Search Results - "Metcalf, Chester A."

AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance by O'Hare, Thomas, Shakespeare, William C., Zhu, Xiaotian, Eide, Christopher A., Rivera, Victor M., Wang, Frank, Adrian, Lauren T., Zhou, Tianjun, Huang, Wei-Sheng, Xu, Qihong, Metcalf, Chester A., Tyner, Jeffrey W., Loriaux, Marc M., Corbin, Amie S., Wardwell, Scott, Ning, Yaoyu, Keats, Jeffrey A., Wang, Yihan, Sundaramoorthi, Raji, Thomas, Mathew, Zhou, Dong, Snodgrass, Joseph, Commodore, Lois, Sawyer, Tomi K., Dalgarno, David C., Deininger, Michael W.N., Druker, Brian J., Clackson, Tim

“…Inhibition of BCR-ABL by imatinib induces durable responses in many patients with chronic myeloid leukemia (CML), but resistance attributable to kinase domain…”
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Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant by Huang, Wei-Sheng, Metcalf, Chester A, Sundaramoorthi, Raji, Wang, Yihan, Zou, Dong, Thomas, R. Mathew, Zhu, Xiaotian, Cai, Lisi, Wen, David, Liu, Shuangying, Romero, Jan, Qi, Jiwei, Chen, Ingrid, Banda, Geetha, Lentini, Scott P, Das, Sasmita, Xu, Qihong, Keats, Jeff, Wang, Frank, Wardwell, Scott, Ning, Yaoyu, Snodgrass, Joseph T, Broudy, Marc I, Russian, Karin, Zhou, Tianjun, Commodore, Lois, Narasimhan, Narayana I, Mohemmad, Qurish K, Iuliucci, John, Rivera, Victor M, Dalgarno, David C, Sawyer, Tomi K, Clackson, Tim, Shakespeare, William C

“…In the treatment of chronic myeloid leukemia (CML) with BCR-ABL kinase inhibitors, the T315I gatekeeper mutant has emerged as resistant to all currently…”
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Identification of Src-specific phosphorylation site on focal adhesion kinase: Dissection of the role of Src SH2 and catalytic functions and their consequences for tumor cell behavior by BRUNTON, Valerie G, AVIZIENYTE, Egle, FINCHAM, Valerie J, SERRELS, Bryan, METCALF, Chester A, SAWYER, Tomi K, FRAME, Margaret C

“…Src tyrosine kinase expression and activity are elevated during colon cancer progression. How this contributes to the malignant phenotype is not fully…”
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Discovery of a Novel Cabazitaxel Nanoparticle–Drug Conjugate (CRLX522) with Improved Pharmacokinetic Properties and Anticancer Effects Using a β‑Cyclodextrin–PEG Copolymer Based Delivery Platform by Metcalf, Chester A, Svenson, Sonke, Hwang, Jungyeon, Tripathi, Snehlata, Gangal, Geeti, Kabir, Sujan, Lazarus, Douglas, Cole, Roderic, Sweryda-Krawiec, Beata, Shum, Pochi, Brown, Donna, Case, Roy I, van der Poll, Derek, Rohde, Ellen, Harlfinger, Stephanie, Teng, Chi-Hse, Eliasof, Scott

“…Novel nanoparticle–drug conjugates (NDCs) containing diverse, clinically relevant anticancer drug payloads (docetaxel, cabazitaxel, and gemcitabine) were…”
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Activity of Dual SRC-ABL Inhibitors Highlights the Role of BCR/ABL Kinase Dynamics in Drug Resistance by Azam, Mohammad, Nardi, Valentina, Shakespeare, William C., Metcalf, Chester A., Bohacek, Regine S., Wang, Yihan, Sundaramoorthi, Raji, Sliz, Piotr, Veach, Darren R., Bornmann, William G., Clarkson, Bayard, Dalgarno, David C., Sawyer, Tomi K., Daley, George Q.

“…Mutation in the ABL kinase domain is the principal mechanism of imatinib resistance in patients with chronic myelogenous leukemia. Many mutations favor active…”
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Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML by O'Hare, Thomas, Pollock, Roy, Stoffregen, Eric P., Keats, Jeffrey A., Abdullah, Omar M., Moseson, Erika M., Rivera, Victor M., Tang, Hao, Metcalf, Chester A., Bohacek, Regine S., Wang, Yihan, Sundaramoorthi, Raji, Shakespeare, William C., Dalgarno, David, Clackson, Tim, Sawyer, Tomi K., Deininger, Michael W., Druker, Brian J.

“…The deregulated, oncogenic tyrosine kinase Bcr-Abl causes chronic myeloid leukemia (CML). Imatinib mesylate (Gleevec, STI571), a Bcr-Abl kinase inhibitor,…”
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Discovery of Azaindole Ureas as a Novel Class of Bacterial Gyrase B Inhibitors by Zhang, Jing, Yang, Qingyi, Cross, Jason B, Romero, Jan Antoinette C, Poutsiaka, Katherine M, Epie, Felix, Bevan, Douglas, Wang, Bin, Zhang, Yanzhi, Chavan, Ajit, Zhang, Xin, Moy, Terence, Daniel, Anu, Nguyen, Kien, Chamberlain, Brian, Carter, Nicole, Shotwell, Joseph, Silverman, Jared, Metcalf, Chester A, Ryan, Dominic, Lippa, Blaise, Dolle, Roland E

“…The emergence and spread of multidrug resistant bacteria are widely believed to endanger human health. New drug targets and lead compounds exempt from…”
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Antiangiogenic and antitumor effects of src inhibition in ovarian carcinoma by HAN, Liz Y, LANDEN, Charles N, SHAKESPEARE, William C, YIHAN WANG, SUNDARAMOORTH, Raji, METCALF, Chester A, DALGARNO, David C, SAWYER, Tomi K, GALLICK, Gary E, SOOD, Anil K, TREVINO, Jose G, HALDER, Jyotsnabaran, LIN, Yvonne G, KAMAT, Aparna A, KIM, Tae-Jin, MERRITT, William M, COLEMAN, Robert L, GERSHENSON, David M

“…Src, a nonreceptor tyrosine kinase, is a key mediator for multiple signaling pathways that regulate critical cellular functions and is often aberrantly…”
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Structure-based discovery of LpxC inhibitors by Zhang, Jing, Chan, Audrey, Lippa, Blaise, Cross, Jason B., Liu, Christopher, Yin, Ning, Romero, Jan Antoinette C., Lawrence, Jonathan, Heney, Ryan, Herradura, Prudencio, Goss, Jennifer, Clark, Cynthia, Abel, Cassandra, Zhang, Yanzhi, Poutsiaka, Katherine M., Epie, Felix, Conrad, Mary, Mahamoon, Azard, Nguyen, Kien, Chavan, Ajit, Clark, Edward, Li, Tong-chuan, Cheng, Robert K., Wood, Michael, Andersen, Ole A., Brooks, Mark, Kwong, Jason, Barker, John, Parr, Ian Barrie, Gu, Yugui, Ryan, M. Dominic, Coleman, Scott, Metcalf, Chester A.

“…[Display omitted] The emergence and spread of multidrug-resistant (MDR) Gram negative bacteria presents a serious threat for public health. Novel…”
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Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design by Cross, Jason B, Zhang, Jing, Yang, Qingyi, Mesleh, Michael F, Romero, Jan Antoinette C, Wang, Bin, Bevan, Doug, Poutsiaka, Katherine M, Epie, Felix, Moy, Terence, Daniel, Anu, Shotwell, Joseph, Chamberlain, Brian, Carter, Nicole, Andersen, Ole, Barker, John, Ryan, M. Dominic, Metcalf, Chester A, Silverman, Jared, Nguyen, Kien, Lippa, Blaise, Dolle, Roland E

“…The ATPase subunit of DNA gyrase B is an attractive antibacterial target due to high conservation across bacteria and the essential role it plays in DNA…”
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AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes by Summy, Justin M, Trevino, Jose G, Lesslie, Donald P, Baker, Cheryl H, Shakespeare, William C, Wang, Yihan, Sundaramoorthi, Raji, Metcalf, 3rd, Chester A, Keats, Jeffrey A, Sawyer, Tomi K, Gallick, Gary E

“…c-Src is frequently activated in human malignancies, including colon, breast, and pancreatic carcinomas. Several recent studies have shown that activation of…”
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Src Inhibitors in Metastatic Bone Disease by Boyce, Brendan F, Xing, Lianping, Yao, Zhenqiang, Yamashita, Teruhito, Shakespeare, William C, Wang, Yihan, Metcalf, 3rd, Chester A, Sundaramoorthi, Raji, Dalgarno, David C, Iuliucci, John D, Sawyer, Tomi K

“…Src tyrosine kinase was the first gene product shown to have an essential function in bone using recombinant DNA technology after its expression was knocked…”
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Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors by Zhang, Jing, Yang, Qingyi, Romero, Jan Antoinette C, Cross, Jason, Wang, Bin, Poutsiaka, Katherine M, Epie, Felix, Bevan, Douglas, Wu, Yuchuan, Moy, Terence, Daniel, Anu, Chamberlain, Brian, Carter, Nicole, Shotwell, Joseph, Arya, Anu, Kumar, Vipul, Silverman, Jared, Nguyen, Kien, Metcalf, Chester A, Ryan, Dominic, Lippa, Blaise, Dolle, Roland E

“…Antibacterials with a novel mechanism of action offer a great opportunity to combat widespread antimicrobial resistance. Bacterial DNA Gyrase is a clinically…”
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Editor's Note: Identification of Src-Specific Phosphorylation Site on Focal Adhesion Kinase: Dissection of the Role of Src SH2 and Catalytic Functions and Their Consequences for Tumor Cell Behavior by Brunton, Valerie G., Avizienyte, Egle, Fincham, Valerie J., Serrels, Bryan, Metcalf, Chester A., Sawyer, Tomi K., Frame, Margaret C.

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Future Anti-Catabolic Therapeutic Targets in Bone Disease by BOYCE, BRENDAN F., XING, LIANPING, YAO, ZHENQIANG, SHAKESPEARE, WILLIAM C., WANG, YIHAN, METCALF III, CHESTER A., SUNDARAMOORTHI, RAJI, DALGARNO, DAVID C., IULIUCCI, JOHN D., SAWYER, TOMI K.

“…:  Understanding of the regulation of bone catabolism has advanced significantly over the past two decades with the identification of key enzymes that regulate…”
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Bone-Targeted 2,6,9-Trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases by Wang, Yihan, Metcalf, Chester A., Shakespeare, William C., Sundaramoorthi, Raji, Keenan, Terence P., Bohacek, Regine S., van Schravendijk, Marie Rose, Violette, Shiela M., Narula, Surinder S., Dalgarno, David C., Haraldson, Chad, Keats, Jeffrey, Liou, Shuenn, Mani, Ukti, Pradeepan, Selvi, Ram, Mary, Adams, Susan, Weigele, Manfred, Sawyer, Tomi K.

“…Novel bone-targeted 2,6,9-trisubstituted purine template-based inhibitors of Src tyrosine kinase are described. Drug design studies of known purine compounds…”
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In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit by Corbin, Amie S., Demehri, Shadmehr, Griswold, Ian J., Wang, Yihan, Metcalf, Chester A., Sundaramoorthi, Raji, Shakespeare, William C., Snodgrass, Joseph, Wardwell, Scott, Dalgarno, David, Iuliucci, John, Sawyer, Tomi K., Heinrich, Michael C., Druker, Brian J., Deininger, Michael W.N.

“…Oncogenic mutations of the Kit receptor tyrosine kinase occur in several types of malignancy. Juxtamembrane domain mutations are common in gastrointestinal…”
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Targeting protein kinases for bone disease: discovery and development of Src inhibitors by Metcalf, 3rd, Chester A, van Schravendijk, Marie Rose, Dalgarno, David C, Sawyer, Tomi K

“…The dynamic and highly regulated processes of bone remodeling involve two major cells, osteoclasts and osteoblasts, both of which command a multitude of…”
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Novel protein kinase inhibitors: SMART drug design technology by Sawyer, Tomi K, Bohacek, Regine S, Metcalf, 3rd, Chester A, Shakespeare, William C, Wang, Yihan, Sundaramoorthi, Raji, Keenan, Terence, Narula, Surinder, Weigele, Manfred, Dalgarno, David C

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Structure-based design of novel nonpeptide inhibitors of the Src SH2 domain: Phosphotyrosine mimetics exploiting multifunctional group replacement chemistry by Sundaramoorthi, Raji, Kawahata, Noriyuki, Yang, Michael G., Shakespeare, William C., Metcalf III, Chester A., Wang, Yihan, Merry, Taylor, Eyermann, Charles J., Bohacek, Regine S., Narula, Surinder, Dalgarno, David C., Sawyer, Tomi K.

“…A series of novel nonpeptide inhibitors of the pp60c‐Src (Src) SH2 domain is described that exploit multifunctional group replacement of the phenylphosphate…”
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