Search Results - "Albom, Mark S"

Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK) by Ott, Gregory R, Cheng, Mangeng, Learn, Keith S, Wagner, Jason, Gingrich, Diane E, Lisko, Joseph G, Curry, Matthew, Mesaros, Eugen F, Ghose, Arup K, Quail, Matthew R, Wan, Weihua, Lu, Lihui, Dobrzanski, Pawel, Albom, Mark S, Angeles, Thelma S, Wells-Knecht, Kevin, Huang, Zeqi, Aimone, Lisa D, Bruckheimer, Elizabeth, Anderson, Nathan, Friedman, Jay, Fernandez, Sandra V, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D

“…Analogues structurally related to anaplastic lymphoma kinase (ALK) inhibitor 1 were optimized for metabolic stability. The results from this endeavor not only…”
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Depletion of autoreactive plasma cells and treatment of lupus nephritis in mice using CEP-33779, a novel, orally active, selective inhibitor of JAK2 by Lu, Lily D, Stump, Kristine L, Wallace, Nate H, Dobrzanski, Pawel, Serdikoff, Cynthia, Gingrich, Diane E, Dugan, Benjamin J, Angeles, Thelma S, Albom, Mark S, Mason, Jennifer L, Ator, Mark A, Dorsey, Bruce D, Ruggeri, Bruce A, Seavey, Matthew M

“…Accumulating evidence suggests that autoreactive plasma cells play an important role in systemic lupus erythematosus (SLE). In addition, several…”
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A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis by Stump, Kristine L, Lu, Lily D, Dobrzanski, Pawel, Serdikoff, Cynthia, Gingrich, Diane E, Dugan, Ben J, Angeles, Thelma S, Albom, Mark S, Ator, Mark A, Dorsey, Bruce D, Ruggeri, Bruce A, Seavey, Matthew M

“…Janus kinase 2 (JAK2) is involved in the downstream activation of signal transducer and activator of transcription 3 (STAT3) and STAT5 and is responsible for…”
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Discovery of an Orally Efficacious Inhibitor of Anaplastic Lymphoma Kinase by Gingrich, Diane E, Lisko, Joseph G, Curry, Matthew A, Cheng, Mangeng, Quail, Matthew, Lu, Lihui, Wan, Weihua, Albom, Mark S, Angeles, Thelma S, Aimone, Lisa D, Haltiwanger, R. Curtis, Wells-Knecht, Kevin, Ott, Gregory R, Ghose, Arup K, Ator, Mark A, Ruggeri, Bruce, Dorsey, Bruce D

“…Anaplastic lymphoma kinase (ALK) is a promising therapeutic target for the treatment of cancer, supported by considerable favorable preclinical and clinical…”
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Anaplastic lymphoma kinase activity is essential for the proliferation and survival of anaplastic large-cell lymphoma cells by Wan, Weihua, Albom, Mark S., Lu, Lihui, Quail, Matthew R., Becknell, Nadine C., Weinberg, Linda R., Reddy, Dandu R., Holskin, Beverly P., Angeles, Thelma S., Underiner, Ted L., Meyer, Sheryl L., Hudkins, Robert L., Dorsey, Bruce D., Ator, Mark A., Ruggeri, Bruce A., Cheng, Mangeng

“…The roles of aberrant expression of constitutively active ALK chimeric proteins in the pathogenesis of anaplastic large-cell lymphoma (ALCL) have been well…”
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Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis by Tripathy, Rabindranath, Reiboldt, Alyssa, Messina, Patricia A., Iqbal, Mohamed, Singh, Jasbir, Bacon, Edward R., Angeles, Thelma S., Yang, Shi X., Albom, Mark S., Robinson, Candy, Chang, Hong, Ruggeri, Bruce A., Mallamo, John P.

“…Structural analysis of the essential binding elements of the oxindole-based kinase inhibitor ( 1) led to the identification of a novel class of…”
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Strategies to Mitigate the Bioactivation of 2-Anilino-7-Aryl-Pyrrolo[2,1-f][1,2,4]triazines: Identification of Orally Bioavailable, Efficacious ALK Inhibitors by Mesaros, Eugen F, Thieu, Tho V, Wells, Gregory J, Zificsak, Craig A, Wagner, Jason C, Breslin, Henry J, Tripathy, Rabindranath, Diebold, James L, McHugh, Robert J, Wohler, Ashley T, Quail, Matthew R, Wan, Weihua, Lu, Lihui, Huang, Zeqi, Albom, Mark S, Angeles, Thelma S, Wells-Knecht, Kevin J, Aimone, Lisa D, Cheng, Mangeng, Ator, Mark A, Ott, Gregory R, Dorsey, Bruce D

“…Chemical strategies to mitigate cytochrome P450-mediated bioactivation of novel 2,7-disubstituted pyrrolo­[2,1-f]­[1,2,4]­triazine ALK inhibitors are described…”
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ALK Mutants in the Kinase Domain Exhibit Altered Kinase Activity and Differential Sensitivity to Small Molecule ALK Inhibitors by Lu, Lihui, Ghose, Arup K, Quail, Matthew R, Albom, Mark S, Durkin, John T, Holskin, Beverly P, Angeles, Thelma S, Meyer, Sheryl L, Ruggeri, Bruce A, Cheng, Mangeng

“…Abnormal expression of constitutively active anaplastic lymphoma kinase (ALK) chimeric proteins in the pathogenesis of anaplastic large-cell lymphoma (ALCL) is…”
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CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers by Cheng, Mangeng, Quail, Matthew R, Gingrich, Diane E, Ott, Gregory R, Lu, Lihui, Wan, Weihua, Albom, Mark S, Angeles, Thelma S, Aimone, Lisa D, Cristofani, Flavio, Machiorlatti, Rodolfo, Abele, Cristina, Ator, Mark A, Dorsey, Bruce D, Inghirami, Giorgio, Ruggeri, Bruce A

“…Anaplastic lymphoma kinase (ALK) is constitutively activated in a number of human cancer types due to chromosomal translocations, point mutations, and gene…”
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A Selective, Orally Bioavailable 1,2,4-Triazolo[1,5-a]pyridine-Based Inhibitor of Janus Kinase 2 for Use in Anticancer Therapy: Discovery of CEP-33779 by Dugan, Benjamin J, Gingrich, Diane E, Mesaros, Eugen F, Milkiewicz, Karen L, Curry, Matthew A, Zulli, Allison L, Dobrzanski, Pawel, Serdikoff, Cynthia, Jan, Mahfuza, Angeles, Thelma S, Albom, Mark S, Mason, Jennifer L, Aimone, Lisa D, Meyer, Sheryl L, Huang, Zeqi, Wells-Knecht, Kevin J, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D

“…Members of the JAK family of nonreceptor tyrosine kinases play a critical role in the growth and progression of many cancers and in inflammatory diseases. JAK2…”
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Design, Synthesis, and Anaplastic Lymphoma Kinase (ALK) Inhibitory Activity for a Novel Series of 2,4,8,22-Tetraazatetracyclo[14.3.1.13,7.19,13]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene Macrocycles by Breslin, Henry J, Lane, Brandon M, Ott, Gregory R, Ghose, Arup K, Angeles, Thelma S, Albom, Mark S, Cheng, Mangeng, Wan, Weihua, Haltiwanger, R. Curtis, Wells-Knecht, Kevin J, Dorsey, Bruce D

“…A novel set of 2,4,8,22-tetraazatetracyclo­[14.3.1.13,7.19,13]­docosa-1­(20),3­(22),4,6,9­(21),10,12,16,18-nonaene macrocycles were prepared as potential…”
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Synthesis and Biological Profile of the pan-Vascular Endothelial Growth Factor Receptor/Tyrosine Kinase with Immunoglobulin and Epidermal Growth Factor-Like Homology Domains 2 (VEGF-R/TIE-2) Inhibitor 11-(2-Methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): A Novel Oncology Therapeutic Agent by Hudkins, Robert L, Becknell, Nadine C, Zulli, Allison L, Underiner, Ted L, Angeles, Thelma S, Aimone, Lisa D, Albom, Mark S, Chang, Hong, Miknyoczki, Sheila J, Hunter, Kathryn, Jones-Bolin, Susan, Zhao, Hugh, Bacon, Edward R, Mallamo, John P, Ator, Mark A, Ruggeri, Bruce A

“…A substantial body of evidence supports the utility of antiangiogenesis inhibitors as a strategy to block or attenuate tumor-induced angiogenesis and…”
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Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase by Mesaros, Eugen F., Angeles, Thelma S., Albom, Mark S., Wagner, Jason C., Aimone, Lisa D., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Olsen, Mark, Kordwitz, Emily, Haltiwanger, R. Curtis, Landis, Amy J., Cheng, Mangeng, Ruggeri, Bruce A., Ator, Mark A., Dorsey, Bruce D., Ott, Gregory R.

“…[Display omitted] The diastereoselective synthesis and biological activity of piperidine-3,4-diol and piperidine-3-ol-derived pyrrolotriazine inhibitors of…”
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1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors by Tripathy, Rabindranath, Ghose, Arup, Singh, Jasbir, Bacon, Edward R., Angeles, Thelma S., Yang, Shi X., Albom, Mark S., Aimone, Lisa D., Herman, Joseph L., Mallamo, John P.

“…Discovery of 1,2,3-Thiadiazole substituted pyrazolones as potent KDR kinase inhibitors along with their potency, cellular data, improved PK profile, and…”
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2,7-Disubstituted-pyrrolo[2,1-f][1,2,4]triazines: New Variant of an Old Template and Application to the Discovery of Anaplastic Lymphoma Kinase (ALK) Inhibitors with in Vivo Antitumor Activity by Ott, Gregory R, Wells, Gregory J, Thieu, Tho V, Quail, Matthew R, Lisko, Joseph G, Mesaros, Eugen F, Gingrich, Diane E, Ghose, Arup K, Wan, Weihua, Lu, Lihui, Cheng, Mangeng, Albom, Mark S, Angeles, Thelma S, Huang, Zeqi, Aimone, Lisa D, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D

“…A novel 2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazine scaffold has been designed as a new kinase inhibitor platform mimicking the bioactive conformation of…”
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Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: Control of selectivity by a benzyloxy group by Tripathy, Rabindranath, McHugh, Robert J., Ghose, Arup K., Ott, Gregory R., Angeles, Thelma S., Albom, Mark S., Huang, Zeck, Aimone, Lisa D., Cheng, Mangeng, Dorsey, Bruce D.

“…Anaplastic lymphoma kinase (ALK) is transmembrane receptor tyrosine kinase, with oncogenic variants that have been implicated in ALCL, NSCLC and other cancers…”
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Synthesis and structure–activity relationships of 1,2,3,4-tetrahydropyrido[2,3- b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase by Milkiewicz, Karen L., Weinberg, Linda R., Albom, Mark S., Angeles, Thelma S., Cheng, Mangeng, Ghose, Arup K., Roemmele, Renee C., Theroff, Jay P., Underiner, Ted L., Zificsak, Craig A., Dorsey, Bruce D.

“…Dysregulation of the anaplastic lymphoma kinase (ALK) is implicated in a variety of cancers. A series of tetrahydropyrido[2,3- b]pyrazines was constructed as…”
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Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models by Mesaros, Eugen F., Burke, Jason P., Parrish, Jonathan D., Dugan, Benjamin J., Anzalone, Andrew V., Angeles, Thelma S., Albom, Mark S., Aimone, Lisa D., Quail, Matthew R., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Ator, Mark A., Ruggeri, Bruce A., Cheng, Mangeng, Ott, Gregory R., Dorsey, Bruce D.

“…The synthesis and biological evaluation of potent and selective anaplastic lymphoma kinase (ALK) inhibitors from a novel class of 2,4-diaminopyrimidines,…”
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Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors by Zificsak, Craig A, Theroff, Jay P, Aimone, Lisa D, Angeles, Thelma S, Albom, Mark S, Cheng, Mangeng, Mesaros, Eugen F, Ott, Gregory R, Quail, Matthew R, Underiner, Ted L, Wan, Weihua, Dorsey, Bruce D

“…The incorporation of R,R-1,2-diaminocyclohexane at C4 in a series of 2,4-diaminopyrimidines led to a number of ALK inhibitors in which optimized activity was…”
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Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors by Weinberg, Linda R., Albom, Mark S., Angeles, Thelma S., Husten, Jean, Lisko, Joseph G., McHugh, Robert J., Milkiewicz, Karen L., Murthy, Seetha, Ott, Gregory R., Theroff, Jay P., Tripathy, Rabindranath, Underiner, Ted L., Zificsak, Craig A., Dorsey, Bruce D.

“…The HGF-c-Met signaling axis is an important paracrine mediator of epithelial–mesenchymal cell interactions involving the regulation of multiple cellular…”
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