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A Novel Probe for Spliceosomal Proteins that Induces Autophagy and Death of Melanoma Cells Reveals New Targets for Melanoma Drug Discovery.

Palrasu M, Knapinska AM, Diez J, Smith L, LaVoi T, Giulianotti M, Houghten RA, Fields GB, Minond D.

Cell Physiol Biochem. 2019;53(4):656-686. doi: 10.33594/000000164.


A Novel Class of Common Docking Domain Inhibitors That Prevent ERK2 Activation and Substrate Phosphorylation.

Sammons RM, Perry NA, Li Y, Cho EJ, Piserchio A, Zamora-Olivares DP, Ghose R, Kaoud TS, Debevec G, Bartholomeusz C, Gurevich VV, Iverson TM, Giulianotti M, Houghten RA, Dalby KN.

ACS Chem Biol. 2019 Jun 21;14(6):1183-1194. doi: 10.1021/acschembio.9b00093. Epub 2019 May 13.


Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist.

Fleming KA, Freeman KT, Powers MD, Santos RG, Debevec G, Giulianotti MA, Houghten RA, Doering SR, Pinilla C, Haskell-Luevano C.

J Med Chem. 2019 Mar 14;62(5):2738-2749. doi: 10.1021/acs.jmedchem.9b00053. Epub 2019 Feb 28.


Scaffold Ranking and Positional Scanning Identify Novel Neurite Outgrowth Promoters with Nanomolar Potency.

Al-Ali H, Debevec G, Santos RG, Houghten RA, Davis JC, Nefzi A, Lemmon VP, Bixby JL, Giulianotti MA.

ACS Med Chem Lett. 2018 Sep 24;9(10):1057-1062. doi: 10.1021/acsmedchemlett.8b00425. eCollection 2018 Oct 11.


Identification of a Novel Polyamine Scaffold With Potent Efflux Pump Inhibition Activity Toward Multi-Drug Resistant Bacterial Pathogens.

Fleeman RM, Debevec G, Antonen K, Adams JL, Santos RG, Welmaker GS, Houghten RA, Giulianotti MA, Shaw LN.

Front Microbiol. 2018 Jun 14;9:1301. doi: 10.3389/fmicb.2018.01301. eCollection 2018.


Exploring the chemical space of peptides for drug discovery: a focus on linear and cyclic penta-peptides.

Díaz-Eufracio BI, Palomino-Hernández O, Houghten RA, Medina-Franco JL.

Mol Divers. 2018 May;22(2):259-267. doi: 10.1007/s11030-018-9812-9. Epub 2018 Feb 14.


Highly Selective and Potent α4β2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats.

Wu J, Cippitelli A, Zhang Y, Debevec G, Schoch J, Ozawa A, Yu Y, Liu H, Chen W, Houghten RA, Welmaker GS, Giulianotti MA, Toll L.

J Med Chem. 2017 Dec 28;60(24):10092-10104. doi: 10.1021/acs.jmedchem.7b01250. Epub 2017 Dec 13.


A one-pot multicomponent approach to a new series of morphine derivatives and their biological evaluation.

Shao J, Houghten RA, Dooley CT, Cazares M, McLaughlin JP, Eans SO, Ganno ML, Hoot MR, Giulianotti MA, Yu Y.

Org Biomol Chem. 2017 Sep 26;15(37):7796-7801. doi: 10.1039/c7ob01924f.


Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries.

Giulianotti MA, Vesely BA, Azhari A, Souza A, LaVoi T, Houghten RA, Kyle DE, Leahy JW.

ACS Med Chem Lett. 2017 Jul 10;8(8):802-807. doi: 10.1021/acsmedchemlett.7b00045. eCollection 2017 Aug 10.


Mu-Opioid receptor biased ligands: A safer and painless discovery of analgesics?

Madariaga-Mazón A, Marmolejo-Valencia AF, Li Y, Toll L, Houghten RA, Martinez-Mayorga K.

Drug Discov Today. 2017 Nov;22(11):1719-1729. doi: 10.1016/j.drudis.2017.07.002. Epub 2017 Jul 22. Review.


Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa1-Arg-(pI)DPhe-Xaa4-NH2.

Doering SR, Freeman KT, Schnell SM, Haslach EM, Dirain M, Debevec G, Geer P, Santos RG, Giulianotti MA, Pinilla C, Appel JR, Speth RC, Houghten RA, Haskell-Luevano C.

J Med Chem. 2017 May 25;60(10):4342-4357. doi: 10.1021/acs.jmedchem.7b00301. Epub 2017 May 15.


Identification of 5,6-dihydroimidazo[2,1-b]thiazoles as a new class of antimicrobial agents.

Li Y, Bionda N, Fleeman R, Wang H, Ozawa A, Houghten RA, Shaw L.

Bioorg Med Chem. 2016 Nov 1;24(21):5633-5638. doi: 10.1016/j.bmc.2016.09.027. Epub 2016 Sep 12.


Characterization of Potent SMAC Mimetics that Sensitize Cancer Cells to TNF Family-Induced Apoptosis.

Welsh K, Milutinovic S, Ardecky RJ, Gonzalez-Lopez M, Ganji SR, Teriete P, Finlay D, Riedl S, Matsuzawa S, Pinilla C, Houghten R, Vuori K, Reed JC, Cosford ND.

PLoS One. 2016 Sep 12;11(9):e0161952. doi: 10.1371/journal.pone.0161952. eCollection 2016.


Small-Molecule Inhibitors Targeting Topoisomerase I as Novel Antituberculosis Agents.

Sandhaus S, Annamalai T, Welmaker G, Houghten RA, Paz C, Garcia PK, Andres A, Narula G, Rodrigues Felix C, Geden S, Netherton M, Gupta R, Rohde KH, Giulianotti MA, Tse-Dinh YC.

Antimicrob Agents Chemother. 2016 Jun 20;60(7):4028-36. doi: 10.1128/AAC.00288-16. Print 2016 Jul.


Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.

Li Y, Cazares M, Wu J, Houghten RA, Toll L, Dooley C.

J Med Chem. 2016 Feb 11;59(3):1239-45. doi: 10.1021/acs.jmedchem.5b01899. Epub 2016 Jan 29.


Direct Phenotypic Screening in Mice: Identification of Individual, Novel Antinociceptive Compounds from a Library of 734,821 Pyrrolidine Bis-piperazines.

Houghten RA, Ganno ML, McLaughlin JP, Dooley CT, Eans SO, Santos RG, LaVoi T, Nefzi A, Welmaker G, Giulianotti MA, Toll L.

ACS Comb Sci. 2016 Jan 11;18(1):51-64. doi: 10.1021/acscombsci.5b00126. Epub 2016 Jan 5.


Identification of Small Molecule Inhibitors of Human As(III) S-Adenosylmethionine Methyltransferase (AS3MT).

Dong H, Madegowda M, Nefzi A, Houghten RA, Giulianotti MA, Rosen BP.

Chem Res Toxicol. 2015 Dec 21;28(12):2419-25. doi: 10.1021/acs.chemrestox.5b00432. Epub 2015 Dec 6.


SAR Studies of Exosite-Binding Substrate-Selective Inhibitors of A Disintegrin And Metalloprotease 17 (ADAM17) and Application as Selective in Vitro Probes.

Knapinska AM, Dreymuller D, Ludwig A, Smith L, Golubkov V, Sohail A, Fridman R, Giulianotti M, LaVoi TM, Houghten RA, Fields GB, Minond D.

J Med Chem. 2015 Aug 13;58(15):5808-24. doi: 10.1021/acs.jmedchem.5b00354. Epub 2015 Aug 4.


Parallel Synthesis of Hexahydrodiimidazodiazepines Heterocyclic Peptidomimetics and Their in Vitro and in Vivo Activities at μ (MOR), δ (DOR), and κ (KOR) Opioid Receptors.

Eans SO, Ganno ML, Mizrachi E, Houghten RA, Dooley CT, McLaughlin JP, Nefzi A.

J Med Chem. 2015 Jun 25;58(12):4905-17. doi: 10.1021/jm501637c. Epub 2015 Jun 4.


Combinatorial Libraries As a Tool for the Discovery of Novel, Broad-Spectrum Antibacterial Agents Targeting the ESKAPE Pathogens.

Fleeman R, LaVoi TM, Santos RG, Morales A, Nefzi A, Welmaker GS, Medina-Franco JL, Giulianotti MA, Houghten RA, Shaw LN.

J Med Chem. 2015 Apr 23;58(8):3340-55. doi: 10.1021/jm501628s. Epub 2015 Apr 1.


Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.

Hu M, Giulianotti MA, McLaughlin JP, Shao J, Debevec G, Maida LE, Geer P, Cazares M, Misler J, Li L, Dooley C, Ganno ML, Eans SO, Mizrachi E, Santos RG, Yongye AB, Houghten RA, Yu Y.

Eur J Med Chem. 2015 Mar 6;92:270-81. doi: 10.1016/j.ejmech.2014.12.049. Epub 2014 Dec 29.


Discovery of a potent and selective α3β4 nicotinic acetylcholine receptor antagonist from an α-conotoxin synthetic combinatorial library.

Chang YP, Banerjee J, Dowell C, Wu J, Gyanda R, Houghten RA, Toll L, McIntosh JM, Armishaw CJ.

J Med Chem. 2014 Apr 24;57(8):3511-21. doi: 10.1021/jm500183r. Epub 2014 Apr 3.


Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).

Haslach EM, Huang H, Dirain M, Debevec G, Geer P, Santos RG, Giulianotti MA, Pinilla C, Appel JR, Doering SR, Walters MA, Houghten RA, Haskell-Luevano C.

J Med Chem. 2014 Jun 12;57(11):4615-28. doi: 10.1021/jm500064t. Epub 2014 May 14.


Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis.

Onwuha-Ekpete L, Tack L, Knapinska A, Smith L, Kaushik G, Lavoi T, Giulianotti M, Houghten RA, Fields GB, Minond D.

J Med Chem. 2014 Feb 27;57(4):1599-608. doi: 10.1021/jm4019542. Epub 2014 Feb 5.


Libraries from Libraries: A Series of Sulfonamide Linked Heterocycles Derived from the Same Scaffold.

Debevec G, Chen W, Yu Y, Houghten RA, Giulianotti MA.

Tetrahedron Lett. 2013 Aug 7;54(32). doi: 10.1016/j.tetlet.2013.06.003.


Glycosylation of a disintegrin and metalloprotease 17 affects its activity and inhibition.

Chavaroche A, Cudic M, Giulianotti M, Houghten RA, Fields GB, Minond D.

Anal Biochem. 2014 Mar 15;449:68-75. doi: 10.1016/j.ab.2013.12.018. Epub 2013 Dec 19.


Scaffold ranking and positional scanning utilized in the discovery of nAChR-selective compounds suitable for optimization studies.

Wu J, Zhang Y, Maida LE, Santos RG, Welmaker GS, LaVoi TM, Nefzi A, Yu Y, Houghten RA, Toll L, Giulianotti MA.

J Med Chem. 2013 Dec 27;56(24):10103-17. doi: 10.1021/jm401543h. Epub 2013 Dec 12.


Dissociation of antimicrobial and hemolytic activities of gramicidin S through N-methylation modification.

Li Y, Bionda N, Yongye A, Geer P, Stawikowski M, Cudic P, Martinez K, Houghten RA.

ChemMedChem. 2013 Nov;8(11):1865-72. doi: 10.1002/cmdc.201300232. Epub 2013 Sep 10.


Conditional probabilistic analysis for prediction of the activity landscape and relative compound activities.

Santos RG, Giulianotti MA, Houghten RA, Medina-Franco JL.

J Chem Inf Model. 2013 Oct 28;53(10):2613-25. doi: 10.1021/ci400243e. Epub 2013 Sep 17.


Ligand/kappa-opioid receptor interactions: insights from the X-ray crystal structure.

Martinez-Mayorga K, Byler KG, Yongye AB, Giulianotti MA, Dooley CT, Houghten RA.

Eur J Med Chem. 2013 Aug;66:114-21. doi: 10.1016/j.ejmech.2013.05.021. Epub 2013 May 30.


Selective agonists and antagonists of formylpeptide receptors: duplex flow cytometry and mixture-based positional scanning libraries.

Pinilla C, Edwards BS, Appel JR, Yates-Gibbins T, Giulianotti MA, Medina-Franco JL, Young SM, Santos RG, Sklar LA, Houghten RA.

Mol Pharmacol. 2013 Sep;84(3):314-24. doi: 10.1124/mol.113.086595. Epub 2013 Jun 20.


Activity of ADAM17 (a disintegrin and metalloprotease 17) is regulated by its noncatalytic domains and secondary structure of its substrates.

Stawikowska R, Cudic M, Giulianotti M, Houghten RA, Fields GB, Minond D.

J Biol Chem. 2013 Aug 2;288(31):22871-9. doi: 10.1074/jbc.M113.462267. Epub 2013 Jun 18.


Parallel synthesis of 1,6-disubstituted-1,2,4-triazin-3-ones on solid-phase.

Hu M, Huang W, Giulianotti MA, Houghten RA, Yu Y.

ACS Comb Sci. 2013 Jul 8;15(7):335-9. doi: 10.1021/co400064d. Epub 2013 Jun 13.


The mathematics of a successful deconvolution: a quantitative assessment of mixture-based combinatorial libraries screened against two formylpeptide receptors.

Santos RG, Appel JR, Giulianotti MA, Edwards BS, Sklar LA, Houghten RA, Pinilla C.

Molecules. 2013 May 30;18(6):6408-24. doi: 10.3390/molecules18066408.


Rapid scanning structure-activity relationships in combinatorial data sets: identification of activity switches.

Medina-Franco JL, Edwards BS, Pinilla C, Appel JR, Giulianotti MA, Santos RG, Yongye AB, Sklar LA, Houghten RA.

J Chem Inf Model. 2013 Jun 24;53(6):1475-85. doi: 10.1021/ci400192y. Epub 2013 Jun 7.


The role of imidazole in peptide cyclization by transesterification: parallels to the catalytic triads of serine proteases.

Byler KG, Li Y, Houghten RA, Martinez-Mayorga K.

Org Biomol Chem. 2013 May 14;11(18):2979-87. doi: 10.1039/c3ob27464k.


Identification of a small molecule that selectively inhibits mouse PC2 over mouse PC1/3: a computational and experimental study.

Yongye AB, Vivoli M, Lindberg I, Appel JR, Houghten RA, Martinez-Mayorga K.

PLoS One. 2013;8(2):e56957. doi: 10.1371/journal.pone.0056957. Epub 2013 Feb 22.


Discovery of novel antinociceptive α-conotoxin analogues from the direct in vivo screening of a synthetic mixture-based combinatorial library.

Armishaw CJ, Banerjee J, Ganno ML, Reilley KJ, Eans SO, Mizrachi E, Gyanda R, Hoot MR, Houghten RA, McLaughlin JP.

ACS Comb Sci. 2013 Mar 11;15(3):153-61. doi: 10.1021/co300152x. Epub 2013 Feb 27.


HTS by NMR of combinatorial libraries: a fragment-based approach to ligand discovery.

Wu B, Zhang Z, Noberini R, Barile E, Giulianotti M, Pinilla C, Houghten RA, Pasquale EB, Pellecchia M.

Chem Biol. 2013 Jan 24;20(1):19-33. doi: 10.1016/j.chembiol.2012.10.015.


Shifting from the single to the multitarget paradigm in drug discovery.

Medina-Franco JL, Giulianotti MA, Welmaker GS, Houghten RA.

Drug Discov Today. 2013 May;18(9-10):495-501. doi: 10.1016/j.drudis.2013.01.008. Epub 2013 Jan 20. Review.


Identification of B cell and T cell epitopes using synthetic peptide combinatorial libraries.

Pinilla C, Appel JR, Judkowski V, Houghten RA.

Curr Protoc Immunol. 2012 Nov;Chapter 9:Unit9.5. doi: 10.1002/0471142735.im0905s99.


The Multi-Leu peptide inhibitor discriminates between PACE4 and furin and exhibits antiproliferative effects on prostate cancer cells.

Levesque C, Fugère M, Kwiatkowska A, Couture F, Desjardins R, Routhier S, Moussette P, Prahl A, Lammek B, Appel JR, Houghten RA, D'Anjou F, Dory YL, Neugebauer W, Day R.

J Med Chem. 2012 Dec 13;55(23):10501-11. doi: 10.1021/jm3011178. Epub 2012 Nov 14.


Fluorescent mu selective opioid ligands from a mixture based cyclic peptide library.

Li Y, Dooley CT, Misler JA, Debevec G, Giulianotti MA, Cazares ME, Maida L, Houghten RA.

ACS Comb Sci. 2012 Dec 10;14(12):673-9. doi: 10.1021/co300110t. Epub 2012 Nov 8.


Palladium-catalyzed C-H functionalization using guanidine as a directing group: ortho arylation and olefination of arylguanidines.

Shao J, Chen W, Giulianotti MA, Houghten RA, Yu Y.

Org Lett. 2012 Nov 2;14(21):5452-5. doi: 10.1021/ol302533w. Epub 2012 Oct 24.


Discovery of novel inhibitors of a disintegrin and metalloprotease 17 (ADAM17) using glycosylated and non-glycosylated substrates.

Minond D, Cudic M, Bionda N, Giulianotti M, Maida L, Houghten RA, Fields GB.

J Biol Chem. 2012 Oct 19;287(43):36473-87. doi: 10.1074/jbc.M112.389114. Epub 2012 Aug 27.


A novel method for the determination of isokinetic ratios and its application in the synthesis of two new positional scanning libraries.

Giulianotti MA, Debevec G, Santos RG, Maida LE, Chen W, Ou L, Yu Y, Dooley CT, Houghten RA.

ACS Comb Sci. 2012 Sep 10;14(9):503-12. doi: 10.1021/co300060s. Epub 2012 Aug 28.


Expanding the medicinally relevant chemical space with compound libraries.

López-Vallejo F, Giulianotti MA, Houghten RA, Medina-Franco JL.

Drug Discov Today. 2012 Jul;17(13-14):718-26. doi: 10.1016/j.drudis.2012.04.001. Epub 2012 Apr 10. Review.


Multitarget structure-activity relationships characterized by activity-difference maps and consensus similarity measure.

Medina-Franco JL, Yongye AB, Pérez-Villanueva J, Houghten RA, Martínez-Mayorga K.

J Chem Inf Model. 2011 Sep 26;51(9):2427-39. doi: 10.1021/ci200281v. Epub 2011 Aug 29.


Antagonists of IAP-family anti-apoptotic proteins - Probe 2.

Lopez M, Welsh K, Yuan H, Stonich D, Su Y, Garcia X, Cuddy M, Houghten R, Sergienko E, Reed JC, Ardecky R, Reddy S, Finlay D, Vuori K, Dad S, Chung TDY, Cosford NDP.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 Sep 1 [updated 2011 Feb 10].

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