Search Results - "WAINSCOTT, David B"

LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept by Coskun, Tamer, Urva, Shweta, Roell, William C., Qu, Hongchang, Loghin, Corina, Moyers, Julie S., O’Farrell, Libbey S., Briere, Daniel A., Sloop, Kyle W., Thomas, Melissa K., Pirro, Valentina, Wainscott, David B., Willard, Francis S., Abernathy, Matthew, Morford, LaRonda, Du, Yu, Benson, Charles, Gimeno, Ruth E., Haupt, Axel, Milicevic, Zvonko

“…With an increasing prevalence of obesity, there is a need for new therapies to improve body weight management and metabolic health. Multireceptor agonists in…”
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Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist by Willard, Francis S, Douros, Jonathan D, Gabe, Maria Bn, Showalter, Aaron D, Wainscott, David B, Suter, Todd M, Capozzi, Megan E, van der Velden, Wijnand Jc, Stutsman, Cynthia, Cardona, Guemalli R, Urva, Shweta, Emmerson, Paul J, Holst, Jens J, D'Alessio, David A, Coghlan, Matthew P, Rosenkilde, Mette M, Campbell, Jonathan E, Sloop, Kyle W

“…Tirzepatide (LY3298176) is a dual GIP and GLP-1 receptor agonist under development for the treatment of type 2 diabetes mellitus (T2DM), obesity, and…”
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Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan by Nelson, David L, Phebus, Lee A, Johnson, Kirk W, Wainscott, David B, Cohen, Marlene L, Calligaro, David O, Xu, Yao-Chang

“…Lasmiditan (also known as COL-144 and LY573144; 2,4,6-trifluoro-N-[6-[(1-methylpiperidin-4-yl)carbonyl]pyridin-2yl]benzamide) is a high-affinity, highly…”
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Pharmacologic characterization of the cloned human trace amine-associated receptor1 (TAAR1) and evidence for species differences with the rat TAAR1 by Wainscott, David B, Little, Sheila P, Yin, Tinggui, Tu, Yuan, Rocco, Vincent P, He, John X, Nelson, David L

“…The hemagglutinin-tagged human trace amine-associated receptor1 (TAAR1) was stably coexpressed with rat Galpha(s) in the AV12-664 cell line, and receptor…”
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Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist by Kawai, Takahiro, Sun, Bingfa, Yoshino, Hitoshi, Feng, Dan, Suzuki, Yoshiyuki, Fukazawa, Masanori, Nagao, Shunsuke, Wainscott, David B., Showalter, Aaron D., Droz, Brian A., Kobilka, Tong Sun, Coghlan, Matthew P., Willard, Francis S., Kawabe, Yoshiki, Kobilka, Brian K., Sloop, Kyle W.

“…Glucagon-like peptide-1 receptor (GLP-1R) agonists are efficacious antidiabetic medications that work by enhancing glucose-dependent insulin secretion and…”
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Structural insights into probe-dependent positive allosterism of the GLP-1 receptor by Bueno, Ana B., Sun, Bingfa, Willard, Francis S., Feng, Dan, Ho, Joseph D., Wainscott, David B., Showalter, Aaron D., Vieth, Michal, Chen, Qi, Stutsman, Cynthia, Chau, Betty, Ficorilli, James, Agejas, Francisco J., Cumming, Graham R., Jiménez, Alma, Rojo, Isabel, Kobilka, Tong Sun, Kobilka, Brian K., Sloop, Kyle W.

“…Drugs that promote the association of protein complexes are an emerging therapeutic strategy. We report discovery of a G protein-coupled receptor (GPCR) ligand…”
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Positive Allosteric Modulation of the Glucagon-like Peptide-1 Receptor by Diverse Electrophiles by Bueno, Ana B., Showalter, Aaron D., Wainscott, David B., Stutsman, Cynthia, Marín, Aranzazu, Ficorilli, James, Cabrera, Over, Willard, Francis S., Sloop, Kyle W.

“…Therapeutic intervention to activate the glucagon-like peptide-1 receptor (GLP-1R) enhances glucose-dependent insulin secretion and improves energy balance in…”
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639-P: GIP Receptor Agonism Enhances Weight Loss from Either a Biased or an Unbiased GLP-1 Receptor Agonist in DIO Mice by COGHLAN, MATTHEW P., O’FARRELL, LIBBEY, SHOWALTER, AARON D., WAINSCOTT, DAVID B., STUTSMAN, CYNTHIA, CARDONA, GUEMALLI, CABRERA, OVER, ALSINA-FERNANDEZ, JORGE, WILLARD, FRANCIS S., SLOOP, KYLE, COSKUN, TAMER

“…GIP receptor (GIPR) agonism enhances the reduction of food intake and weight loss induced by GLP-1 receptor (GLP-1R) agonism. Recently, GLP-1R agonists have…”
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The incretin co-agonist tirzepatide requires GIPR for hormone secretion from human islets by El, Kimberley, Douros, Jonathan D., Willard, Francis S., Novikoff, Aaron, Sargsyan, Ashot, Perez-Tilve, Diego, Wainscott, David B., Yang, Bin, Chen, Alex, Wothe, Donald, Coupland, Callum, Tschöp, Mattias H., Finan, Brian, D’Alessio, David A., Sloop, Kyle W., Müller, Timo D., Campbell, Jonathan E.

“…The incretins glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 1 (GLP-1) mediate insulin responses that are proportionate to…”
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Discovery of an Orally Efficacious Positive Allosteric Modulator of the Glucagon-like Peptide‑1 Receptor by Willard, Francis S, Wainscott, David B, Showalter, Aaron D, Stutsman, Cynthia, Ma, Wenzhen, Cardona, Guemalli R, Zink, Richard W, Corkins, Christopher M, Chen, Qi, Yumibe, Nathan, Agejas, Javier, Cumming, Graham R, Minguez, José Miguel, Jiménez, Alma, Mateo, Ana I, Castaño, Ana M, Briere, Daniel A, Sloop, Kyle W, Bueno, Ana B

“…The identification of LSN3318839, a positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R), is described. LSN3318839 increases the…”
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679-P: The Novel GIP, GLP-1, and Glucagon Triple Receptor Agonist LY3437943 Exhibits Robust Efficacy in Preclinical Models of Obesity and Diabetes by COSKUN, TAMER, MOYERS, JULIE S., ROELL, WILLIAM C., O’FARRELL, LIBBEY, REGMI, AJIT, RUAN, XIAOPING, SHOWALTER, AARON D., SLOOP, KYLE, WAINSCOTT, DAVID B., WILLARD, FRANCIS S., FICORILLI, JAMES V., CABRERA, OVER, URVA, SHWETA, COOPER, FARIBA NOROUZIYAN, GUO, LILI, ALSINA-FERNANDEZ, JORGE, QU, HONGCHANG

“…The ever-growing prevalence of obesity and its associated comorbidities (T2D, NASH/NAFLD) is driving the need to discover new therapies for improving metabolic…”
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Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists by DEYI ZHANG, KOHLMAN, Dan, NELSON, David L. G, SCHAUS, John M, XU, Yao-Chang, KRUSHINSKI, Joseph, LIANG, Sidney, YING, Bai-Ping, REILLY, John E, DINN, Sean R, WAINSCOTT, David B, NUTTER, Suzanne, GOUGH, Wendy

“…Several fused bicyclic systems have been investigated to serve as the core structure of potent and selective 5-HT1F receptor agonists. Replacement of the…”
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Indoloxypropanolamine analogues as 5-HT1A receptor antagonists by KRUSHINSKI, Joseph H, SCHAUS, John M, THOMPSON, Dennis C, CALLIGARO, David O, NELSON, David L, LUECKE, Susan H, WAINSCOTT, David B, WONG, David T

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Novel Potent 5-HT1F Receptor Agonists:  Structure−Activity Studies of a Series of Substituted N-[3-(1-Methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides by Filla, Sandra A, Mathes, Brian M, Johnson, Kirk W, Phebus, Lee A, Cohen, Marlene L, Nelson, David L, Zgombick, John M, Erickson, Jon A, Schenck, Kathryn W, Wainscott, David B, Branchek, Theresa A, Schaus, John M

“…Compound 1a (LY334370), a selective 5-HT1F receptor agonist (SSOFRA), inhibited dural inflammation in the neurogenic plasma protein extravasation model of…”
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[3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties by Wainscott, David B, Krushinski, Jr, Joseph H, Audia, James E, Schaus, John M, Zgombick, John M, Lucaites, Virginia L, Nelson, David L

“…[(3)H]LY334370 was developed as a radioligand to study the characteristics of this compound's interaction with the 5-HT(1F) receptor. Monovalent or divalent…”
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Dihydrobenzofuran Analogues of Hallucinogens. 3. Models of 4-Substituted (2,5-Dimethoxyphenyl)alkylamine Derivatives with Rigidified Methoxy Groups by Monte, Aaron P, Marona-Lewicka, Danuta, Parker, Matthew A, Wainscott, David B, Nelson, David L, Nichols, David E

“…Tetrahydrobenzodifuran functionalities were employed as conformationally restricted bioisosteres of the aromatic methoxy groups in prototypical hallucinogenic…”
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Dihydrobenzofuran Analogues of Hallucinogens. 4. Mescaline Derivatives by Monte, Aaron P, Waldman, Steve R, Marona-Lewicka, Danuta, Wainscott, David B, Nelson, David L, Sanders-Bush, Elaine, Nichols, David E

“…Dihydrobenzofuran and tetrahydrobenzodifuran functionalities were employed as conformationally restricted bioisosteres of the aromatic methoxy groups in the…”
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Substituted furo[3,2-b]pyridines: novel bioisosteres of 5-HT1F receptor agonists by MATHES, Brian M, HUDZIAK, Kevin J, FILLA, Sandra A, SCHAUS, John M, XU, Yao-Chang, NELSON, David L, WAINSCOTT, David B, NUTTER, Suzanne E, GOUGH, Wendy H, BRANCHEK, Theresa A, ZGOMBICK, John M

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Substituted furo[3,2- b]pyridines: novel bioisosteres of 5-HT 1F receptor agonists by Mathes, Brian M., Hudziak, Kevin J., Schaus, John M., Xu, Yao-Chang, Nelson, David L., Wainscott, David B., Nutter, Suzanne E., Gough, Wendy H., Branchek, Theresa A., Zgombick, John M., Filla, Sandra A.

“…Synthesis and evaluation of a series of 2,3,5- and 3,5-substituted furo[3,2- b]pyridines were undertaken in order to investigate their utility as bioisosteres…”
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Substituted Naphthofurans as Hallucinogenic Phenethylamine−Ergoline Hybrid Molecules with Unexpected Muscarinic Antagonist Activity by Monte, Aaron P, Marona-Lewicka, Danuta, Lewis, Mechelle M, Mailman, Richard B, Wainscott, David B, Nelson, David L, Nichols, David E

“…A series of substituted racemic naphthofurans were synthesized as “hybrid” molecules of the two major prototypical hallucinogenic drug classes, the…”
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