LDDN Publications

Earlier publications:

Recent publication and patents

Rietz A., Li H., Quist K.M., Cherry J.J., Lorson C.L., Burnett B.G., Kern N.L., Calder A.N., Fritsche M., Lusic H., Boaler P.J., Choi S., Xing X., Glicksman M.A., Cuny G.D., Androphy E.J., Hodgetts K.J. Discovery of a Small Molecule Probe That Post-Translationally Stabilizes the Survival Motor Neuron Protein for the Treatment of Spinal Muscular Atrophy. Journal of Medicinal Chemistry 2017, 60, 4594-4610.

Choi S., Calder A.N., Miller, E.H., Anderson K.P., Fiejtek D.K., Rietz A., Li H., Cherry J.J., Quist K.M., Xing X., Glicksman M.A., Cuny G.D., Lorson C.L., Androphy E.A., Hodgetts K.J. Optimization of a series of heterocycles as survival motor neuron gene transcription enhancers. Bioorganic & Medicinal Chemistry Letters 2017, 27, 5144-5148.

Tarrant J., Hodgetts K.J., Chenard B.L., Krause J., Doller D.: “The Discovery of the MCH-1 Receptor Antagonist NGD-4715 for the Potential Treatment of Obesity” in Comprehensive Medicinal Chemistry, Eds Chackalamannil Rotella and Ward, Elsevier Science 2017. ISBN: 9780128032008.

Cherry J., Calder A., Hodgetts K., Androphy E.: “SMN-upregulating small molecules” in Spinal Muscular Atrophy: Disease Mechanisms and Therapy, Eds. Sumner, Paushkin, and Ko; Academic Press, 2016, Chapter 17, 283-297. ISBN: 9780128036853.

Calder A., Androphy E., Hodgetts K.J. Small Molecules in Development for the Treatment of Spinal Muscular Atrophy. Journal of Medicinal Chemistry 2016, 59, 10067–10083.

Takahashi K, Kong Q, Lin Y, Stouffer N, Schulte DA, Lai L, Liu Q, Chang l, Dominguez S, Xing X, Cuny GD, Hodgetts K, Glicksman MA, Lin CG. Restored Glial Glutamate Transporter EAAT2 Function as a Potential Therapeutic Approach for Alzheimer's Disease. Journal of Experimental Medicine 2015, 212, 319-332.

Hodgetts K.: “CNS Drug Optimization – Medicinal Chemistry” invited chapter in Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects, Eds. Di and Kerns, Wiley 2015, Chapter 19, 425-445. ISBN: 978-1-118-78835-6.

Hodgetts K., Lin C-L.: Preparation of pyridazine derivatives as EAAT2 activators, WO 2017123991

Androphy E.J., Hodgetts K., Calder A.N.; Preparation of amidopyridothiazoles and amidopyridoxazoles and their use in combination therapies for treatment of spinal muscular atrophy, US 2017023922

Cuny G., Glicksman M., Hodgetts K., Mathieu S., Perrella Y., Darmency V., Lusic H.: Preparation of pyrimidine compounds as inhibitors of heat shock protein 90 family of chaperone proteins, WO 2015192119.

1. Cherry JJ, Osman EY, Evans MC, Choi S, Xing X, Cuny GD, Glicksman MA, Lorson CL, Androphy EJ. Enhancement of SMN protein levels in a mouse model of spinal muscular atrophy using novel drug-like compounds. EMBO Mol Med. 2013 Jul;5(7):1103-18. PMID:23740718. 2. Zhang X, Hermandez I, Rei D, Mair W, Laha JK, Cornwell ME, Cuny GD, Tsai LH,Steen JA, Kosik KS. Diaminothiazoles Modify Tau Phosphorylation and Improve the Tauopathy in Mouse Models. J Biol Chem. 2013 Jun 4. PubMed PMID: 23737518.

3. Sanvitale CE, Kerr G, Chaikuad A, Ramel MC, Mohedas AH, Reichert S, Wang Y, Triffitt JT, Cuny GD, Yu PB, Hill CS, Bullock AN. A new class of small molecule inhibitor of BMP signaling. PLoS One. 2013 Apr 30;8(4):e62721. PubMed PMID: 23646137; PubMed Central PMCID: PMC3639963.

4. Mohedas AH, Xing X, Armstrong KA, Bullock AN, Cuny GD, Yu PB. Development of an ALK2-Biased BMP Type I Receptor Kinase Inhibitor. ACS Chem Biol. 2013 Apr 30. PubMed PMID: 23547776.

5. Maki JL, Tres Brazell J, Teng X, Cuny GD, Degterev A. Expression andpurification of active receptor interacting protein 1 kinase using a baculovirus system. Protein Expr Purif. 2013 Jun;89(2):156-61. PubMed PMID: 23523699; PubMedCentral PMCID: PMC3653991.

6. McNamara CR, Ahuja R, Osafo-Addo AD, Barrows D, Kettenbach A, Skidan I, Teng X, Cuny GD, Gerber S, Degterev A. Akt Regulates TNFα synthesis downstream of RIP1 kinase activation during necroptosis. PLoS One. 2013;8(3):e56576. PubMed PMID: 23469174; PubMedCentral PMCID: PMC3585731.

7. Liu M, Bender SA, Cuny GD, Sherman W, Glicksman M, Ray SS. Type II Kinase Inhibitors Show an Unexpected Inhibition Mode against Parkinson's Disease-Linked LRRK2 Mutant G2019S. Biochemistry. 2013 Mar 1. PubMed PMID:23379419.

8. Glicksman M, Pajak L, Lam K. Stem cell themes: promises and challenges. J Biomol Screen. 2012 Oct;17(9):E1-3.PMID:23023569

9. Gorla SK, Kavitha M, Zhang M, Liu X, Sharling L, Gollapalli DR, Striepen B, Hedstrom L, Cuny GD. Selective and Potent Urea Inhibitors of Cryptosporidium parvum Inosine 5'-Monophosphate Dehydrogenase. J Med Chem. 2012 Sep 13;55(17):7759-71. PubMed PMID: 22950983.

10. Lin CL, Kong Q, Cuny GD, Glicksman MA. Glutamate transporter EAAT2: a new target for the treatment of neurodegenerative diseases. Future Med Chem. 2012Sep;4(13):1689-700. PubMed PMID: 22924507.

11. Abraham CR, Chen C, Cuny GD, Glicksman MA, Zeldich E. Small-molecule Klotho enhancers as novel treatment of neurodegeneration. Future Med Chem. 2012 Sep;4(13):1671-9. PubMed PMID: 22924505.

12. Cuny GD. Foreword: neurodegenerative diseases: challenges and opportunities.Future Med Chem. 2012 Sep;4(13):1647-9. PubMed PMID:22924500.

13. Choi S, Keys H, Staples RJ, Yuan J, Degterev A, Cuny GD. Optimization of tricyclic Nec-3 necroptosis inhibitors for in vitro liver microsomal stability. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5685-8.PMCID: PMC3434878.

14. Maki JL, Smith EE, Teng X, Ray SS, Cuny GD, Degterev A. Fluorescence polarization assay for inhibitors of the kinase domain of receptor interacting protein 1. Anal Biochem. 2012 Aug 15;427(2):164-74. PubMed PMID: 22658960; PMCID: PMC3398245.

15. Hellal M, Singh S, Cuny GD. Synthesis of tetracyclic indoles via intramolecular α-arylation of ketones. J Org Chem. 2012 Apr 20;77(8):4123-30. PMID: 22480284.

16. Kirubakaran S, Gorla SK, Sharling L, Zhang M, Liu X, Ray SS, Macpherson IS, Striepen B, Hedstrom L, Cuny GD. Structure-activity relationship study of selective benzimidazole-based inhibitors of Cryptosporidium parvum IMPDH. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1985-8. PubMed PMID: 22310229;PMCID: PMC3289519.

17. Pejo E, Cotten JF, Kelly EW, Le Ge R, Cuny GD, Laha JK, Liu J, Lin XJ, Raines DE. In vivo and in vitro pharmacological studies of methoxycarbonyl-carboetomidate. Anesth Analg. 2012 Aug;115(2):297-304. PMID: 21965364; PMCID: PMC3252484.

18. So PP, Zeldich E, Seyb KI, Huang MM, Concannon JB, King GD, Chen CD, Cuny GD, Glicksman MA, Abraham CR. Lowering of amyloid beta peptide production with a small molecule inhibitor of amyloid-β precursor protein dimerization. Am J Neurodegener Dis. 2012 May 30;1(1):75-87. PubMed PMID: 22822474; PMCID: PMC3401075.

19.  Wright PD, Wightman N, Huang M, Weiss A, Sapp PC, Cuny GD, Ivinson AJ, Glicksman MA, Ferrante RJ, Matson W, Matson S, Brown RH Jr. A high-throughput screen to identify inhibitors of SOD1 transcription. Front Biosci (Elite Ed). 2012 Jun 1;4:2801-8. PubMed PMID: 22652679.

20. Hart MJ, Glicksman M, Liu M, Sharma MK, Cuny G, Galvan V. Development of a high-throughput screen targeting caspase-8-mediated cleavage of the amyloid precursor protein. Anal Biochem. 2012 Feb 15;421(2):467-76. PMID:22178911

21. Glicksman MA. The preclinical discovery of amyotrophic lateral sclerosis drugs. Expert Opin Drug Discov. 2011 Nov;6(11):1127-38. PubMed PMID: 22646982; PMCID: PMC3367799.

22. Arkin MR, Glicksman MA, Fu H, Havel JJ, Du Y. Inhibition of Protein-Protein Interactions: Non-Cellular Assay Formats. 2012 Mar 18 [updated 2012 Oct 01]. In: Sittampalam GS, Gal-Edd N, Arkin M, Auld D, Austin C, Bejcek B, Glicksman M, Inglese J, Lemmon V, Li Z, McGee J, McManus O, Minor L, Napper A, Riss T, Trask OJ, Weidner J, editors. Assay Guidance Manual Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-. Available from  http://www.ncbi.nlm.nih.gov/books/NBK92000/PubMed PMID: 22553871.

23.  Cuny GD, Ulyanova NP, Patnaik D, Liu JF, Lin X, Auerbach K, Ray SS, Xian J, Glicksman MA, Stein RL, Higgins JM. Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. Bioorg Med Chem Lett. 2012 Mar 1;22(5):2015-9. PubMed PMID: 22335895; PubMed Central PMCID: PMC3288743.

24. Costa SC, Schmitz AM, Jahufar FF, Boyd JD, Cho MY, Glicksman MA, Lesser CF. A new means to identify type 3 secreted effectors: functionally interchangeable class IB chaperones recognize a conserved sequence. MBio. 2012 Feb 14;3(1). pii: e00243-11. PubMed PMID: 22334517; PubMed Central PMCID: PMC3280449.

25. Cherry JJ, Evans MC, Ni J, Cuny GD, Glicksman MA, Androphy EJ. Identification of novel compounds that increase SMN protein levels using an improved SMN2 reporter cell assay. J Biomol Screen. 2012 Apr;17(4):481-95. PubMed PMID: 22233647.

26. Tang X, Seyb KI, Huang M, Schuman ER, Shi P, Zhu H, Glicksman MA. A high-throughput screening method for small-molecule inhibitors of the aberrant mutant SOD1 and dynein complex interaction. J Biomol Screen. 2012 Mar;17(3):314-26. Epub 2011 Dec 1. PubMed PMID: 22140121.

27. Liu M, Kang S, Ray S, Jackson J, Zaitsev AD, Gerber SA, Cuny GD, Glicksman MA. Kinetic, mechanistic, and structural modeling studies of truncated wild-type leucine-rich repeat kinase 2 and the G2019S mutant. Biochemistry. 2011 Nov 1;50(43):9399-408. PMID: 21961647; PMCID:PMC3205922.

28. Wilkinson K, Boyd JD, Glicksman M, Moore KJ, El Khoury J. A high content drug screen identifies ursolic acid as an inhibitor of amyloid beta protein interactions with its receptor CD36. J Biol Chem. 2011 Oct 7;286(40):34914-22. Epub 2011 Aug 11. PMID:21835916

29. King GD, Chen C, Huang MM, Zeldich E, Brazee PL, Schuman ER, Robin M, Cuny GD, Glicksman MA, Abraham CR. Identification of novel small molecules that elevate Klotho expression. Biochem J. 2012 Jan 1;441(1):453-61. PubMed PMID:21939436.

30. Xing X, Chang LC, Kong Q, Colton CK, Lai L, Glicksman MA, Lin CL, Cuny GD. Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5774-7. PubMed PMID: 21875806; PubMed Central PMCID: PMC3172717.

31. Garkavtsev I, Chauhan VP, Wong HK, Mukhopadhyay A, Glicksman MA, Peterson RT, Jain RK. Dehydro-alpha-lapachone, a plant product with antivascular activity. Proc Natl Acad Sci U S A. 2011 Jul 12;108(28):11596-601. PubMed PMID: 21709229; PubMed Central PMCID: PMC3136298.

32.  Shishova EY, Stoll JM, Ersoy BA, Shrestha S, Scapa EF, Li Y, Niepel MW, Su Y, Jelicks LA, Stahl GL, Glicksman MA, Gutierrez-Juarez R, Cuny GD, Cohen DE. Genetic ablation or chemical inhibition of phosphatidylcholine transfer protein attenuates diet-induced hepatic glucose production. Hepatology. 2011 Aug;54(2):664-74. PubMed PMID:21538437; PubMed Central PMCID: PMC3144994. 

33. Wright PD, Huang M, Weiss A, Matthews J, Wightman N, Glicksman M, Brown RH Jr. Screening for inhibitors of the SOD1 gene promoter: pyrimethamine does not reduce SOD1 levels in cell and animal models. Neurosci Lett. 2010 Oct 4;482(3):188-92. Epub 2010 Jul 16. PMID:20638444

34. Cullen V, Sardi SP, Ng J, Xu YH, Sun Y, Tomlinson JJ, Kolodziej P, Kahn I, Saftig P, Woulfe J, Rochet JC, Glicksman MA, Cheng SH, Grabowski GA, Shihabuddin LS, Schlossmacher MG. Acid β-glucosidase mutants linked to Gaucher disease, Parkinson disease, and Lewy body dementia alter α-synuclein processing. Ann Neurol. 2011 Jun;69(6):940-53.  PMID: 21472771.

35.  Laha JK, Cuny GD. Synthesis of fused imidazoles, pyrroles, and indoles with a defined stereocenter α to nitrogen utilizing Mitsunobu alkylation followed by palladium-catalyzed cyclization. J Org Chem. 2011 Oct 21;76(20):8477-82. PubMed PMID: 21913645.

36.  Laha JK, Barolo SM, Rossi RA, Cuny GD. Synthesis of carbolines by photostimulated cyclization of anilinohalopyridines. J Org Chem. 2011 Aug 5;76(15):6421-5. PubMed PMID: 21739958.

37.  Steinbicker AU, Sachidanandan C, Vonner AJ, Yusuf RZ, Deng DY, Lai CS, Rauwerdink KM, Winn JC, Saez B, Cook CM, Szekely BA, Roy CN, Seehra JS, Cuny GD, Scadden DT, Peterson RT, Bloch KD, Yu PB. Inhibition of bone morphogenetic protein signaling attenuates anemia associated with inflammation. Blood. 2011 May 5;117(18):4915-23. PubMed PMID: 21393479; PMCID:PMC3100698.

38.  Laha JK, Zhang X, Qiao L, Liu M, Chatterjee S, Robinson S, Kosik KS, Cuny GD. Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors. Bioorg Med Chem Lett. 2011 Apr 1;21(7):2098-101. PMID: 21353545; PMCID: PMC3062192.

39.  Cuny GD, Robin M, Ulyanova NP, Patnaik D, Pique V, Casano G, Liu JF, Lin X, Xian J, Glicksman MA, Stein RL, Higgins JM. Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3491-4. PMID: 20836251; PMCID:PMC3118465.

40. Liu M, Poulose S, Schuman E, Zaitsev AD, Dobson B, Auerbach K, Seyb K, Cuny GD, Glicksman MA, Stein RL, Yue Z. Development of a mechanism-based high-throughput screen assay for leucine-rich repeat kinase 2--discovery of LRRK2 inhibitors. Anal Biochem. 2010 Sep 15;404(2):186-92.PMID: 20566370; PMCID: PMC2921631.

41. Colton CK, Kong Q, Lai L, Zhu MX, Seyb KI, Cuny GD, Xian J, Glicksman MA, Lin CL. Identification of translational activators of glial glutamate transporter EAAT2 through cell-based high-throughput screening: an approach to prevent excitotoxicity. J Biomol Screen. 2010 Jul;15(6):653-62. PMID: 20508255; PMCID: PMC3016154.

42. Liu M, Girma E, Glicksman MA, Stein RL. Kinetic mechanistic studies of Cdk5/p25-catalyzed H1P phosphorylation: metal effect and solvent kinetic isotope effect. Biochemistry. 2010 Jun 15;49(23):4921-9. PMID: 20491486; PMCID: PMC2921628.

43.  Kuohung W, Burnett M, Mukhtyar D, Schuman E, Ni J, Crowley WF, Glicksman MA, Kaiser UB. A high-throughput small-molecule ligand screen targeted to agonists and antagonists of the G-protein-coupled receptor GPR54. J Biomol Screen. 2010 Jun;15(5):508-17. PMID: 20460252.

44. Ouertatani-Sakouhi H, Liu M, El-Turk F, Cuny GD, Glicksman MA, Lashuel HA. Kinetic-based high-throughput screening assay to discover novel classes of macrophage migration inhibitory factor inhibitors. J Biomol Screen. 2010 Apr;15(4):347-58. PMID: 20231420.

45. Liu M, Dobson B, Glicksman MA, Yue Z, Stein RL. Kinetic mechanistic studies of wild-type leucine-rich repeat kinase 2: characterization of the kinase and GTPase activities. Biochemistry. 2010 Mar 9;49(9):2008-17. PMID: 20146535; PMCID: PMC2897705.

46.  Zeng X, Sigoillot F, Gaur S, Choi S, Pfaff KL, Oh DC, Hathaway N, Dimova N, Cuny GD, King RW. Pharmacologic inhibition of the anaphase-promoting complex induces a spindle checkpoint-dependent mitotic arrest in the absence of spindle damage. Cancer Cell. 2010 Oct 19;18(4):382-95. PMID: 20951947; PMCID: PMC2957475.

47.  Hellal M, Cuny GD. Synthesis of the indolizino[7,6-c]quinoline alkaloid isaindigotidione. Org Lett. 2010 Oct 15;12(20):4628-31. PubMed PMID: 20845915.

48.  Leissring MA, Malito E, Hedouin S, Reinstatler L, Sahara T, Abdul-Hay SO, Choudhry S, Maharvi GM, Fauq AH, Huzarska M, May PS, Choi S, Logan TP, Turk BE, Cantley LC, Manolopoulou M, Tang WJ, Stein RL, Cuny GD, Selkoe DJ. Designed inhibitors of insulin-degrading enzyme regulate the catabolism and activity of insulin. PLoS One. 2010 May 7;5(5):e10504. PMID: 20498699; PMCID: PMC2866327.

49.  Hellal M, Cuny GD. Intramolecular Aldol reaction of N-acylated (2-aminophenyl)-alpha-oxoacetic acids: rapid access to tri- and tetracyclic 1,2-dihydroquinolin-2(1H)-ones. J Org Chem. 2010 May 21;75(10):3465-8. PMID: 20394404.

50.  Nowak RJ, Cuny GD, Choi S, Lansbury PT, Ray SS. Improving binding specificity of pharmacological chaperones that target mutant superoxide dismutase-1 linked to familial amyotrophic lateral sclerosis using computational methods. J Med Chem. 2010 Apr 8;53(7):2709-18. PMID: 20232802; PMCID:PMC2881568.

51.  Cotten JF, Forman SA, Laha JK, Cuny GD, Husain SS, Miller KW, Nguyen HH, Kelly EW, Stewart D, Liu A, Raines DE. Carboetomidate: a pyrrole analog of etomidate designed not to suppress adrenocortical function. Anesthesiology. 2010 Mar;112(3):637-44 PMID: 20179500;PMCID: PMC2830733.

52.  Lee K, Campbell J, Swoboda JG, Cuny GD, Walker S. Development of improved inhibitors of wall teichoic acid biosynthesis with potent activity against Staphylococcus aureus. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1767-70. PMID: 20138521; PMCID: PMC2844852.

53.  Macpherson IS, Kirubakaran S, Gorla SK, Riera TV, D'Aquino JA, Zhang M, Cuny GD, Hedstrom L. The structural basis of Cryptosporidium -specific IMP dehydrogenase inhibitor selectivity. J Am Chem Soc. 2010 Feb 3;132(4):1230-1. Erratum in: J Am Chem Soc. 2010 May 12;132(18):6610. PMID: 20052976; PMCID: PMC2819028.

54.  Rosenbaum DM, Degterev A, David J, Rosenbaum PS, Roth S, Grotta JC, Cuny GD, Yuan J, Savitz SI. Necroptosis, a novel form of caspase-independent cell death, contributes to neuronal damage in a retinal ischemia-reperfusion injury model. J Neurosci Res. 2010 May 5;88(7):1569-76. PMID: 20025059.

55. Qiao L, Choi S, Case A, Gainer TG, Seyb K, Glicksman MA, Lo DC, Stein RL,Cuny GD. Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6122-6. PMID:19783434; PMCID: PMC2785710.

56. Cuny GD. Kinase inhibitors as potential therapeutics for acute and chronic neurodegenerative conditions. Curr Pharm Des. 2009;15(34):3919-39. Review. PMID: 19751204.

57. Maurya SK, Gollapalli DR, Kirubakaran S, Zhang M, Johnson CR, Benjamin NN, Hedstrom L, Cuny GD. Triazole inhibitors of Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase. J Med Chem. 2009 Aug 13;52(15):4623-30. PMID: 19624136; PMCID: PMC2810100.

58. Cuny GD. A new class of UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC) inhibitors for the treatment of Gram-negative infections: PCT application WO 2008027466. Expert Opin Ther Pat. 2009 Jun;19(6):893-9. PMID: 19473108.

59. Cabrol C, Huzarska MA, Dinolfo C, Rodriguez MC, Reinstatler L, Ni J, Yeh LA, Cuny GD, Stein RL, Selkoe DJ, Leissring MA. Small-molecule activators of insulin-degrading enzyme discovered through high-throughput compound screening. PLoS One. 2009;4(4):e5274. PMID: 19384407; PMCID: PMC2668070.

60. Laha JK, Petrou P, Cuny GD. One-pot synthesis of alpha-carbolines via sequential palladium-catalyzed aryl amination and intramolecular arylation. J Org Chem. 2009 Apr 17;74(8):3152-5. PMID: 19323545.

61.  Patnaik D, Jun Xian, Glicksman MA, Cuny GD, Stein RL, Higgins JM. Identification of small molecule inhibitors of the mitotic kinase haspin by high-throughput screening using a homogeneous time-resolved fluorescence resonance energy transfer assay. J Biomol Screen. 2008 Dec;13(10):1025-34. Epub 2008 Oct 31. PMID: 18978305; PMCID: PMC2615828.

62. Seyb KI, Schuman ER, Ni J, Huang MM, Michaelis ML, Glicksman MA. Identification of small molecule inhibitors of beta-amyloid cytotoxicity through a cell-based high-throughput screening platform. J Biomol Screen. 2008 Oct;13(9):870-8. Epub 2008 Sep 23. PMID: 18812568; PMCID:PMC2754199.

63. Wagle N, Xian J, Shishova EY, Wei J, Glicksman MA, Cuny GD, Stein RL, Cohen DE. Small-molecule inhibitors of phosphatidylcholine transfer protein/StarD2 identified by high-throughput screening. Anal Biochem. 2008 Dec 1;383(1):85-92. PMID: 18762160; PMCID: PMC2783649.

64. Liu M, Choi S, Cuny GD, Ding K, Dobson BC, Glicksman MA, Auerbach K, Stein RL. Kinetic studies of Cdk5/p25 kinase: phosphorylation of tau and complex inhibition by two prototype inhibitors. Biochemistry. 2008 Aug 12;47(32):8367-77. PMID: 18636751.

65. Yu PB, Deng DY, Lai CS, Hong CC, Cuny GD, Bouxsein ML, Hong DW, McManus PM, Katagiri T, Sachidanandan C, Kamiya N, Fukuda T, Mishina Y, Peterson RT, Bloch KD. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med. 2008 Dec;14(12):1363-9. Erratum in: Nat Med. 2009 Jan;15(1):117. PMID: 19029982; PMCID: PMC2846458.

66.  Moe ST, Thompson AB, Smith GM, Fredenburg RA, Stein RL, Jacobson AR. Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs. Bioorg Med Chem. 2009 Apr 15;17(8):3072-9. PMID:19329331

67.  Cuny GD, Yu PB, Laha JK, Xing X, Liu JF, Lai CS, Deng DY, Sachidanandan C, Bloch KD, Peterson RT. Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4388-92. PMID: 18621530; PMCID: PMC2570262.

68.  You Z, Savitz SI, Yang J, Degterev A, Yuan J, Cuny GD, Moskowitz MA, Whalen MJ. Necrostatin-1 reduces histopathology and improves functional outcome after controlled cortical impact in mice. J Cereb Blood Flow Metab. 2008 Sep;28(9):1564-73. PMID: 18493258; PMCID:PMC2831087.

69.  Teng X, Keys H, Yuan J, Degterev A, Cuny GD. Structure-activity relationship and liver microsome stability studies of pyrrole necroptosis inhibitors. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3219-23. PMID:18467094; PMCID: PMC2519155.

70.  Degterev A, Hitomi J, Germscheid M, Ch'en IL, Korkina O, Teng X, Abbott D, Cuny GD, Yuan C, Wagner G, Hedrick SM, Gerber SA, Lugovskoy A, Yuan J. Identification of RIP1 kinase as a specific cellular target of necrostatins. Nat Chem Biol. 2008 May;4(5):313-21. PubMed PMID: 18408713.

71. Glicksman MA, Cuny GD, Liu M, Dobson B, Auerbach K, Stein RL, Kosik KS. New approaches to the discovery of cdk5 inhibitors. Curr Alzheimer Res. 2007 Dec;4(5):547-9. Review. PMID: 18220519.

72. Donahue CP, Ni J, Rozners E, Glicksman MA, Wolfe MS. Identification of tau stem loop RNA stabilizers. J Biomol Screen. 2007 Sep;12(6):789-99. PMID: 17525136.

73. Rossi C, Padmanaban D, Ni J, Yeh LA, Glicksman MA, Waldner H. Identifying druglike inhibitors of myelin-reactive T cells by phenotypic high-throughput screening of a small-molecule library. J Biomol Screen. 2007 Jun;12(4):481-9. PMID: 17478482.

74.  Teng X, Keys H, Jeevanandam A, Porco JA Jr, Degterev A, Yuan J, Cuny GD. Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6836-40. PMID: 17964153; PMCID: PMC2169518.

75.  Stein RL. A new model for academics based drug discovery. Curr Alzheimer Res. 2007 Dec;4(5):574-6. PMID:18220526

76.  Case A, Stein RL. Kinetic analysis of the interaction of tissue transglutaminase with a nonpeptidic slow-binding inhibitor. Biochemistry. 2007 Jan 30;46(4):1106-15. PMID:17240993

77.  Mermerian AH, Case A, Stein RL, Cuny GD. Structure-activity relationship, kinetic mechanism, and selectivity for a new class of ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitors. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3729-32. PMID: 17449248.

78.  Jagtap PG, Degterev A, Choi S, Keys H, Yuan J, Cuny GD. Structure-activity relationship study of tricyclic necroptosis inhibitors. J Med Chem. 2007 Apr 19;50(8):1886-95. PubMed PMID: 17361994.

79.  Luchansky SJ, Lansbury PT Jr, Stein RL. Substrate recognition and catalysis by UCH-L1. Biochemistry. 2006 Dec 12;45(49):14717-25. PMID:17144664

80. Case A, Stein RL. Mechanistic studies of ubiquitin C-terminal hydrolase L1. Biochemistry. 2006 Feb 21;45(7):2443-52. PMID:16475834

81. Bandyopadhyay S, Ni J, Ruggiero A, Walshe K, Rogers MS, Chattopadhyay N, Glicksman MA, Rogers JT. A high-throughput drug screen targeted to the 5'untranslated region of Alzheimer amyloid precursor protein mRNA. J Biomol Screen. 2006 Aug;11(5):469-80. PMID: 16928984.

82.  Broom WJ, Auwarter KE, Ni J, Russel DE, Yeh LA, Maxwell MM, Glicksman M, Kazantsev AG, Brown RH Jr. Two approaches to drug discovery in SOD1-mediated ALS. J Biomol Screen. 2006 Oct;11(7):729-35. PMID:16928982

83.  Ravel S, Patrel D, Koffi M, Jamonneau V, Cuny G. Cyclical transmission of Trypanosoma brucei gambiense in Glossina palpalis gambiensis displays great differences among field isolates. Acta Trop. 2006 Nov;100(1-2):151-5. PubMed PMID: 17069743.

84.  Barolo SM, Teng X, Cuny GD, Rossi RA. Syntheses of aporphine and homoaporphine alkaloids by intramolecular ortho-arylation of phenols with aryl halides via SRN1 reactions in liquid ammonia. J Org Chem. 2006 Oct 27;71(22):8493-9. PubMed PMID: 17064025.

85.  Tucker S, Ahl M, Cho HH, Bandyopadhyay S, Cuny GD, Bush AI, Goldstein LE, Westaway D, Huang X, Rogers JT. RNA therapeutics directed to the non coding regions of APP mRNA, in vivo anti-amyloid efficacy of paroxetine, erythromycin, and N-acetyl cysteine. Curr Alzheimer Res. 2006 Jul;3(3):221-7. PubMed PMID:16842099.

86.  Nicholson MJ, Moradi B, Seth NP, Xing X, Cuny GD, Stein RL, Wucherpfennig KW. Small molecules that enhance the catalytic efficiency of HLA-DM. J Immunol. 2006 Apr 1;176(7):4208-20. PMID: 16547258; PMCID:PMC3412064.

87.  Zhang D, Xing X, Cuny GD. Synthesis of hydantoins from enantiomerically pure alpha-amino amides without epimerization. J Org Chem. 2006 Feb 17;71(4):1750-3. PMID: 16468841.

88.  Degterev A, Huang Z, Boyce M, Li Y, Jagtap P, Mizushima N, Cuny GD, Mitchison TJ, Moskowitz MA, Yuan J. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol. 2005 Jul;1(2):112-9. Epub 2005 May 29. Erratum in: Nat Chem Biol. 2005 Sep;1(4):234. PubMed PMID: 16408008.

89.  Case A, Ni J, Yeh LA, Stein RL. Development of a mechanism-based assay for tissue transglutaminase--results of a high-throughput screen and discovery of inhibitors. Anal Biochem. 2005 Mar 15;338(2):237-44. PMID:15745743

90.  Teng X, Degterev A, Jagtap P, Xing X, Choi S, Denu R, Yuan J, Cuny GD. Structure-activity relationship study of novel necroptosis inhibitors. Bioorg Med Chem Lett. 2005 Nov 15;15(22):5039-44. PubMed PMID: 16153840.

91.  Ahn JS, Radhakrishnan ML, Mapelli M, Choi S, Tidor B, Cuny GD, Musacchio A, Yeh LA, Kosik KS. Defining Cdk5 ligand chemical space with small molecule inhibitors of tau phosphorylation. Chem Biol. 2005 Jul;12(7):811-23. PMID:16039528.

92.  Duval E, Case A, Stein RL, Cuny GD. Structure-activity relationship study of novel tissue transglutaminase inhibitors. Bioorg Med Chem Lett. 2005 Apr 1;15(7):1885-9. PMID: 15780627.

93.  Yeh LA, Padmanaban D, Ho P, Xing X, Rowley P, Morse LJ, Jensen RV, Cuny GD. Effects of a verbenachalcone derivative on neurite outgrowth, inhibition of caspase induction and gene expression. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1193-6. PubMed PMID: 15686940.

94.  Choi S, Haggart D, Toll L, Cuny GD. Synthesis, receptor binding and functional studies of mesoridazine stereoisomers. Bioorg Med Chem Lett. 2004 Sep 6;14(17):4379-82. PMID: 15357957.

95. Morse LJ, Payton SM, Cuny GD, Rogers JT. FDA-preapproved drugs targeted to the translational regulation and processing of the amyloid precursor protein. J Mol Neurosci. 2004;24(1):129-36. PubMed PMID: 15314261.

96. Liu Y, Lashuel HA, Choi S, Xing X, Case A, Ni J, Yeh LA, Cuny GD, Stein RL, Lansbury PT Jr. Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line. Chem Biol. 2003 Sep;10(9):837-46. PubMed PMID: 14522054.

97. Stein RL. High-throughput screening in academia: the Harvard experience. J Biomol Screen. 2003 Dec;8(6):615-9. PMID:14711386

98. Case A, Stein RL. Kinetic analysis of the action of tissue transglutaminase on peptide and protein substrates. Biochemistry. 2003 Aug 12;42(31):9466-81. PMID:12899634

99. Leissring MA, Lu A, Condron MM, Teplow DB, Stein RL, Farris W, Selkoe DJ.  Kinetics of amyloid beta-protein degradation determined by novel fluorescence- and fluorescence polarization-based assays. J Biol Chem. 2003 Sep 26;278(39):37314-20. PMID:12867419

100. Case A, Huskey WP, Stein RL. Enzymatic reaction of silent substrates: kinetic theory and application to the serine protease chymotrypsin. Biochemistry. 2003 Apr 29;42(16):4727-32. PMID:12705836

101. Case A, Stein RL. Mechanistic origins of the substrate selectivity of serine proteases. Biochemistry. 2003 Mar 25;42(11):3335-48. PMID:12641466

102. Stein RL. A new model for drug discovery--meeting our societal obligation. Drug Discov Today. 2003 Mar 15;8(6):245-8. PMID:12623234

Publications

Dr. Kevin Hodgetts

Director of The Laboratory for Drug Discovery in Neurodegeneration

65 Landsdowne Street

Cambridge, Massachusetts 02139

U.S.A.

Telephone: 617-768-8640

Email: khodgetts@bwh.harvard.edu

Contact

The Laboratory for Drug Discovery in Neurodegeneration