Search Results - "Falsey, James R."

Chronic glucose-dependent insulinotropic polypeptide receptor (GIPR) agonism desensitizes adipocyte GIPR activity mimicking functional GIPR antagonism by Killion, Elizabeth A., Chen, Michelle, Falsey, James R., Sivits, Glenn, Hager, Todd, Atangan, Larissa, Helmering, Joan, Lee, Jae, Li, Hongyan, Wu, Bin, Cheng, Yuan, Véniant, Murielle M., Lloyd, David J.

“…Antagonism or agonism of the glucose-dependent insulinotropic polypeptide (GIP) receptor (GIPR) prevents weight gain and leads to dramatic weight loss in…”
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GIPR antagonist antibodies conjugated to GLP-1 peptide are bispecific molecules that decrease weight in obese mice and monkeys by Lu, Shu-Chen, Chen, Michelle, Atangan, Larissa, Killion, Elizabeth A., Komorowski, Renee, Cheng, Yuan, Netirojjanakul, Chawita, Falsey, James R., Stolina, Marina, Dwyer, Denise, Hale, Clarence, Stanislaus, Shanaka, Hager, Todd, Thomas, Veena A., Harrold, John M., Lloyd, David J., Véniant, Murielle M.

“…Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) regulate glucose and energy homeostasis. Targeting both pathways with…”
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Discovery of selective biaryl ethers as PDE10A inhibitors: Improvement in potency and mitigation of Pgp-mediated efflux by Rzasa, Robert M., Hu, Essa, Rumfelt, Shannon, Chen, Ning, Andrews, Kristin L., Chmait, Samer, Falsey, James R., Zhong, Wenge, Jones, Adrie D., Porter, Amy, Louie, Steven W., Zhao, Xiaoning, Treanor, James J.S., Allen, Jennifer R.

“…We report the discovery of a novel series of biaryl ethers as potent and selective PDE10A inhibitors. Structure–activity studies improved the potency and…”
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Discovery of Highly Selective and Potent p38 Inhibitors Based on a Phthalazine Scaffold by Herberich, Brad, Cao, Guo-Qiang, Chakrabarti, Partha P, Falsey, James R, Pettus, Liping, Rzasa, Robert M, Reed, Anthony B, Reichelt, Andreas, Sham, Kelvin, Thaman, Maya, Wurz, Ryan P, Xu, Shimin, Zhang, Dawei, Hsieh, Faye, Lee, Matthew R, Syed, Rashid, Li, Vivian, Grosfeld, David, Plant, Matthew H, Henkle, Bradley, Sherman, Lisa, Middleton, Scot, Wong, Lu Min, Tasker, Andrew S

“…Investigations into the structure−activity relationships (SAR) of a series of phthalazine-based inhibitors of p38 are described. These efforts originated from…”
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A GIPR antagonist conjugated to GLP-1 analogues promotes weight loss with improved metabolic parameters in preclinical and phase 1 settings by Véniant, Murielle M., Lu, Shu-Chen, Atangan, Larissa, Komorowski, Renee, Stanislaus, Shanaka, Cheng, Yuan, Wu, Bin, Falsey, James R., Hager, Todd, Thomas, Veena A., Ambhaikar, Malhar, Sharpsten, Lucie, Zhu, Yineng, Kurra, Vamsi, Jeswani, Rohini, Oberoi, Rajneet K., Parnes, Jane R., Honarpour, Narimon, Neutel, Joel, Strande, Jennifer L.

“…Obesity is a major public health crisis. Multi-specific peptides have emerged as promising therapeutic strategies for clinical weight loss. Glucagon-like…”
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Palladium-Catalyzed Chemoselective Monoarylation of Hydrazides for the Synthesis of [1,2,4]Triazolo[4,3-a]pyridines by Reichelt, Andreas, Falsey, James R, Rzasa, Robert M, Thiel, Oliver R, Achmatowicz, Michal M, Larsen, Robert D, Zhang, Dawei

“…An efficient and convenient method for the synthesis of [1,2,4]triazolo[4,3-a]pyridines was exemplified by the synthesis of 20 analogues bearing a variety of…”
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Use of Cryopreserved Hepatocytes as Part of an Integrated Strategy to Characterize In Vivo Clearance for Peptide-Antibody Conjugate Inhibitors of Nav1.7 in Preclinical Species by Foti, Robert S, Biswas, Kaustav, Aral, Jennifer, Be, Xuhai, Berry, Loren, Cheng, Yuan, Conner, Kip, Falsey, James R, Glaus, Charles, Herberich, Brad, Hickman, Dean, Ikotun, Tayo, Li, Hongyan, Long, Jason, Huang, Liyue, Miranda, Les P, Murray, Justin, Moyer, Bryan, Netirojjanakul, Chawita, Nixey, Thomas E, Sham, Kelvin, Soto, Marcus, Tegley, Christopher M, Tran, Linh, Wu, Bin, Yin, Lin, Rock, Dan A

“…The identification of nonopioid alternatives to treat chronic pain has received a great deal of interest in recent years. Recently, the engineering of a series…”
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Engineering Antibody Reactivity for Efficient Derivatization to Generate NaV1.7 Inhibitory GpTx‑1 Peptide–Antibody Conjugates by Biswas, Kaustav, Nixey, Thomas E, Murray, Justin K, Falsey, James R, Yin, Li, Liu, Hantao, Gingras, Jacinthe, Hall, Brian E, Herberich, Brad, Holder, Jerry Ryan, Li, Hongyan, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, Soriano, Brian D, Soto, Marcus, Tran, Linh, Tegley, Christopher M, Zou, Anrou, Gunasekaran, Kannan, Moyer, Bryan D, Doherty, Liz, Miranda, Les P

“…The voltage-gated sodium channel NaV1.7 is a genetically validated pain target under investigation for the development of analgesics. A therapeutic with a less…”
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Peptide and Small Molecule Microarray for High Throughput Cell Adhesion and Functional Assays by Falsey, James R, Renil, M, Park, Steven, Li, Shijun, Lam, Kit S

“…A novel class of chemical microchips consisting of glass microscope slides was prepared for the covalent attachment of small molecule ligands and peptides…”
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N-substituted azaindoles as potent inhibitors of Cdc7 kinase by Bryan, Marian C., Falsey, James R., Frohn, Mike, Reichelt, Andreas, Yao, Guomin, Bartberger, Michael D., Bailis, Julie M., Zalameda, Leeanne, Miguel, Tisha San, Doherty, Elizabeth M., Allen, John G.

“…Cdc7 kinase is responsible for the initiation and regulation of DNA replication and has been proposed as a target for cancer therapy. We have identified a…”
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Rapid Development of Piperidine Carboxamides as Potent and Selective Anaplastic Lymphoma Kinase Inhibitors by Bryan, Marian C, Whittington, Douglas A, Doherty, Elizabeth M, Falsey, James R, Cheng, Alan C, Emkey, Renee, Brake, Rachael L, Lewis, Richard T

“…Piperidine carboxamide 1 was identified as a novel inhibitor of anaplastic lymphoma kinase (ALK enzyme assay IC50 = 0.174 μM) during high throughput screening,…”
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Engineering Na V 1.7 Inhibitory JzTx-V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics by Murray, Justin K, Wu, Bin, Tegley, Christopher M, Nixey, Thomas E, Falsey, James R, Herberich, Brad, Yin, Li, Sham, Kelvin, Long, Jason, Aral, Jennifer, Cheng, Yuan, Netirojjanakul, Chawita, Doherty, Liz, Glaus, Charles, Ikotun, Tayo, Li, Hongyan, Tran, Linh, Soto, Marcus, Salimi-Moosavi, Hossein, Ligutti, Joseph, Amagasu, Shanti, Andrews, Kristin L, Be, Xuhai, Lin, Min-Hwa Jasmine, Foti, Robert S, Ilch, Christopher P, Youngblood, Beth, Kornecook, Thomas J, Karow, Margaret, Walker, Kenneth W, Moyer, Bryan D, Biswas, Kaustav, Miranda, Les P

“…Drug discovery research on new pain targets with human genetic validation, including the voltage-gated sodium channel Na 1.7, is being pursued to address the…”
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Engineering Antibody Reactivity for Efficient Derivatization to Generate Na V 1.7 Inhibitory GpTx-1 Peptide-Antibody Conjugates by Biswas, Kaustav, Nixey, Thomas E, Murray, Justin K, Falsey, James R, Yin, Li, Liu, Hantao, Gingras, Jacinthe, Hall, Brian E, Herberich, Brad, Holder, Jerry Ryan, Li, Hongyan, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, Soriano, Brian D, Soto, Marcus, Tran, Linh, Tegley, Christopher M, Zou, Anrou, Gunasekaran, Kannan, Moyer, Bryan D, Doherty, Liz, Miranda, Les P

“…The voltage-gated sodium channel Na 1.7 is a genetically validated pain target under investigation for the development of analgesics. A therapeutic with a less…”
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Engineering NaV1.7 Inhibitory JzTx‑V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics by Murray, Justin K, Wu, Bin, Tegley, Christopher M, Nixey, Thomas E, Falsey, James R, Herberich, Brad, Yin, Li, Sham, Kelvin, Long, Jason, Aral, Jennifer, Cheng, Yuan, Netirojjanakul, Chawita, Doherty, Liz, Glaus, Charles, Ikotun, Tayo, Li, Hongyan, Tran, Linh, Soto, Marcus, Salimi-Moosavi, Hossein, Ligutti, Joseph, Amagasu, Shanti, Andrews, Kristin L, Be, Xuhai, Lin, Min-Hwa Jasmine, Foti, Robert S, Ilch, Christopher P, Youngblood, Beth, Kornecook, Thomas J, Karow, Margaret, Walker, Kenneth W, Moyer, Bryan D, Biswas, Kaustav, Miranda, Les P

“…Drug discovery research on new pain targets with human genetic validation, including the voltage-gated sodium channel NaV1.7, is being pursued to address the…”
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