya LG, Macklis RM, Skaliter R, Komarova EA, Gudkov AV., 2006. Small molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. Nature Chemical Biology, 2006 July 23; 2(7): 1-5 (PMID: 16862141)

24. Komarova EA, Kondratov RV, Wang K, Christov K, Golovkina TV, Goldblum JR, Gudkov AV., 2004. Dual effect of p53 on radiation sensitivity in vivo: p53 promotes hematopoietic injury, but protects from gastro-intestinal syndrome in mice. Oncogene 23(2): 3265-3271 (PMID: 15064735)

25. Komarov PG, Komarova EA, Kondratov RV, Christov-Tselkov K, Coon JS, Chernov MV, Gudkov AV., 1999. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science, 285(2): 1733-1737 (PMID: 10481009)

Curaxin Technology: CBL0137 & Predecessor

26. Burkhart C, Fleyshman D, Kohrn R, Commane M, Garrigan J, Kurbatov V, Toshkov I, Ramachandran R, Martello L, Gurova KV. 2014. Curaxin CBL0137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer. Oncotarget Nov 30;5(22):11038-53. (PMID: 25402820)

27. Garcia H, Miecznikowski JC, Safina A, Commane M, Ruusulehto A, Kilpinen S, Leach RW, Attwood K, Li Y, Degan S, Omilian AR, Guryanova O, Papantonopoulou O, Wang J, Buck M, Liu S, Morrison C, Gurova KV, 2013. Facilitates Chromatin Transcription Complex Is an “Accelerator” of Tumor Transformation and Potential Marker and Target of Aggressive Cancers. Cell Reports. Jul 2. pii: S2211-1247(13)00291-X. doi: 10.1016/j.celrep.2013.06.013. (PMID: 23831030)

28. Koman IE, Commane M, Paszkiewicz G, Hoonjan B, Pal S, Safina A, Toshkov I, Purmal AA, Wang D, Liu S, Morrison C, Gudkov AV and Gurova KV., 2012. Targeting FACT Complex Suppresses Mammary Tumorigenesis in Her2/neu Transgenic Mice. Cancer Prevention Research, Aug;5(8):1025-35. (PMID:22689915)

29. Gasparian AV, Burkhart CA, Purmal AA, Brodsky L, Pal M, Saranadasa M, Bosykh DA, Commane M, Guryanova OA, Pal S, Safina A, Sviridov S, Koman IE, Veith J, Komar AA, Gudkov AV, Gurova KV., 2011.Curaxins: Anticancer Compounds that Simultaneously Suppress Nf-kB and Activate p53 by Targeting FACT. Science Translational Medicine 3(95):95ra72 (PMID: 21832239)

30. Gudkov AV, Gurova KV, Komarova EA. Inflammation and p53: A Tale of Two Stresses. Genes Cancer. 2011 Apr;2(4):503-16 (PMID: 21779518)

31. Neznanov N, Gorbachev AV, Neznanova L, Komarov AP, Gurova KV, Gasparian AV, Banerjee AK, Almasan A, Fairchild RL, Gudkov AV., 2009. Anti-malaria drug blocks proteotoxic stress response: anti-cancer implications. Cell Cycle 8(23):3960-3970 (PMID: 19901558)

32. Guo C, Gasparian AV, Zhuang Z, Bosykh DA, Komar AA, Gudkov AV, Gurova KV., et al., 2009.9Aminoacridine-based anticancer drugs target the PI3K/AKT/mTOR, NF-kappaB and p53 pathways. Oncogene 28(8): 1151-1161 (PMID: 19137016)

33. Gurova KV, Hill JE, Guo C, Prokvolit A, Burdelya LG, Samoylova E, Khodyakova AV, Ganapathi R, Ganapathi M, Tararova ND, Bosykh D, Lvovskiy D, Webb TR, Stark GR, Gudkov AV., 2005. Small molecules that reactivate p53 in renal cell carcinoma reveal a NF-kappaB-dependent mechanism of p53 suppression in tumors. Proceedings of the National Academy of Science 102(48):17448-17453 (PMID: 16287968)

Other Supporting Publications

34. Draetta GF, Depinho RA. 2011. Cancer drug discovery faces the FACT. Science Translational Medicine 3(95):95ps34 (PMID: 21832237)

35. Gasparian AV, Neznanov N, Jha S, Galkin O, Moran JJ, Gudkov AV, Gurova KV, Komar AA., 2010. Inhibition of encephalomyocarditis virus and poliovirus replication by quinacrine: implications for the design and discovery of novel antiviral drugs. Journal of Virology 84 (18): 9390-9397 (PMID: 20631142)

36. Mollapour M, Neckers L., 2010. Quinacrine: New anti-tumor application for an old anti-malaria drug. Cell Cycle 9(2):228. Epub 2010 Jan 15. (PMID: 20061796)

37. Chau CH, Figg WD., 2009. New tricks from an old drug: a role for quinacrine in anti-cancer therapy? Cell Cycle 8(24):4024-5. Epub 2009 Dec 15. (PMID: 19959937)

38. Dai C, Whitesell L, Rogers AB, Lindquist S., 2007. Heat Shock Factor 1 Is a Powerful Multifaceted Modifier of Carcinogenesis. Cell 130: 1005-1018 (PMID: 17889646)

39. Boiko AD, Porteous S, Razorenova OV, Krivokrysenko VI, Williams BR, Gudkov AV., 2006. A systematic search for downstream mediators of tumor suppressor function of p53 reveals a major role of BTG2 in suppression of Ras-induced transformation. Genes & Development 20(2):236-52 (PMID: 16418486)

40. Komarova EA, Krivokrysenko V, Wang K, Neznanov N, Chernov MV, Komarov PG, Brennan ML, Golovkina TV, Rokhlin OW, Kuprash DV, Nedospasov SA, Hazen SL, Feinstein E, Gudkov AV., 2005. p53 is a suppressor of inflammatory response in mice. FASEB Journal 19(8):1030-1032 (PMID: 15811878) http://www.ncbi.nlm.nih.gov/pubmed/15811878

41. Gudkov AV, Komarova EA., 2005. Prospective therapeutic applications of p53 inhibitors. Biochemical and Biophysical Research Communications 331(1): 726-736 (PMID: 15865929)

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