Search Results - "Kohlmann, Anna"

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase by Huang, Wei-Sheng, Liu, Shuangying, Zou, Dong, Thomas, Mathew, Wang, Yihan, Zhou, Tianjun, Romero, Jan, Kohlmann, Anna, Li, Feng, Qi, Jiwei, Cai, Lisi, Dwight, Timothy A, Xu, Yongjin, Xu, Rongsong, Dodd, Rory, Toms, Angela, Parillon, Lois, Lu, Xiaohui, Anjum, Rana, Zhang, Sen, Wang, Frank, Keats, Jeffrey, Wardwell, Scott D, Ning, Yaoyu, Xu, Qihong, Moran, Lauren E, Mohemmad, Qurish K, Jang, Hyun Gyung, Clackson, Tim, Narasimhan, Narayana I, Rivera, Victor M, Zhu, Xiaotian, Dalgarno, David, Shakespeare, William C

“…In the treatment of echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase positive (ALK+) non-small-cell lung cancer (NSCLC),…”
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Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients by Garner, Andrew P, Gozgit, Joseph M, Anjum, Rana, Vodala, Sadanand, Schrock, Alexa, Zhou, Tianjun, Serrano, Cesar, Eilers, Grant, Zhu, Meijun, Ketzer, Julia, Wardwell, Scott, Ning, Yaoyu, Song, Youngchul, Kohlmann, Anna, Wang, Frank, Clackson, Tim, Heinrich, Michael C, Fletcher, Jonathan A, Bauer, Sebastian, Rivera, Victor M

“…KIT is the major oncogenic driver of gastrointestinal stromal tumors (GIST). Imatinib, sunitinib, and regorafenib are approved therapies; however, efficacy is…”
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Application of MM-GB/SA and WaterMap to SRC Kinase Inhibitor Potency Prediction by Kohlmann, Anna, Zhu, Xiaotian, Dalgarno, David

“…WaterMap and MM-GB/SA scoring methods were applied to an extensive congeneric series of small-molecule SRC inhibitors with high-quality enzyme data and well…”
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Abstract 2644: AP32788, a potent, selective inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, in preclinical models by Gonzalvez, Francois, Zhu, Xiaotian, Huang, Wei-Sheng, Baker, Theresa E., Ning, Yaoyu, Wardwell, Scott D., Nadworny, Sara, Zhang, Sen, Das, Biplab, Gong, Yongjin, Greenfield, Matthew T., Jang, Hyun G., Kohlmann, Anna, Li, Feng, Taslimi, Paul M., Tugnait, Meera, Xu, Yongjin, Ye, Emily Y., Youngsaye, Willmen W., Zech, Stephan G., Zhang, Yun, Zhou, Tianjun, Narasimhan, Narayana I., Dalgarno, David C., Shakespeare, William C., Rivera, Victor M.

“…Abstract In non-small cell lung cancer (NSCLC), multiple classes of activating mutations have been identified in EGFR and HER2 that vary widely in their…”
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Novel Autotaxin Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis: A Clinical Candidate Discovered Using DNA-Encoded Chemistry by Cuozzo, John W, Clark, Matthew A, Keefe, Anthony D, Kohlmann, Anna, Mulvihill, Mark, Ni, Haihong, Renzetti, Louis M, Resnicow, Daniel I, Ruebsam, Frank, Sigel, Eric A, Thomson, Heather A, Wang, Ce, Xie, Zhifeng, Zhang, Ying

“…The activity of the secreted phosphodiesterase autotaxin produces the inflammatory signaling molecule LPA and has been associated with a number of human…”
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Computational and Functional Analyses of HER2 Mutations Reveal Allosteric Activation Mechanisms and Altered Pharmacologic Effects by Ishiyama, Noboru, O'Connor, Matthew, Salomatov, Andrei, Romashko, Darlene, Thakur, Shalabh, Mentes, Ahmet, Hopkins, Julia F, Frampton, Garrett M, Albacker, Lee A, Kohlmann, Anna, Roberts, Christopher, Buck, Elizabeth

“…Amplification of HER2 can drive the proliferation of cancer cells, and several inhibitors of HER2 have been successfully developed. Recent advances in…”
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Exploration of Cryptic Pockets Using Enhanced Sampling Along Normal Modes: A Case Study of KRAS G12D by Vithani, Neha, Zhang, She, Thompson, Jeffrey P., Patel, Lara A., Demidov, Alex, Xia, Junchao, Balaeff, Alexander, Mentes, Ahmet, Arnautova, Yelena A., Kohlmann, Anna, Lawson, J. David, Nicholls, Anthony, Skillman, A. Geoffrey, LeBard, David N.

“…Identification of cryptic pockets has the potential to open new therapeutic opportunities by discovering ligand binding sites that remain hidden in static apo…”
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Bispecific Estrogen Receptor α Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening by Disch, Jeremy S, Duffy, Jennifer M, Lee, Esther C. Y, Gikunju, Diana, Chan, Betty, Levin, Benjamin, Monteiro, Michael I, Talcott, Sarah A, Lau, Anthony C, Zhou, Fei, Kozhushnyan, Anton, Westlund, Neil E, Mullins, Patrick B, Yu, Yan, von Rechenberg, Moritz, Zhang, Junyi, Arnautova, Yelena A, Liu, Yanbin, Zhang, Ying, McRiner, Andrew J, Keefe, Anthony D, Kohlmann, Anna, Clark, Matthew A, Cuozzo, John W, Huguet, Christelle, Arora, Shilpi

“…Bispecific degraders (PROTACs) of ERα are expected to be advantageous over current inhibitors of ERα signaling (aromatase inhibitors/SERMs/SERDs) used to treat…”
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Discovery of Novel, Potent Inhibitors of Hydroxy Acid Oxidase 1 (HAO1) Using DNA-Encoded Chemical Library Screening by Lee, Esther C. Y, McRiner, Andrew J, Georgiadis, Katy E, Liu, Julie, Wang, Zooey, Ferguson, Andrew D, Levin, Benjamin, von Rechenberg, Moritz, Hupp, Christopher D, Monteiro, Michael I, Keefe, Anthony D, Olszewski, Allison, Eyermann, Charles J, Centrella, Paolo, Liu, Yanbin, Arora, Shilpi, Cuozzo, John W, Zhang, Ying, Clark, Matthew A, Huguet, Christelle, Kohlmann, Anna

“…Inhibition of hydroxy acid oxidase 1 (HAO1) is a strategy to mitigate the accumulation of toxic oxalate that results from reduced activity of…”
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Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non–small cell lung cancer by Huang, Wei-Sheng, Li, Feng, Gong, Yongjin, Zhang, Yun, Youngsaye, Willmen, Xu, Yongjin, Zhu, Xiaotian, Greenfield, Matthew T., Kohlmann, Anna, Taslimi, Paul M., Toms, Angela, Zech, Stephan G., Zhou, Tianjun, Das, Biplab, Jang, Hyun G., Tugnait, Meera, Ye, Yihua E., Gonzalvez, Francois, Baker, Theresa E., Nadworny, Sara, Ning, Yaoyu, Wardwell, Scott D., Zhang, Sen, Gould, Alexandra E., Hu, Yongbo, Lane, Weston, Skene, Robert J., Zou, Hua, Clackson, Tim, Narasimhan, Narayana I., Rivera, Victor M., Dalgarno, David C., Shakespeare, William C.

“…[Display omitted] In the treatment of non–small cell lung cancer (NSCLC), patients harboring exon 20 insertion mutations in the epidermal growth factor…”
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Abstract A06: Biophysical and biochemical characterization of KRAS G12C inhibition through the SMARTTM platform by Zhou, Minyun, Yuzhakov, Alexander, Benod, Cindy C, Xue, Linlong, Silver, Alec D, Iyer, Ganesh, Townson, Sharon A., Jin, Meizhong, Perl, Nicholas R., Kohlmann, Anna, Mann, Alan S., Akcay, Gizem, May, Earl W.

“…Abstract RAS proteins are small GTPases involved in cell proliferation, survival, and differentiation, and are mutationally activated in about a third of all…”
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Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery by Zech, Stephan G, Kohlmann, Anna, Zhou, Tianjun, Li, Feng, Squillace, Rachel M, Parillon, Lois E, Greenfield, Matthew T, Miller, David P, Qi, Jiwei, Thomas, R. Mathew, Wang, Yihan, Xu, Yongjin, Miret, Juan J, Shakespeare, William C, Zhu, Xiaotian, Dalgarno, David C

“…Choline kinase α (ChoKα) is an enzyme involved in the synthesis of phospholipids and thereby plays key roles in regulation of cell proliferation, oncogenic…”
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Abstract B37: Development of inhibitors of the activated form of KRAS G12C by Stewart, Michelle L., Perl, Nicholas R., Lee, Seung-Joo, Xue, Linlong, Zhou, Minyun, Simon, Jonah, Luly, Kathryn M., Grigoriu, Siminia, Yuzhakov, Alex, Silver, Alec, Lowe, Jason T., Benod, Cindy C., Mann, Alan S., Verdine, Gregory L., Rigby, Alan C., Mulvihill, Mark J., May, Earl W., Kohlmann, Anna, Townson, Sharon A., Pollock, Roy M., Jin, Meizhong

“…Abstract Activating mutations in RAS proteins occur in ~1/3 of human cancers. These mutations impair the ability of the protein to hydrolyze GTP to GDP. As a…”
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Abstract A98: An in vitro mutagenesis screen identifies L1951R and G2032R as drug-resistant mutants of CD74-ROS1 by Anjum, Rana, Vodala, Sadanand, Kohlmann, Anna, Rivera, Victor M., Garner, Andrew P.

“…Abstract NSCLC can be divided into a series of genomically-defined subsets, each generally containing a distinct molecular driver. The development of drugs…”
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Abstract 5346: Discovery of new targeted protein degraders using DNA-encoded chemistry by Keefe, Anthony D., Disch, Jeremy S., Duffy, Jennifer, Lee, Esther C., Gikunju, Diana, Chan, Betty, Levin, Benjamin D., Monteiro, Michael I., Talcott, Sarah A., Lau, Anthony, Zhou, Fei, Kozhushnyan, Anton, Westlund, Neil E., Mullins, Patrick B., Yu, Yan, von Rechenberg, Moritz, Zhang, Junyi, Arnautova, Yelena, Liu, Yanbin, Zhang, Ying, McRiner, Andrew J., Kohlmann, Anna, Clark, Matthew A., Cuozzo, John W., Huguet, Christelle, Arora, Shilpi

“…Abstract Bispecific degraders (PROTACs) of ERα are expected to be advantageous over current inhibitors of ERα signaling (aromatase inhibitors/SERMs/SERDs) used…”
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Abstract 2827: Discovery of AP26113, a potent, orally active inhibitor of anaplastic lymphoma kinase and clinically relevant mutants by Huang, Wei-Sheng, Li, Feng, Cai, Lisi, Xu, Yongjin, Zhang, Sen, Wardwell, Scott D., Ning, Yaoyu, Kohlmann, Anna, Zhou, Tianjun, Ye, Emily Y., Zhu, Xiaotian, Narasimhan, Narayana I., Clackson, Tim, Rivera, Victor M., Dalgarno, David, Shakespeare, William C.

“…Abstract Phosphorus, despite its abundance in the human body, is rarely found in drug molecules, with clinical utility limited to a few phosphonic or…”
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Fragment Growing and Linking Lead to Novel Nanomolar Lactate Dehydrogenase Inhibitors by Kohlmann, Anna, Zech, Stephan G, Li, Feng, Zhou, Tianjun, Squillace, Rachel M, Commodore, Lois, Greenfield, Matthew T, Lu, Xiaohui, Miller, David P, Huang, Wei-Sheng, Qi, Jiwei, Thomas, R. Mathew, Wang, Yihan, Zhang, Sen, Dodd, Rory, Liu, Shuangying, Xu, Rongsong, Xu, Yongjin, Miret, Juan J, Rivera, Victor, Clackson, Tim, Shakespeare, William C, Zhu, Xiaotian, Dalgarno, David C

“…Lactate dehydrogenase A (LDH-A) catalyzes the interconversion of lactate and pyruvate in the glycolysis pathway. Cancer cells rely heavily on glycolysis…”
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Abstract 3236: Small molecule inhibitors of choline kinase lead to reduced phosphocholine levels and induction of apoptosis in cancer cells by Squillace, Rachel M., Zech, Stephan, Li, Feng, Kohlmann, Anna, Miller, David, Greenfield, Matthew, Ning, Yaoyu, Commodore, Lois, Miret, Juan, Wang, Frank, Zhou, Tianjun, Wang, Yihan, Thomas, Matthew, Qi, Jiwei, Xu, Yongjin, Rivera, Victor, Clackson, Tim, Zhu, Xiaotian, Shakespeare, William, Delgarno, David

“…Abstract Choline Kinase (ChoK) catalyzes the synthesis of phosphocholine (pCho) as the first step in the Kennedy pathway towards synthesis of the major…”
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