Pesquisa | BVS Doenças Infecciosas e Parasitárias

1.

Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.

Schubart, Anna; Anderson, Karen; Mainolfi, Nello; Sellner, Holger; Ehara, Takeru; Adams, Christopher M; Mac Sweeney, Aengus; Liao, Sha-Mei; Crowley, Maura; Littlewood-Evans, Amanda; Sarret, Sophie; Wieczorek, Grazyna; Perrot, Ludovic; Dubost, Valérie; Flandre, Thierry; Zhang, Yuzhou; Smith, Richard J H; Risitano, Antonio M; Karki, Rajeshri G; Zhang, Chun; Valeur, Eric; Sirockin, Finton; Gerhartz, Bernd; Erbel, Paulus; Hughes, Nicola; Smith, Thomas M; Cumin, Frederic; Argikar, Upendra A; Haraldsson, Börje; Mogi, Muneto; Sedrani, Richard; Wiesmann, Christian; Jaffee, Bruce; Maibaum, Jürgen; Flohr, Stefanie; Harrison, Richard; Eder, Jörg.

Proc Natl Acad Sci U S A ; 116(16): 7926-7931, 2019 04 16.

Artigo em Inglês | MEDLINE | ID: mdl-30926668

2.

A small-molecule inhibitor of C5 complement protein.

Jendza, Keith; Kato, Mitsunori; Salcius, Michael; Srinivas, Honnappa; De Erkenez, Andrea; Nguyen, Anh; McLaughlin, Doug; Be, Celine; Wiesmann, Christian; Murphy, Jason; Bolduc, Philippe; Mogi, Muneto; Duca, Jose; Namil, Abdel; Capparelli, Michael; Darsigny, Veronique; Meredith, Erik; Tichkule, Ritesh; Ferrara, Luciana; Heyder, Jessica; Liu, Fang; Horton, Patricia A; Romanowski, Michael J; Schirle, Markus; Mainolfi, Nello; Anderson, Karen; Michaud, Gregory A.

Nat Chem Biol ; 15(7): 666-668, 2019 07.

Artigo em Inglês | MEDLINE | ID: mdl-31209353

3.

Human SHMT inhibitors reveal defective glycine import as a targetable metabolic vulnerability of diffuse large B-cell lymphoma.

Ducker, Gregory S; Ghergurovich, Jonathan M; Mainolfi, Nello; Suri, Vipin; Jeong, Stephanie K; Hsin-Jung Li, Sophia; Friedman, Adam; Manfredi, Mark G; Gitai, Zemer; Kim, Hahn; Rabinowitz, Joshua D.

Proc Natl Acad Sci U S A ; 114(43): 11404-11409, 2017 10 24.

Artigo em Inglês | MEDLINE | ID: mdl-29073064

4.

Targeted protein degradation mechanisms.

Zhang, Yi; Loh, Christine; Chen, Jesse; Mainolfi, Nello.

Drug Discov Today Technol ; 31: 53-60, 2019 Apr.

Artigo em Inglês | MEDLINE | ID: mdl-31200860

5.

IRAK4 degrader in hidradenitis suppurativa and atopic dermatitis: a phase 1 trial.

Ackerman, Lindsay; Acloque, Gerard; Bacchelli, Sandro; Schwartz, Howard; Feinstein, Brian J; La Stella, Phillip; Alavi, Afsaneh; Gollerkeri, Ashwin; Davis, Jeffrey; Campbell, Veronica; McDonald, Alice; Agarwal, Sagar; Karnik, Rahul; Shi, Kelvin; Mishkin, Aimee; Culbertson, Jennifer; Klaus, Christine; Enerson, Bradley; Massa, Virginia; Kuhn, Eric; Sharma, Kirti; Keaney, Erin; Barnes, Randy; Chen, Dapeng; Zheng, Xiaozhang; Rong, Haojing; Sabesan, Vijay; Ho, Chris; Mainolfi, Nello; Slavin, Anthony; Gollob, Jared A.

Nat Med ; 29(12): 3127-3136, 2023 Dec.

Artigo em Inglês | MEDLINE | ID: mdl-37957373

6.

Serine synthesis pathway inhibition cooperates with dietary serine and glycine limitation for cancer therapy.

Tajan, Mylène; Hennequart, Marc; Cheung, Eric C; Zani, Fabio; Hock, Andreas K; Legrave, Nathalie; Maddocks, Oliver D K; Ridgway, Rachel A; Athineos, Dimitris; Suárez-Bonnet, Alejandro; Ludwig, Robert L; Novellasdemunt, Laura; Angelis, Nikolaos; Li, Vivian S W; Vlachogiannis, Georgios; Valeri, Nicola; Mainolfi, Nello; Suri, Vipin; Friedman, Adam; Manfredi, Mark; Blyth, Karen; Sansom, Owen J; Vousden, Karen H.

Nat Commun ; 12(1): 366, 2021 01 14.

Artigo em Inglês | MEDLINE | ID: mdl-33446657

7.

Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.

Mainolfi, Nello; Ehara, Takeru; Karki, Rajeshri G; Anderson, Karen; Mac Sweeney, Aengus; Liao, Sha-Mei; Argikar, Upendra A; Jendza, Keith; Zhang, Chun; Powers, James; Klosowski, Daniel W; Crowley, Maura; Kawanami, Toshio; Ding, Jian; April, Myriam; Forster, Cornelia; Serrano-Wu, Michael; Capparelli, Michael; Ramqaj, Rrezarta; Solovay, Catherine; Cumin, Frederic; Smith, Thomas M; Ferrara, Luciana; Lee, Wendy; Long, Debby; Prentiss, Melissa; De Erkenez, Andrea; Yang, Louis; Liu, Fang; Sellner, Holger; Sirockin, Finton; Valeur, Eric; Erbel, Paulus; Ostermeier, Daniela; Ramage, Paul; Gerhartz, Bernd; Schubart, Anna; Flohr, Stefanie; Gradoux, Nathalie; Feifel, Roland; Vogg, Barbara; Wiesmann, Christian; Maibaum, Jürgen; Eder, Jörg; Sedrani, Richard; Harrison, Richard A; Mogi, Muneto; Jaffee, Bruce D; Adams, Christopher M.

J Med Chem ; 63(11): 5697-5722, 2020 06 11.

Artigo em Inglês | MEDLINE | ID: mdl-32073845

8.

Limited Environmental Serine and Glycine Confer Brain Metastasis Sensitivity to PHGDH Inhibition.

Ngo, Bryan; Kim, Eugenie; Osorio-Vasquez, Victoria; Doll, Sophia; Bustraan, Sophia; Liang, Roger J; Luengo, Alba; Davidson, Shawn M; Ali, Ahmed; Ferraro, Gino B; Fischer, Grant M; Eskandari, Roozbeh; Kang, Diane S; Ni, Jing; Plasger, Ariana; Rajasekhar, Vinagolu K; Kastenhuber, Edward R; Bacha, Sarah; Sriram, Roshan K; Stein, Benjamin D; Bakhoum, Samuel F; Snuderl, Matija; Cotzia, Paolo; Healey, John H; Mainolfi, Nello; Suri, Vipin; Friedman, Adam; Manfredi, Mark; Sabatini, David M; Jones, Drew R; Yu, Min; Zhao, Jean J; Jain, Rakesh K; Keshari, Kayvan R; Davies, Michael A; Vander Heiden, Matthew G; Hernando, Eva; Mann, Matthias; Cantley, Lewis C; Pacold, Michael E.

Cancer Discov ; 10(9): 1352-1373, 2020 09.

Artigo em Inglês | MEDLINE | ID: mdl-32571778

9.

Serine Metabolism Supports Macrophage IL-1ß Production.

Rodriguez, Arianne E; Ducker, Gregory S; Billingham, Leah K; Martinez, Carlos A; Mainolfi, Nello; Suri, Vipin; Friedman, Adam; Manfredi, Mark G; Weinberg, Samuel E; Rabinowitz, Joshua D; Chandel, Navdeep S.

Cell Metab ; 29(4): 1003-1011.e4, 2019 04 02.

Artigo em Inglês | MEDLINE | ID: mdl-30773464

10.

Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.

Karki, Rajeshri G; Powers, James; Mainolfi, Nello; Anderson, Karen; Belanger, David B; Liu, Donglei; Ji, Nan; Jendza, Keith; Gelin, Christine F; Mac Sweeney, Aengus; Solovay, Catherine; Delgado, Omar; Crowley, Maura; Liao, Sha-Mei; Argikar, Upendra A; Flohr, Stefanie; La Bonte, Laura R; Lorthiois, Edwige L; Vulpetti, Anna; Brown, Ann; Long, Debby; Prentiss, Melissa; Gradoux, Nathalie; de Erkenez, Andrea; Cumin, Frederic; Adams, Christopher; Jaffee, Bruce; Mogi, Muneto.

J Med Chem ; 62(9): 4656-4668, 2019 05 09.

Artigo em Inglês | MEDLINE | ID: mdl-30995036

11.

The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.

Adams, Christopher M; Anderson, Karen; Artman, Gerald; Bizec, Jean-Claude; Cepeda, Rosemarie; Elliott, Jason; Fassbender, Elizabeth; Ghosh, Malay; Hanks, Shawn; Hardegger, Leo A; Hosagrahara, Vinayak P; Jaffee, Bruce; Jendza, Keith; Ji, Nan; Johnson, Leland; Lee, Wendy; Liu, Donglei; Liu, Fang; Long, Debby; Ma, Fupeng; Mainolfi, Nello; Meredith, Erik L; Miranda, Karl; Peng, Yao; Poor, Stephen; Powers, James; Qiu, Yubin; Rao, Chang; Shen, Siyuan; Sivak, Jeremy M; Solovay, Catherine; Tarsa, Peter; Woolfenden, Amber; Zhang, Chun; Zhang, Yiqin.

J Med Chem ; 61(4): 1622-1635, 2018 02 22.

Artigo em Inglês | MEDLINE | ID: mdl-29400470

12.

Serine Is an Essential Metabolite for Effector T Cell Expansion.

Ma, Eric H; Bantug, Glenn; Griss, Takla; Condotta, Stephanie; Johnson, Radia M; Samborska, Bozena; Mainolfi, Nello; Suri, Vipin; Guak, Hannah; Balmer, Maria L; Verway, Mark J; Raissi, Thomas C; Tsui, Harmony; Boukhaled, Giselle; Henriques da Costa, Sofia; Frezza, Christian; Krawczyk, Connie M; Friedman, Adam; Manfredi, Mark; Richer, Martin J; Hess, Christoph; Jones, Russell G.

Cell Metab ; 25(2): 345-357, 2017 02 07.

Artigo em Inglês | MEDLINE | ID: mdl-28111214

13.

Evolution of a New Class of VEGFR-2 Inhibitors from Scaffold Morphing and Redesign.

Mainolfi, Nello; Karki, Rajeshri; Liu, Fang; Anderson, Karen.

ACS Med Chem Lett ; 7(4): 363-7, 2016 Apr 14.

Artigo em Inglês | MEDLINE | ID: mdl-27096042

14.

Core Replacements in a Potent Series of VEGFR-2 Inhibitors and Their Impact on Potency, Solubility, and hERG.

Mainolfi, Nello; Powers, James; Meredith, Erik; Elliott, Jason; Gunderson, Karl G; Poor, Stephen; Liu, Fang; Anderson, Karen.

ACS Med Chem Lett ; 7(4): 357-62, 2016 Apr 14.

Artigo em Inglês | MEDLINE | ID: mdl-27096041

15.

The intermolecular Pauson-Khand reaction.

Gibson, Susan E; Mainolfi, Nello.

Angew Chem Int Ed Engl ; 44(20): 3022-37, 2005 May 13.

Artigo em Inglês | MEDLINE | ID: mdl-15800868

16.

Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration.

Meredith, Erik L; Mainolfi, Nello; Poor, Stephen; Qiu, Yubin; Miranda, Karl; Powers, James; Liu, Donglei; Ma, Fupeng; Solovay, Catherine; Rao, Chang; Johnson, Leland; Ji, Nan; Artman, Gerald; Hardegger, Leo; Hanks, Shawn; Shen, Siyuan; Woolfenden, Amber; Fassbender, Elizabeth; Sivak, Jeremy M; Zhang, Yiqin; Long, Debby; Cepeda, Rosemarie; Liu, Fang; Hosagrahara, Vinayak P; Lee, Wendy; Tarsa, Peter; Anderson, Karen; Elliott, Jason; Jaffee, Bruce.

J Med Chem ; 58(23): 9273-86, 2015 Dec 10.

Artigo em Inglês | MEDLINE | ID: mdl-26568411

17.

An effective prodrug strategy to selectively enhance ocular exposure of a cannabinoid receptor (CB1/2) agonist.

Mainolfi, Nello; Powers, James; Amin, Jakal; Long, Debby; Lee, Wendy; McLaughlin, Margaret E; Jaffee, Bruce; Brain, Christopher; Elliott, Jason; Sivak, Jeremy M.

J Med Chem ; 56(13): 5464-72, 2013 Jul 11.

Artigo em Inglês | MEDLINE | ID: mdl-23738526

18.

Serine Is an Essential Metabolite for Effector T Cell Expansion.

Ma, Eric H; Bantug, Glenn; Griss, Takla; Condotta, Stephanie; Johnson, Radia M; Samborska, Bozena; Mainolfi, Nello; Suri, Vipin; Guak, Hannah; Balmer, Maria L; Verway, Mark J; Raissi, Thomas C; Tsui, Harmony; Boukhaled, Giselle; Henriques da Costa, Sofia; Frezza, Christian; Krawczyk, Connie M; Friedman, Adam; Manfredi, Mark; Richer, Martin J; Hess, Christoph; Jones, Russell G.

Cell Metab ; 25(2): 482, 2017 02 07.

Artigo em Inglês | MEDLINE | ID: mdl-28178570

19.

Continuous flow coupling and decarboxylation reactions promoted by copper tubing.

Zhang, Yun; Jamison, Timothy F; Patel, Sejal; Mainolfi, Nello.

Org Lett ; 13(2): 280-3, 2011 Jan 21.

Artigo em Inglês | MEDLINE | ID: mdl-21141809

20.

A cyclobutadiene equivalent in the catalytic Pauson-Khand reaction.

Gibson, Susan E; Mainolfi, Nello; Kalindjian, S Barret; Wright, Paul T.

Angew Chem Int Ed Engl ; 43(42): 5680-2, 2004 Oct 25.

Artigo em Inglês | MEDLINE | ID: mdl-15495152

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Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.

A small-molecule inhibitor of C5 complement protein.

Human SHMT inhibitors reveal defective glycine import as a targetable metabolic vulnerability of diffuse large B-cell lymphoma.

Targeted protein degradation mechanisms.

IRAK4 degrader in hidradenitis suppurativa and atopic dermatitis: a phase 1 trial.

Serine synthesis pathway inhibition cooperates with dietary serine and glycine limitation for cancer therapy.

Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.

Limited Environmental Serine and Glycine Confer Brain Metastasis Sensitivity to PHGDH Inhibition.

Serine Metabolism Supports Macrophage IL-1ß Production.

Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.

The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.

Serine Is an Essential Metabolite for Effector T Cell Expansion.

Evolution of a New Class of VEGFR-2 Inhibitors from Scaffold Morphing and Redesign.

Core Replacements in a Potent Series of VEGFR-2 Inhibitors and Their Impact on Potency, Solubility, and hERG.

The intermolecular Pauson-Khand reaction.

Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration.

An effective prodrug strategy to selectively enhance ocular exposure of a cannabinoid receptor (CB1/2) agonist.

Serine Is an Essential Metabolite for Effector T Cell Expansion.

Continuous flow coupling and decarboxylation reactions promoted by copper tubing.

A cyclobutadiene equivalent in the catalytic Pauson-Khand reaction.