Nonclassical Size Dependence of Permeation Defines Bounds for Passive Adsorption of Large Drug Molecules von Pye, Cameron R, Hewitt, William M, Schwochert, Joshua, Haddad, Terra D, Townsend, Chad E, Etienne, Lyns, Lao, Yongtong, Limberakis, Chris, Furukawa, Akihiro, Mathiowetz, Alan M, Price, David A, Liras, Spiros, Lokey, R. Scott

Volltext

Discovery of Potent and Orally Bioavailable Macrocyclic Peptide–Peptoid Hybrid CXCR7 Modulators von Boehm, Markus, Beaumont, Kevin, Jones, Rhys, Kalgutkar, Amit S., Zhang, Liying, Atkinson, Karen, Bai, Guoyun, Brown, Janice A., Eng, Heather, Goetz, Gilles H., Holder, Brian R., Khunte, Bhagyashree, Lazzaro, Sarah, Limberakis, Chris, Ryu, Sangwoo, Shapiro, Michael J., Tylaska, Laurie, Yan, Jiangli, Turner, Rushia, Leung, Siegfried S. F., Ramaseshan, Mahesh, Price, David A., Liras, Spiros, Jacobson, Matthew P., Earp, David J., Lokey, R. Scott, Mathiowetz, Alan M., Menhaji-Klotz, Elnaz

Volltext

Peptide to Peptoid Substitutions Increase Cell Permeability in Cyclic Hexapeptides von Schwochert, Joshua, Turner, Rushia, Thang, Melissa, Berkeley, Ray F, Ponkey, Alexandra R, Rodriguez, Kelsie M, Leung, Siegfried S F, Khunte, Bhagyashree, Goetz, Gilles, Limberakis, Chris, Kalgutkar, Amit S, Eng, Heather, Shapiro, Michael J, Mathiowetz, Alan M, Price, David A, Liras, Spiros, Jacobson, Matthew P, Lokey, R. Scott

Volltext

A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification von Nolte, Whitney M, Fortin, Jean-Philippe, Stevens, Benjamin D, Aspnes, Gary E, Griffith, David A, Hoth, Lise R, Ruggeri, Roger B, Mathiowetz, Alan M, Limberakis, Chris, Hepworth, David, Carpino, Philip A

Volltext

class of selective antibacterials derived from a protein kinase inhibitor pharmacophore von Miller, J. Richard, Dunham, Steve, Mochalkin, Igor, Banotai, Craig, Bowman, Matthew, Buist, Susan, Dunkle, Bill, Hanna, Debra, Harwood, H. James, Huband, Michael D, Karnovsky, Alla, Kuhn, Michael, Limberakis, Chris, Liu, Jia Y, Mehrens, Shawn, Mueller, W. Thomas, Narasimhan, Lakshmi, Ogden, Adam, Ohren, Jeff, Prasad, J.V.N. Vara, Shelly, John A, Skerlos, Laura, Sulavik, Mark, Thomas, V. Hayden, VanderRoest, Steve, Wang, LiAnn, Wang, Zhigang, Whitton, Amy, Zhu, Tong, Stover, C. Kendall

Volltext

Convergent Syntheses of Isomeric Imidazolospiroketones as Templates for Acetyl-CoA Carboxylase (ACC) Inhibitors von Limberakis, Chris, Smith, Aaron C., Bagley, Scott W., Yayla, Hatice G., Kung, Daniel W., Griffith, David A.

Volltext

Bioorthogonal Tethering Enhances Drug Fragment Affinity for G Protein-Coupled Receptors in Live Cells von Mattheisen, Jordan M., Limberakis, Chris, Ruggeri, Roger B., Dowling, Matthew S., am Ende, Christopher W., Ceraudo, Emilie, Huber, Thomas, McClendon, Christopher L., Sakmar, Thomas P.

Volltext

Cyclic Peptide Design Guided by Residual Dipolar Couplings, J‑Couplings, and Intramolecular Hydrogen Bond Analysis von Farley, Kathleen A, Che, Ye, Navarro-Vázquez, Armando, Limberakis, Chris, Anderson, Dennis, Yan, Jiangli, Shapiro, Michael, Shanmugasundaram, Veerabahu, Gil, Roberto R

Volltext

Route Optimization of the Non-covalent Modulator of Hemoglobin PF-07059013 for the Treatment of Sickle Cell Disease, Part I: From Discovery Synthesis to First Kilogram-Scale Manufa... von Baldwin, Aaron, Cabral, Shawn, Jones, Kris N., Kohrt, Jeffrey T., Limberakis, Chris, Liu, Yiyang, Magano, Javier, Monfette, Sebastien, Nematalla, Asaad, Ovaska, Sami, Piotrowski, David W., Piper, Jared L., Raggon, Jeffrey W., Thuma, Benjamin A., Wei, Liuqing

Volltext

Liver‐Targeted Small‐Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis von McClure, Kim F., Piotrowski, David W., Petersen, Donna, Wei, Liuqing, Xiao, Jun, Londregan, Allyn T., Kamlet, Adam S., Dechert‐Schmitt, Anne‐Marie, Raymer, Brian, Ruggeri, Roger B., Canterbury, Daniel, Limberakis, Chris, Liras, Spiros, DaSilva‐Jardine, Paul, Dullea, Robert G., Loria, Paula M., Reidich, Benjamin, Salatto, Christopher T., Eng, Heather, Kimoto, Emi, Atkinson, Karen, King‐Ahmad, Amanda, Scott, Dennis, Beaumont, Kevin, Chabot, Jeffrey R., Bolt, Michael W., Maresca, Kevin, Dahl, Kenneth, Arakawa, Ryosuke, Takano, Akihiro, Halldin, Christer

Volltext

6-Azaspiro[2.5]octanes as small molecule agonists of the human glucagon-like peptide-1 receptor von Aspnes, Gary E., Bagley, Scott W., Coffey, Steven B., Conn, Edward L., Curto, John M., Edmonds, David J., Genovino, Julien, Griffith, David A., Ingle, Gajendra, Jiao, Wenhua, Limberakis, Chris, Mathiowetz, Alan M., Piotrowski, David W., Rose, Colin R., Ruggeri, Roger B., Wei, Liuqing

Volltext

PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease von Gopalsamy, Ariamala, Aulabaugh, Ann E., Barakat, Amey, Beaumont, Kevin C., Cabral, Shawn, Canterbury, Daniel P., Casimiro-Garcia, Agustin, Chang, Jeanne S., Chen, Ming Z., Choi, Chulho, Dow, Robert L., Fadeyi, Olugbeminiyi O., Feng, Xidong, France, Scott P., Howard, Roger M., Janz, Jay M., Jasti, Jayasankar, Jasuja, Reema, Jones, Lyn H., King-Ahmad, Amanda, Knee, Kelly M., Kohrt, Jeffrey T., Limberakis, Chris, Liras, Spiros, Martinez, Carlos A., McClure, Kim F., Narayanan, Arjun, Narula, Jatin, Novak, Jonathan J., O'Connell, Thomas N., Parikh, Mihir D., Piotrowski, David W., Plotnikova, Olga, Robinson, Ralph P., Sahasrabudhe, Parag, Sharma, Raman, Thuma, Benjamin A., Vasa, Dipy, Wei, Liuqing, Wenzel, A. Zane, Withka, Jane M., Xiao, Jun, Yayla, Hatice G.

Volltext

Discovery and evaluation of non-basic small molecule modulators of the atypical chemokine receptor CXCR7 von Aspnes, Gary E., Menhaji-Klotz, Elnaz, Boehm, Markus, Londregan, Allyn T., Lee, Esther C.Y., Limberakis, Chris, Coffey, Steven B., Brown, Janice A., Jones, Rhys M., Hesp, Kevin D.

Volltext

A New and Useful Method for the Macrocyclization of Linear Peptides von Londregan, Allyn T, Farley, Kathleen A, Limberakis, Chris, Mullins, Patrick B, Piotrowski, David W

Volltext

Macrocyclizations for Medicinal Chemistry: Synthesis of Druglike Macrocycles by High-Concentration Ullmann Coupling von Collins, James C, Farley, Kathleen A, Limberakis, Chris, Liras, Spiros, Price, David, James, Keith

Volltext

In vitro metabolism of the glucagon-like peptide-1 (GLP-1)-derived metabolites GLP-1(9-36)amide and GLP-1(28-36)amide in mouse and human hepatocytes von Sharma, Raman, McDonald, Thomas S, Eng, Heather, Limberakis, Chris, Stevens, Benjamin D, Patel, Sheena, Kalgutkar, Amit S

Volltext

Short Hydrophobic Peptides with Cyclic Constraints Are Potent Glucagon-like Peptide‑1 Receptor (GLP-1R) Agonists von Hoang, Huy N, Song, Kun, Hill, Timothy A, Derksen, David R, Edmonds, David J, Kok, W. Mei, Limberakis, Chris, Liras, Spiros, Loria, Paula M, Mascitti, Vincent, Mathiowetz, Alan M, Mitchell, Justin M, Piotrowski, David W, Price, David A, Stanton, Robert V, Suen, Jacky Y, Withka, Jane M, Griffith, David A, Fairlie, David P

Volltext

Comparative pharmacokinetic profile of cyclosporine (CsA) with a decapeptide and a linear analogueElectronic supplementary information (ESI) available. See DOI: 10.1039/c7ob00096k von Price, David A, Eng, Heather, Farley, Kathleen A, Goetz, Gilles H, Huang, Yong, Jiao, Zhaodong, Kalgutkar, Amit S, Kablaoui, Natasha M, Khunte, Bhagyashree, Liras, Spiros, Limberakis, Chris, Mathiowetz, Alan M, Ruggeri, Roger B, Quan, Jun-Min, Yang, Zhen

Volltext

Revisiting N‑to‑O Acyl Shift for Synthesis of Natural Product-like Cyclic Depsipeptides von Schwochert, Joshua, Pye, Cameron, Ahlbach, Christopher, Abdollahian, Yashar, Farley, Kathleen, Khunte, Bhagyashree, Limberakis, Chris, Kalgutkar, Amit S, Eng, Heather, Shapiro, Michael J, Mathiowetz, Alan M, Price, David A, Liras, Spiros, Lokey, R. Scott

Volltext

Demonstration of the innate electrophilicity of 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine (BETP), a small-molecule positive allosteric modulator of th... von Eng, Heather, Sharma, Raman, McDonald, Thomas S, Edmonds, David J, Fortin, Jean-Philippe, Li, Xianping, Stevens, Benjamin D, Griffith, David A, Limberakis, Chris, Nolte, Whitney M, Price, David A, Jackson, Margaret, Kalgutkar, Amit S

Volltext