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Publications 2011

Mechanistic implications for LDL receptor degradation from the PCSK9/LDLR structure at neutral pH.

Lo Surdo P, Bottomley MJ, Calzetta A, Settembre EC, Cirillo A, Pandit S, Ni YG, Hubbard B, Sitlani A, Carfí A. (2011)
EMBO Rep. 2011 Dec 1;12(12):1300-5.

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Structure of herpes simplex virus glycoprotein D bound to the human receptor nectin-1.

Di Giovine P, Settembre EC, Bhargava AK, Luftig MA, Lou H, Cohen GH, Eisenberg RJ, Krummenacher C, Carfi A. (2011)
PLoS Pathog. 2011 Sep;7(9):e1002277.

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Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors.

Ontoria JM, Bufi LL, Torrisi C, Bresciani A, Giomini C, Rowley M, Serafini S, Bin H, Hao W, Steinkühler C, Jones P. (2011)
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5274-82.

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N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists.

Muraglia E, Ontoria JM, Branca D, Dessole G, Bresciani A, Fonsi M, Giuliano C, Llauger Bufi L, Monteagudo E, Palumbi MC, Torrisi C, Rowley M, Steinkühler C, Jones P. (2011)
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5283-8.

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Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 1.

Malancona S, Altamura S, Filocamo G, Kinzel O, Hernando JI, Rowley M, Scarpelli R, Steinkühler C, Jones P. (2011)
Bioorg Med Chem Lett. 2011 Aug 1;21(15):4422-8.

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Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 2.

Kinzel O, Alfieri A, Altamura S, Brunetti M, Bufali S, Colaceci F, Ferrigno F, Filocamo G, Fonsi M, Gallinari P, Malancona S, Hernando JI, Monteagudo E, Orsale MV, Palumbi MC, Pucci V, Rowley M, Sasso R, Scarpelli R, Steinkühler C, Jones P. (2011)
Bioorg Med Chem Lett. 2011 Aug 1;21(15):4429-35.

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Intratumor RNA interference of cell cycle genes slows down tumor progression.

Dharmapuri S, Peruzzi D, Marra E, Palombo F, Bett AJ, Bartz SR, Yong M, Ciliberto G, La Monica N, Buser CA, Toniatti C, Aurisicchio L. (2011)
Gene Ther. 2011 Jul;18(7):727-33.

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