Search Results - "Scherle, Peggy A."

The pharmacokinetics, pharmacodynamics, and safety of baricitinib, an oral JAK 1/2 inhibitor, in healthy volunteers by Shi, Jack G., Chen, Xuejun, Lee, Fiona, Emm, Thomas, Scherle, Peggy A., Lo, Yvonne, Punwani, Naresh, Williams, William V., Yeleswaram, Swamy

“…Baricitinib (also known as LY3009104 or INCB028050), a novel and potent small molecule inhibitor of Janus kinase family of enzymes (JAKs) with selectivity for…”
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Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms by Quintás-Cardama, Alfonso, Vaddi, Kris, Liu, Phillip, Manshouri, Taghi, Li, Jun, Scherle, Peggy A, Caulder, Eian, Wen, Xiaoming, Li, Yanlong, Waeltz, Paul, Rupar, Mark, Burn, Timothy, Lo, Yvonne, Kelley, Jennifer, Covington, Maryanne, Shepard, Stacey, Rodgers, James D, Haley, Patrick, Kantarjian, Hagop, Fridman, Jordan S, Verstovsek, Srdan

“…Constitutive JAK2 activation in hematopoietic cells by the JAK2V617F mutation recapitulates myeloproliferative neoplasm (MPN) phenotypes in mice, establishing…”
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Developing c-MET pathway inhibitors for cancer therapy: progress and challenges by Liu, Xiangdong, Newton, Robert C, Scherle, Peggy A

“…Successfully developed target-based therapies have significantly changed cancer treatment. Among many targets, the c-MET receptor tyrosine kinase and its…”
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INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology by Yue, Eddy W, Sparks, Richard, Polam, Padmaja, Modi, Dilip, Douty, Brent, Wayland, Brian, Glass, Brian, Takvorian, Amy, Glenn, Joseph, Zhu, Wenyu, Bower, Michael, Liu, Xiangdong, Leffet, Lynn, Wang, Qian, Bowman, Kevin J, Hansbury, Michael J, Wei, Min, Li, Yanlong, Wynn, Richard, Burn, Timothy C, Koblish, Holly K, Fridman, Jordan S, Emm, Tom, Scherle, Peggy A, Metcalf, Brian, Combs, Andrew P

“…A data-centric medicinal chemistry approach led to the invention of a potent and selective IDO1 inhibitor 4f, INCB24360 (epacadostat). The molecular structure…”
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Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity by Liu, Xiangdong, Shin, Niu, Koblish, Holly K., Yang, Gengjie, Wang, Qian, Wang, Kathy, Leffet, Lynn, Hansbury, Michael J., Thomas, Beth, Rupar, Mark, Waeltz, Paul, Bowman, Kevin J., Polam, Padmaja, Sparks, Richard B., Yue, Eddy W., Li, Yanlong, Wynn, Richard, Fridman, Jordan S., Burn, Timothy C., Combs, Andrew P., Newton, Robert C., Scherle, Peggy A.

“…Indoleamine 2,3-dioxygenase-1 (IDO1; IDO) mediates oxidative cleavage of tryptophan, an amino acid essential for cell proliferation and survival. IDO1…”
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Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050 by Fridman, Jordan S, Scherle, Peggy A, Collins, Robert, Burn, Timothy C, Li, Yanlong, Li, Jun, Covington, Maryanne B, Thomas, Beth, Collier, Paul, Favata, Margaret F, Wen, Xiaoming, Shi, Jack, McGee, Ryan, Haley, Patrick J, Shepard, Stacey, Rodgers, James D, Yeleswaram, Swamy, Hollis, Greg, Newton, Robert C, Metcalf, Brian, Friedman, Steven M, Vaddi, Kris

“…Inhibiting signal transduction induced by inflammatory cytokines offers a new approach for the treatment of autoimmune diseases such as rheumatoid arthritis…”
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Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors by Koblish, Holly K, Hansbury, Michael J, Bowman, Kevin J, Yang, Gengjie, Neilan, Claire L, Haley, Patrick J, Burn, Timothy C, Waeltz, Paul, Sparks, Richard B, Yue, Eddy W, Combs, Andrew P, Scherle, Peggy A, Vaddi, Kris, Fridman, Jordan S

“…Malignant tumors arise, in part, because the immune system does not adequately recognize and destroy them. Expression of indoleamine-2,3-dioxygenase (IDO;…”
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The Pharmacokinetics, Pharmacodynamics, and Safety of Orally Dosed INCB018424 Phosphate in Healthy Volunteers by Shi, Jack G., Chen, Xuejun, McGee, Ryan F., Landman, Robert R., Emm, Thomas, Lo, Yvonne, Scherle, Peggy A., Punwani, Naresh G., Williams, William V., Yeleswaram, Swamy

“…INCB018424 phosphate, a potent inhibitor of JAK enzymes with selectivity for JAK1&2, is in development for the treatment of myelofibrosis (MF). The oral dose…”
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Targeting ADAM-mediated ligand cleavage to inhibit HER3 and EGFR pathways in non-small cell lung cancer by Zhou, Bin-Bing S., Peyton, Michael, He, Biao, Liu, Changnian, Girard, Luc, Caudler, Eian, Lo, Yvonne, Baribaud, Frederic, Mikami, Iwao, Reguart, Noemi, Yang, Gengjie, Li, Yanlong, Yao, Wenqing, Vaddi, Kris, Gazdar, Adi F., Friedman, Steven M., Jablons, David M., Newton, Robert C., Fridman, Jordan S., Minna, John D., Scherle, Peggy A.

“…We describe here the existence of a heregulin-HER3 autocrine loop, and the contribution of heregulin-dependent, HER2-mediated HER3 activation to gefitinib…”
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Preclinical Evaluation of Local JAK1 and JAK2 Inhibition in Cutaneous Inflammation by Fridman, Jordan S., Scherle, Peggy A., Collins, Robert, Burn, Timothy, Neilan, Claire L., Hertel, Denise, Contel, Nancy, Haley, Patrick, Thomas, Beth, Shi, Jack, Collier, Paul, Rodgers, James D., Shepard, Stacey, Metcalf, Brian, Hollis, Gregory, Newton, Robert C., Yeleswaram, Swamy, Friedman, Steven M., Vaddi, Kris

“…JAKs are required for signaling initiated by several cytokines (e.g., IL-4, IL-12, IL-23, thymic stromal lymphopoietin (TSLP), and IFNγ) implicated in the…”
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Selective Inhibition of ADAM Metalloproteases as a Novel Approach for Modulating ErbB Pathways in Cancer by Fridman, Jordan S, Caulder, Eian, Hansbury, Michael, Liu, Xiangdong, Yang, Genjie, Wang, Qian, Lo, Yvonne, Zhou, Bin-Bing, Pan, Maxwell, Thomas, Sufi M, Grandis, Jennifer R, Zhuo, Jincong, Yao, Wenqing, Newton, Robert C, Friedman, Steven M, Scherle, Peggy A, Vaddi, Kris

“…Purpose: ErbB receptor signaling pathways are important regulators of cell fate, and their dysregulation, through (epi)genetic alterations, plays an etiologic…”
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INCB16562, a JAK1/2 Selective Inhibitor, Is Efficacious against Multiple Myeloma Cells and Reverses the Protective Effects of Cytokine and Stromal Cell Support by Li, Jun, Favata, Margaret, Kelley, Jennifer A., Caulder, Eian, Thomas, Beth, Wen, Xiaoming, Sparks, Richard B., Arvanitis, Ari, Rogers, James D., Combs, Andrew P., Vaddi, Kris, Solomon, Kimberly A., Scherle, Peggy A., Newton, Robert, Fridman, Jordan S.

“…Cytokines in the bone marrow of multiple myeloma patients activate Janus kinase (JAK)/signal transducer and activator of transcription (STAT) signaling…”
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First-in-Human Phase I Study of the Oral Inhibitor of Indoleamine 2,3-Dioxygenase-1 Epacadostat (INCB024360) in Patients with Advanced Solid Malignancies by Beatty, Gregory L, O'Dwyer, Peter J, Clark, Jason, Shi, Jack G, Bowman, Kevin J, Scherle, Peggy A, Newton, Robert C, Schaub, Richard, Maleski, Janet, Leopold, Lance, Gajewski, Thomas F

“…Indoleamine 2,3-dioxygenase-1 (IDO1) catalyzes the degradation of tryptophan to N-formyl-kynurenine. Overexpressed in many solid malignancies, IDO1 can promote…”
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Mechanism of tumor rejection with doublets of CTLA-4, PD-1/PD-L1, or IDO blockade involves restored IL-2 production and proliferation of CD8(+) T cells directly within the tumor microenvironment by Spranger, Stefani, Koblish, Holly K, Horton, Brendan, Scherle, Peggy A, Newton, Robert, Gajewski, Thomas F

“…Blockade of immune inhibitory pathways is emerging as an important therapeutic modality for the treatment of cancer. Single agent treatments have partial…”
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Discovery of Disubstituted Cyclohexanes as a New Class of CC Chemokine Receptor 2 Antagonists by Cherney, Robert J, Mo, Ruowei, Meyer, Dayton T, Nelson, David J, Lo, Yvonne C, Yang, Gengjie, Scherle, Peggy A, Mandlekar, Sandhya, Wasserman, Zelda R, Jezak, Heather, Solomon, Kimberly A, Tebben, Andrew J, Carter, Percy H, Decicco, Carl P

“…We describe the design, synthesis, and evaluation of novel disubstituted cyclohexanes as potent CCR2 antagonists. Exploratory SAR studies led to the…”
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Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2 by Shin, Niu, Baribaud, Frédéric, Wang, Kathy, Yang, Genjie, Wynn, Rich, Covington, Maryanne B., Feldman, Patricia, Gallagher, Karen B., Leffet, Lynn M., Lo, Yvonne Y., Wang, Anlai, Xue, Chu-Biao, Newton, Robert C., Scherle, Peggy A.

“…The chemokine receptor 2 (CCR2) directs migration of monocytes and has been proposed to be a drug target for chronic inflammatory diseases. INCB3344 was first…”
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Rapid Inhibition of Interleukin-6 Signaling and Stat3 Activation Mediated by Mitogen-Activated Protein Kinases by Sengupta, Tapas K., Talbot, Erika S., Scherle, Peggy A., Ivashkiv, Lionel B.

“…Gene activation and cellular differentiation induced by interleukin-6 (IL-6) and transcription factor Stat3 are suppressed by several factors, including…”
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Phase 2 study of the JAK kinase inhibitor ruxolitinib in patients with refractory leukemias, including postmyeloproliferative neoplasm acute myeloid leukemia by Eghtedar, Alireza, Verstovsek, Srdan, Estrov, Zeev, Burger, Jan, Cortes, Jorge, Bivins, Carol, Faderl, Stefan, Ferrajoli, Alessandra, Borthakur, Gautam, George, Solly, Scherle, Peggy A., Newton, Robert C., Kantarjian, Hagop M., Ravandi, Farhad

“…We conducted a phase 2 study of ruxolitinib in patients with relapsed/refractory leukemias. Patients with acceptable performance status (0-2), adequate organ…”
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Targeting the mechanisms of tumoral immune tolerance with small-molecule inhibitors by Muller, Alexander J, Scherle, Peggy A

“…Cancer immunotherapy has been predominantly focused on biologically based intervention strategies. However, recent advances in the understanding of tumour-host…”
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Treatment-Induced Tumor Cell Apoptosis and Secondary Necrosis Drive Tumor Progression in the Residual Tumor Microenvironment through MerTK and IDO1 by Werfel, Thomas A, Elion, David L, Rahman, Bushra, Hicks, Donna J, Sanchez, Violeta, Gonzales-Ericsson, Paula I, Nixon, Mellissa J, James, Jamaal L, Balko, Justin M, Scherle, Peggy A, Koblish, Holly K, Cook, Rebecca S

“…Efferocytosis is the process by which apoptotic cells are cleared from tissue by phagocytic cells. The removal of apoptotic cells prevents them from undergoing…”
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