Search Results - "Hinklin, Ronald J"

A Decarboxylative Cross-Coupling Platform To Access 2‑Heteroaryl Azetidines: Building Blocks with Application in Medicinal Chemistry by Randall, Samuel D., Kowalski, John, Cruz, Cole, Shoemaker, Richard, Tarlton, Eugene, Hinklin, Ronald J.

“…Photoredox-transition metal dual catalysis provides a unique platform for constructing sp 3-rich chemical matter. Here, we report a nickel-catalyzed…”
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SHP2 Inhibition Sensitizes Diverse Oncogene-Addicted Solid Tumors to Re-treatment with Targeted Therapy by Drilon, Alexander, Sharma, Manish R, Johnson, Melissa L, Yap, Timothy A, Gadgeel, Shirish, Nepert, Dale, Feng, Gang, Reddy, Micaela B, Harney, Allison S, Elsayed, Mohamed, Cook, Adam W, Wong, Christina E, Hinklin, Ronald J, Jiang, Yutong, Brown, Eric N, Neitzel, Nickolas A, Laird, Ellen R, Wu, Wen-I, Singh, Anurag, Wei, Ping, Ching, Keith A, Gaudino, John J, Lee, Patrice A, Hartley, Dylan P, Rothenberg, S Michael

“…Rationally targeted therapies have transformed cancer treatment, but many patients develop resistance through bypass signaling pathway activation. PF-07284892…”
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Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity by Fell, Jay B, Fischer, John P, Baer, Brian R, Ballard, Joshua, Blake, James F, Bouhana, Karyn, Brandhuber, Barbara J, Briere, David M, Burgess, Laurence E, Burkard, Michael R, Chiang, Harrah, Chicarelli, Mark J, Davidson, Kevin, Gaudino, John J, Hallin, Jill, Hanson, Lauren, Hee, Kenneth, Hicken, Erik J, Hinklin, Ronald J, Marx, Matthew A, Mejia, Macedonio J, Olson, Peter, Savechenkov, Pavel, Sudhakar, Niranjan, Tang, Tony P, Vigers, Guy P, Zecca, Henry, Christensen, James G

“…KRAS is the most frequently mutated driver oncogene in human cancer, and KRAS mutations are commonly associated with poor prognosis and resistance to standard…”
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Discovery of Pyrazolopyrazines as Selective, Potent, and Mutant-Active MET Inhibitors with Intracranial Efficacy by Bumpers, Quinn A., Pipal, Robert W., Benz-Weeden, Anna M., Brewster, James T., Cook, Adam, Crooks, Amy L., Cruz, Cole, Dwulet, Natalie C., Gaudino, John J., Golec, Daniel, Harrison, Jacqueline A., Hartley, Dylan P., Hassanien, Sherif H., Hicken, Erik J., Kahn, Dean, Laird, Ellen R., Lemieux, Christine, Lewandowski, Nicholas, McCown, Joseph, McDonald, Matthew G., McNulty, Oren, Mou, Tung-Chung, Nguyen, Phong, Oko, Lauren, Opie, Lisa Pieti, Otten, Jennifer, Peck, Spencer C., Polites, Viktor C., Randall, Samuel D., Rosen, Rachel Z., Savechenkov, Pavel, Simpson, Helen, Singh, Anurag, Sparks, Drew, Wickersham, Kyle, Wollenberg, Lance, Wong, Christina E., Wong, Jim, Wu, Wen-I, Elsayed, Mohamed S. A., Hinklin, Ronald J., Tang, Tony P.

“…Mesenchymal-epithelial transition factor (MET) is a receptor tyrosine kinase that serves a critical function in numerous developmental, morphogenic, and…”
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Discovery of 5‑Azaquinoxaline Derivatives as Potent and Orally Bioavailable Allosteric SHP2 Inhibitors by Elsayed, Mohamed S. A., Blake, James F., Boys, Mark L., Brown, Eric, Chapsal, Bruno D., Chicarelli, Mark J., Cook, Adam W., Fell, Jay B., Fischer, John P., Hanson, Lauren, Lemieux, Christine, Martinson, Matthew C., McCown, Joseph, McNulty, Oren T., Mejia, Macedonio J., Neitzel, Nickolas A., Otten, Jennifer N., Rodriguez, Martha E., Wilcox, Daniel, Wong, Christina E., Zhou, Yeyun, Hinklin, Ronald J.

“…SHP2 has emerged as an important target for oncology small-molecule drug discovery. As a nonreceptor tyrosine phosphatase within the MAPK pathway, it has been…”
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Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator by Hinklin, Ronald J., Baer, Brian R., Boyd, Steven A., Chicarelli, Mark D., Condroski, Kevin R., DeWolf, Walter E., Fischer, John, Frank, Michele, Hingorani, Gary P., Lee, Patrice A., Neitzel, Nickolas A., Pratt, Scott A., Singh, Ajay, Sullivan, Francis X., Turner, Timothy, Voegtli, Walter C., Wallace, Eli M., Williams, Lance, Aicher, Thomas D.

“…[Display omitted] Glucose flux through glucokinase (GK) controls insulin release from the pancreas in response to high levels of glucose. Flux through GK is…”
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p-Methoxybenzyl Ether Cleavage by Polymer-Supported Sulfonamides by Hinklin, Ronald J, Kiessling, Laura L

“…p-Methoxybenzyl ethers have been found to transfer from alcohols to sulfonamides in the presence of catalytic trifluoromethanesulfonic acid. This process for…”
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Identification of a New Class of Glucokinase Activators through Structure-Based Design by Hinklin, Ronald J, Boyd, Steven A, Chicarelli, Mark J, Condroski, Kevin R, DeWolf, Walter E, Lee, Patrice A, Lee, Waiman, Singh, Ajay, Thomas, Laurie, Voegtli, Walter C, Williams, Lance, Aicher, Thomas D

“…Glucose flux through glucokinase (GK) controls insulin release from the pancreas in response to high glucose concentrations. Glucose flux through GK also…”
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Identification of the Clinical Development Candidate MRTX849 , a Covalent KRAS G12C Inhibitor for the Treatment of Cancer by Fell, Jay B, Fischer, John P, Baer, Brian R, Blake, James F, Bouhana, Karyn, Briere, David M, Brown, Karin D, Burgess, Laurence E, Burns, Aaron C, Burkard, Michael R, Chiang, Harrah, Chicarelli, Mark J, Cook, Adam W, Gaudino, John J, Hallin, Jill, Hanson, Lauren, Hartley, Dylan P, Hicken, Erik J, Hingorani, Gary P, Hinklin, Ronald J, Mejia, Macedonio J, Olson, Peter, Otten, Jennifer N, Rhodes, Susan P, Rodriguez, Martha E, Savechenkov, Pavel, Smith, Darin J, Sudhakar, Niranjan, Sullivan, Francis X, Tang, Tony P, Vigers, Guy P, Wollenberg, Lance, Christensen, James G, Marx, Matthew A

“…Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new…”
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Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer by Fell, Jay B, Fischer, John P, Baer, Brian R, Blake, James F, Bouhana, Karyn, Briere, David M, Brown, Karin D, Burgess, Laurence E, Burns, Aaron C, Burkard, Michael R, Chiang, Harrah, Chicarelli, Mark J, Cook, Adam W, Gaudino, John J, Hallin, Jill, Hanson, Lauren, Hartley, Dylan P, Hicken, Erik J, Hingorani, Gary P, Hinklin, Ronald J, Mejia, Macedonio J, Olson, Peter, Otten, Jennifer N, Rhodes, Susan P, Rodriguez, Martha E, Savechenkov, Pavel, Smith, Darin J, Sudhakar, Niranjan, Sullivan, Francis X, Tang, Tony P, Vigers, Guy P, Wollenberg, Lance, Christensen, James G, Marx, Matthew A

“…Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new…”
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Discovery of 2‑Pyridylureas as Glucokinase Activators by Hinklin, Ronald J, Aicher, Thomas D, Anderson, Deborah A, Baer, Brian R, Boyd, Steven A, Condroski, Kevin R, DeWolf, Walter E, Kraser, Christopher F, McVean, Maralee, Rhodes, Susan P, Sturgis, Hillary L, Voegtli, Walter C, Williams, Lance, Houze, Jonathan B

“…Glucokinase (GK) is the rate-limiting step for insulin release from the pancreas in response to high levels of glucose. Flux through GK also contributes to…”
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5‑Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties by Kohn, Todd J, Du, Xiaohui, Lai, SuJen, Xiong, YuMei, Komorowski, Renee, Veniant, Murielle, Fu, Zice, Jiao, Xianyun, Pattaropong, Vatee, Chow, David, Cardozo, Mario, Jin, Lixia, Conn, Marion, DeWolf, Walter E, Kraser, Christopher F, Hinklin, Ronald J, Boys, Mark L, Medina, Julio C, Houze, Jonathan, Dransfield, Paul, Coward, Peter

“…Two 1-(4-aryl-5-alkyl-pyridin-2-yl)-3-methylurea glucokinase activators were identified with robust in vivo efficacy. These two compounds possessed higher…”
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Stereoselective N-Glycosylation by Staudinger Ligation by He, Yi, Hinklin, Ronald J, Chang, Jiyoung, Kiessling, Laura L

“…Stereoselective methods for the chemical synthesis of β-N-glycosyl amides are needed to generate glycopeptides and glycoproteins. Here, we report that the…”
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Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394 by Dransfield, Paul J, Pattaropong, Vatee, Lai, Sujen, Fu, Zice, Kohn, Todd J, Du, Xiaohui, Cheng, Alan, Xiong, Yumei, Komorowski, Renee, Jin, Lixia, Conn, Marion, Tien, Eric, DeWolf, Walter E, Hinklin, Ronald J, Aicher, Thomas D, Kraser, Christopher F, Boyd, Steven A, Voegtli, Walter C, Condroski, Kevin R, Veniant-Ellison, Murielle, Medina, Julio C, Houze, Jonathan, Coward, Peter

“…Glucokinase (GK) catalyzes the phosphorylation of glucose to glucose-6-phosphate. We present the structure–activity relationships leading to the discovery of…”
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C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators by Du, Xiaohui, Hinklin, Ronald J, Xiong, Yumei, Dransfield, Paul, Park, Jaehyeon, Kohn, Todd J, Pattaropong, Vatee, Lai, SuJen, Fu, Zice, Jiao, Xianyun, Chow, David, Jin, Lixia, Davda, Jasmine, Veniant, Murielle M, Anderson, Deborah A, Baer, Brian R, Bencsik, Josef R, Boyd, Steven A, Chicarelli, Mark Joseph, Mohr, Peter J, Wang, Bin, Condroski, Kevin R, DeWolf, Walter E, Conn, Marion, Tran, Thanhvien, Yang, Jerry, Aicher, Thomas D, Medina, Julio C, Coward, Peter, Houze, Jonathan B

“…Glucokinase (GK) activators represent a class of type 2 diabetes therapeutics actively pursued due to the central role that GK plays in regulating glucose…”
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Glycosyl Sulfonylcarbamates:  New Glycosyl Donors with Tunable Reactivity by Hinklin, Ronald J, Kiessling, Laura L

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