Search Results - "Kirchhoff, Paul"

Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer by Xiang, Weiguo, Zhao, Lijie, Han, Xin, Qin, Chong, Miao, Bukeyan, McEachern, Donna, Wang, Yu, Metwally, Hoda, Kirchhoff, Paul D, Wang, Lu, Matvekas, Aleksas, He, Miao, Wen, Bo, Sun, Duxin, Wang, Shaomeng

“…We report herein the discovery of exceptionally potent and orally bioavailable PROTAC AR degraders with ARD-2585 being the most promising compound. ARD-2585…”
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Discovery of ARD-2051 as a Potent and Orally Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer by Han, Xin, Zhao, Lijie, Xiang, Weiguo, Miao, Bukeyan, Qin, Chong, Wang, Mi, Xu, Tianfeng, McEachern, Donna, Lu, Jianfeng, Wang, Yu, Metwally, Hoda, Yang, Chao-Yie, Kirchhoff, Paul D., Wang, Lu, Matvekas, Aleksas, Takyi-Williams, John, Wen, Bo, Sun, Duxin, Ator, Mark, Mckean, Robert, Wang, Shaomeng

“…We report the discovery of ARD-2051 as a potent and orally efficacious androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50…”
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Inhibitors of Mycobacterium tuberculosis DosRST signaling and persistence by Zheng, Huiqing, Colvin, Christopher J, Johnson, Benjamin K, Kirchhoff, Paul D, Wilson, Michael, Jorgensen-Muga, Katriana, Larsen, Scott D, Abramovitch, Robert B

“…A high-throughput screen identifies inhibitors of the M. tuberculosis dormancy regulation system, DosRST, including compounds that inhibit autophosphorylation…”
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Discovery of M‑1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression by Zhang, Meng, Aguilar, Angelo, Xu, Shilin, Huang, Liyue, Chinnaswamy, Krishnapriya, Sleger, Taryn, Wang, Bo, Gross, Stefan, Nicolay, Brandon N, Ronseaux, Sebastien, Harvey, Kaitlin, Wang, Yu, McEachern, Donna, Kirchhoff, Paul D, Liu, Zhaomin, Stuckey, Jeanne, Tron, Adriana E, Liu, Tao, Wang, Shaomeng

“…Targeting the menin-MLL protein–protein interaction is being pursued as a new therapeutic strategy for the treatment of acute leukemia carrying…”
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Discovery of a Potent and Selective STAT5 PROTAC Degrader with Strong Antitumor Activity In Vivo in Acute Myeloid Leukemia by Kaneshige, Atsunori, Bai, Longchuan, Wang, Mi, McEachern, Donna, Meagher, Jennifer L., Xu, Renqi, Kirchhoff, Paul D., Wen, Bo, Sun, Duxin, Stuckey, Jeanne A., Wang, Shaomeng

“…STAT5 is an attractive therapeutic target for human cancers. We report herein the discovery of a potent and selective STAT5 degrader with strong antitumor…”
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A selective small-molecule STAT5 PROTAC degrader capable of achieving tumor regression in vivo by Kaneshige, Atsunori, Bai, Longchuan, Wang, Mi, McEachern, Donna, Meagher, Jennifer L., Xu, Renqi, Wang, Yu, Jiang, Wei, Metwally, Hoda, Kirchhoff, Paul D., Zhao, Lijie, Jiang, Hui, Wang, Meilin, Wen, Bo, Sun, Duxin, Stuckey, Jeanne A., Wang, Shaomeng

“…Signal transducer and activator of transcription 5 (STAT5) is an attractive therapeutic target, but successful targeting of STAT5 has proved to be difficult…”
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Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer by Xiang, Weiguo, Zhao, Lijie, Han, Xin, Xu, Tianfeng, Kregel, Steven, Wang, Mi, Miao, Bukeyan, Qin, Chong, Wang, Mingliang, McEachern, Donna, Lu, Jianfeng, Bai, Longchuan, Yang, Chao-Yie, Kirchhoff, Paul D., Takyi-Williams, John, Wang, Lu, Wen, Bo, Sun, Duxin, Ator, Mark, Mckean, Robert, Chinnaiyan, Arul M., Wang, Shaomeng

“…We report herein the discovery and extensive characterization of ARD-1676, a highly potent and orally efficacious PROTAC degrader of the androgen receptor…”
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Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents by Bell, Jessica L., Haak, Andrew J., Wade, Susan M., Kirchhoff, Paul D., Neubig, Richard R., Larsen, Scott D.

“…CCG-1423 (1) is a novel inhibitor of Rho/MKL1/SRF-mediated gene transcription that inhibits invasion of PC-3 prostate cancer cells in a Matrigel model of…”
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Discovery of AK-1690: A Potent and Highly Selective STAT6 PROTAC Degrader by Kaneshige, Atsunori, Yang, Yiqing, Bai, Longchuan, Wang, Mi, Xu, Renqi, Mallik, Leena, Chinnaswamy, Krishnapriya, Metwally, Hoda, Wang, Yu, McEachern, Donna, Tošović, Jelena, Yang, Chao-Yie, Kirchhoff, Paul D, Meagher, Jennifer L, Stuckey, Jeanne A, Wang, Shaomeng

“…STAT6 is an attractive therapeutic target for human cancers and other human diseases. Starting from a STAT6 ligand with = 3.5 μM binding affinity, we obtained…”
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Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors by Waldschmidt, Helen V, Homan, Kristoff T, Cruz-Rodríguez, Osvaldo, Cato, Marilyn C, Waninger-Saroni, Jessica, Larimore, Kelly M, Cannavo, Alessandro, Song, Jianliang, Cheung, Joseph Y, Kirchhoff, Paul D, Koch, Walter J, Tesmer, John J. G, Larsen, Scott D

“…G protein-coupled receptors (GPCRs) are central to many physiological processes. Regulation of this superfamily of receptors is controlled by GPCR kinases…”
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Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors by Waldschmidt, Helen V., Bouley, Renee, Kirchhoff, Paul D., Lee, Pil, Tesmer, John J.G., Larsen, Scott D.

“…[Display omitted] G protein-coupled receptor (GPCR) kinases (GRKs) regulate the desensitization and internalization of GPCRs. Two of these, GRK2 and GRK5, are…”
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Rifamycins – Obstacles and opportunities by Aristoff, Paul A, Garcia, George A, Kirchhoff, Paul D, Hollis Showalter, H.D

“…Summary With nearly one-third of the global population infected by Mycobacterium tuberculosis , TB remains a major cause of death (1.7 million in 2006). TB is…”
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X‑ray Crystal Structures of the Escherichia coli RNA Polymerase in Complex with Benzoxazinorifamycins by Molodtsov, Vadim, Nawarathne, Irosha N, Scharf, Nathan T, Kirchhoff, Paul D, Showalter, H. D. Hollis, Garcia, George A, Murakami, Katsuhiko S

“…Rifampin, a semisynthetic rifamycin, is the cornerstone of current tuberculosis treatment. Among many semisynthetic rifamycins, benzoxazinorifamycins have…”
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Optimization of dipeptidic inhibitors of cathepsin L for improved Toxoplasma gondii selectivity and CNS permeability by Zwicker, Jeffery D., Diaz, Nicolas A., Guerra, Alfredo J., Kirchhoff, Paul D., Wen, Bo, Sun, Duxin, Carruthers, Vern B., Larsen, Scott D.

“…[Display omitted] The neurotropic protozoan Toxoplasma gondii is the second leading cause of death due to foodborne illness in the US, and has been designated…”
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LigScore: a novel scoring function for predicting binding affinities by Krammer, André, Kirchhoff, Paul D., Jiang, X., Venkatachalam, C.M., Waldman, Marvin

“…We present two new empirical scoring functions, LigScore1 and LigScore2, that attempt to accurately predict the binding affinity between ligand molecules and…”
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Inhibitors of TonB function identified by a high-throughput screen for inhibitors of iron acquisition in uropathogenic Escherichia coli CFT073 by Yep, Alejandra, McQuade, Thomas, Kirchhoff, Paul, Larsen, Martha, Mobley, Harry L T

“…The urinary tract is one of the most common sites of infection in humans, and uropathogenic Escherichia coli (UPEC) is the main causative agent of urinary…”
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Identification of Thieno[3,2-b]Pyrrole Derivatives as Novel Small Molecule Inhibitors of Neurotropic Alphaviruses by Peng, Weiping, Peltier, Daniel C., Larsen, Martha J., Kirchhoff, Paul D., Larsen, Scott D., Neubig, Richard R., Miller, David J.

“…Neurotropic alphaviruses such as western, eastern, and Venezuelan equine encephalitis viruses cause serious and potentially fatal central nervous system…”
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Protein cross-linking as a novel mechanism of action of a ubiquitin-activating enzyme inhibitor with anti-tumor activity by Kapuria, Vaibhav, Peterson, Luke F., Showalter, H.D. Hollis, Kirchhoff, Paul D., Talpaz, Moshe, Donato, Nicholas J.

“…Ubiquitin-activating enzyme 1 (UBE1) is a critical regulator of the ubiquitination cycle and its targeted inhibition may be an appropriate therapeutic strategy…”
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Property-based design of a glucosylceramide synthase inhibitor that reduces glucosylceramide in the brain by Larsen, Scott D., Wilson, Michael W., Abe, Akira, Shu, Liming, George, Christopher H., Kirchhoff, Paul, Showalter, H. D. Hollis, Xiang, Jianming, Keep, Richard F., Shayman, James A.

“…Synthesis inhibition is the basis for the treatment of type 1 Gaucher disease by the glucosylceramide synthase (GCS) inhibitor eliglustat tartrate. However,…”
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Novel indole-2-carboxamide compounds are potent broad-spectrum antivirals active against western equine encephalitis virus in vivo by Delekta, Phillip C, Dobry, Craig J, Sindac, Janice A, Barraza, Scott J, Blakely, Pennelope K, Xiang, Jianming, Kirchhoff, Paul D, Keep, Richard F, Irani, David N, Larsen, Scott D, Miller, David J

“…Neurotropic alphaviruses, including western, eastern, and Venezuelan equine encephalitis viruses, cause serious and potentially fatal central nervous system…”
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