Search Results - "Crawford, James J."

Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development by Crawford, James J, Johnson, Adam R, Misner, Dinah L, Belmont, Lisa D, Castanedo, Georgette, Choy, Regina, Coraggio, Melis, Dong, Liming, Eigenbrot, Charles, Erickson, Rebecca, Ghilardi, Nico, Hau, Jonathan, Katewa, Arna, Kohli, Pawan Bir, Lee, Wendy, Lubach, Joseph W, McKenzie, Brent S, Ortwine, Daniel F, Schutt, Leah, Tay, Suzanne, Wei, BinQing, Reif, Karin, Liu, Lichuan, Wong, Harvey, Young, Wendy B

“…Bruton’s tyrosine kinase (Btk) is a nonreceptor cytoplasmic tyrosine kinase involved in B-cell and myeloid cell activation, downstream of B-cell and Fcγ…”
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Chemical space docking enables large-scale structure-based virtual screening to discover ROCK1 kinase inhibitors by Beroza, Paul, Crawford, James J., Ganichkin, Oleg, Gendelev, Leo, Harris, Seth F., Klein, Raphael, Miu, Anh, Steinbacher, Stefan, Klingler, Franca-Maria, Lemmen, Christian

“…With the ever-increasing number of synthesis-on-demand compounds for drug lead discovery, there is a great need for efficient search technologies. We present…”
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Optimized arylomycins are a new class of Gram-negative antibiotics by Smith, Peter A., Koehler, Michael F. T., Girgis, Hany S., Yan, Donghong, Chen, Yongsheng, Chen, Yuan, Crawford, James J., Durk, Matthew R., Higuchi, Robert I., Kang, Jing, Murray, Jeremy, Paraselli, Prasuna, Park, Summer, Phung, Wilson, Quinn, John G., Roberts, Tucker C., Rougé, Lionel, Schwarz, Jacob B., Skippington, Elizabeth, Wai, John, Xu, Min, Yu, Zhiyong, Zhang, Hua, Tan, Man-Wah, Heise, Christopher E.

“…Multidrug-resistant bacteria are spreading at alarming rates, and despite extensive efforts no new class of antibiotic with activity against Gram-negative…”
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Alpha-2 adrenergic receptor agonists: a review of current clinical applications by Giovannitti, Jr, Joseph A, Thoms, Sean M, Crawford, James J

“…The α-2 adrenergic receptor agonists have been used for decades to treat common medical conditions such as hypertension; attention-deficit/hyperactivity…”
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Small Molecule Dysregulation of TEAD Lipidation Induces a Dominant-Negative Inhibition of Hippo Pathway Signaling by Holden, Jeffrey K., Crawford, James J., Noland, Cameron L., Schmidt, Stephen, Zbieg, Jason R., Lacap, Jennifer A., Zang, Richard, Miller, Gregory M., Zhang, Yue, Beroza, Paul, Reja, Rohit, Lee, Wendy, Tom, Jeffrey Y.K., Fong, Rina, Steffek, Micah, Clausen, Saundra, Hagenbeek, Thjis J., Hu, Taishan, Zhou, Zheng, Shen, Hong C., Cunningham, Christian N.

“…The transcriptional enhanced associate domain (TEAD) family of transcription factors serves as the receptors for the downstream effectors of the Hippo pathway,…”
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Learning Medicinal Chemistry Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) Rules from Cross-Company Matched Molecular Pairs Analysis (MMPA) by Kramer, Christian, Ting, Attilla, Zheng, Hao, Hert, Jérôme, Schindler, Torsten, Stahl, Martin, Robb, Graeme, Crawford, James J, Blaney, Jeff, Montague, Shane, Leach, Andrew G, Dossetter, Al G, Griffen, Ed J

“…The first large scale analysis of in vitro absorption, distribution, metabolism, excretion, and toxicity (ADMET) data shared across multiple major pharma has…”
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NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus by Brightbill, Hans D., Suto, Eric, Blaquiere, Nicole, Ramamoorthi, Nandhini, Sujatha-Bhaskar, Swathi, Gogol, Emily B., Castanedo, Georgette M., Jackson, Benjamin T., Kwon, Youngsu C., Haller, Susan, Lesch, Justin, Bents, Karin, Everett, Christine, Kohli, Pawan Bir, Linge, Sandra, Christian, Laura, Barrett, Kathy, Jaochico, Allan, Berezhkovskiy, Leonid M., Fan, Peter W., Modrusan, Zora, Veliz, Kelli, Townsend, Michael J., DeVoss, Jason, Johnson, Adam R., Godemann, Robert, Lee, Wyne P., Austin, Cary D., McKenzie, Brent S., Hackney, Jason A., Crawford, James J., Staben, Steven T., Alaoui Ismaili, Moulay H., Wu, Lawren C., Ghilardi, Nico

“…NF-κB-inducing kinase (NIK) mediates non-canonical NF-κB signaling downstream of multiple TNF family members, including BAFF, TWEAK, CD40, and OX40, which are…”
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An allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance by Hagenbeek, Thijs J, Zbieg, Jason R, Hafner, Marc, Mroue, Rana, Lacap, Jennifer A, Sodir, Nicole M, Noland, Cameron L, Afghani, Shervin, Kishore, Ayush, Bhat, Kamakoti P, Yao, Xiaosai, Schmidt, Stephen, Clausen, Saundra, Steffek, Micah, Lee, Wendy, Beroza, Paul, Martin, Scott, Lin, Eva, Fong, Rina, Di Lello, Paola, Kubala, Marta H, Yang, Michelle N-Y, Lau, Jeffrey T, Chan, Emily, Arrazate, Alfonso, An, Le, Levy, Elizabeth, Lorenzo, Maria N, Lee, Ho-June, Pham, Trang H, Modrusan, Zora, Zang, Richard, Chen, Yi-Chen, Kabza, Michal, Ahmed, Musaddeque, Li, Jason, Chang, Matthew T, Maddalo, Danilo, Evangelista, Marie, Ye, Xin, Crawford, James J, Dey, Anwesha

“…The Hippo pathway is a key growth control pathway that is conserved across species. The downstream effectors of the Hippo pathway, YAP (Yes-associated protein)…”
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Safety Considerations in the Development of Hippo Pathway Inhibitors in Cancers by Kakiuchi-Kiyota, Satoko, Schutten, Melissa M, Zhong, Yu, Crawford, James J, Dey, Anwesha

“…The Hippo pathway is a critical regulator of cell and organ growth and has emerged as a target for therapeutic intervention in cancers. Its signaling is…”
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Potent and selective Bruton’s tyrosine kinase inhibitors: Discovery of GDC-0834 by Young, Wendy B., Barbosa, James, Blomgren, Peter, Bremer, Meire C., Crawford, James J., Dambach, Donna, Gallion, Steve, Hymowitz, Sarah G., Kropf, Jeffrey E., Lee, Seung H., Liu, Lichuan, Lubach, Joseph W., Macaluso, Jen, Maciejewski, Pat, Maurer, Brigitte, Mitchell, Scott A., Ortwine, Daniel F., Di Paolo, Julie, Reif, Karin, Scheerens, Heleen, Schmitt, Aaron, Sowell, C. Gregory, Wang, Xiaojing, Wong, Harvey, Xiong, Jin-Ming, Xu, Jianjun, Zhao, Zhongdong, Currie, Kevin S.

“…[Display omitted] SAR studies focused on improving the pharmacokinetic (PK) properties of the previously reported potent and selective Btk inhibitor CGI-1746…”
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Step-Economic Synthesis of (+)-Crocacin C: A Concise Crotylboronation/[3,3]-Sigmatropic Rearrangement Approach by Pasqua, Adele E, Ferrari, Frank D, Hamman, Chris, Liu, Yanzhou, Crawford, James J, Marquez, Rodolfo

“…The step-economic total synthesis of (+)-crocacin C has been achieved in 20% yield from commercially available starting materials. This approach requires the…”
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Total Synthesis and Stereochemistry of Uncialamycin by Nicolaou, K. C., Zhang, Hongjun, Chen, Jason S., Crawford, James J., Pasunoori, Laxman

“…Unseal the secrets of uncialamycin: The total synthesis of the C26 epimers of the newly discovered enediyne natural product allows its stereochemical…”
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Inhibitors of p21-activated kinases (PAKs) by Rudolph, Joachim, Crawford, James J, Hoeflich, Klaus P, Wang, Weiru

“…The p21-activated kinase (PAK) family of serine/threonine protein kinases plays important roles in cytoskeletal organization, cellular morphogenesis, and…”
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Recent progress on nuclear receptor RORγ modulators by Cyr, Patrick, Bronner, Sarah M., Crawford, James J.

“…[Display omitted] The retinoic acid receptor-related orphan receptor RORγ plays key roles in the development and differentiation of TH17 cells, and thus in…”
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Fast and efficient one step synthesis of dienamides by Mathieson, Jennifer E, Crawford, James J, Schmidtmann, Marc, Marquez, Rodolfo

“…A fast and efficient one-step approach to the synthesis of dienamides is reported. This concise methodology relies on the use of imides as reactive…”
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Hippo pathway inhibition by blocking the YAP/TAZ-TEAD interface: a patent review by Crawford, James J, Bronner, Sarah M, Zbieg, Jason R

“…: The Hippo pathway represents a new and intriguing opportunity for the treatment of cancer. Activation or overexpression of Yes-associated protein (YAP) or…”
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LogD Contributions of Substituents Commonly Used in Medicinal Chemistry by Landry, Matthew L, Crawford, James J

“…The importance of physicochemical property calculation and measurement is well-established in drug discovery. In particular, lipophilicity predictions play a…”
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RORγ antagonists and inverse agonists: a patent review by Bronner, Sarah M, Zbieg, Jason R, Crawford, James J

“…The transcription factor RORγ plays a critical role in the expression of pro-inflammatory cytokine interleukin IL-17 and is therefore an attractive target for…”
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Trust Your Gut: Strategies and Tactics for Intestinally Restricted Drugs by Dorel, Ruth, Wong, Alice R., Crawford, James J.

“…Non-absorbable small-molecule drugs targeted to the gut represent an alternative approach to safe, non-systemic therapeutics. Such drugs remain confined to the…”
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Log D Contributions of Substituents Commonly Used in Medicinal Chemistry by Landry, Matthew L, Crawford, James J

“…The importance of physicochemical property calculation and measurement is well-established in drug discovery. In particular, lipophilicity predictions play a…”
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