Willard, Francis S.

Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist

Willard, F. S., Douros, J. D., Gabe, M. B. N., Showalter, A. D., Wainscott, D. B., Suter, T. M., Capozzi, M. E., van der Velden, W. J. C., Stutsman, C., Cardona, G. R., et al. (2020) · JCI Insight

Diabetes Treatment and ManagementReceptor Mechanisms and Signaling

Cited by 541

LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept.

Coskun, T., Urva, S., Roell, W. C., Qu, H., Loghin, C., Moyers, J. S., O’Farrell, L. S., Briere, D. A., Sloop, K. W., Thomas, M. K., et al. (2022) · Cell Metabolism

Diabetes Treatment and ManagementPharmacology and Obesity Treatment

Cited by 316

Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist

Kawai, T., Sun, B., Yoshino, H., Feng, D., Suzuki, Y., Fukazawa, M., Nagao, S., Wainscott, D. B., Showalter, A. D., Droz, B. A., et al. (2020) · Proceedings of the National Academy of Sciences

Receptor Mechanisms and SignalingDiabetes Treatment and Management

Cited by 231

Novel Small Molecule Glucagon-Like Peptide-1 Receptor Agonist Stimulates Insulin Secretion in Rodents and From Human Islets

Sloop, K. W., Willard, F. S., Brenner, M. B., Ficorilli, J., Valasek, K., Showalter, A. D., Farb, T. B., Cao, J. X. C., Cox, A. L., Michael, M. D., et al. (2010) · Diabetes

Diabetes Treatment and ManagementPancreatic function and diabetes

Cited by 143

The incretin co-agonist tirzepatide requires GIPR for hormone secretion from human islets

El, K., Douros, J. D., Willard, F. S., Novikoff, A., Sargsyan, A., Perez-Tilve, D., Wainscott, D. B., Yang, B., Chen, A., Wothe, D., et al. (2023) · Nature Metabolism

Pancreatic function and diabetesDiabetes Treatment and Management

Cited by 118

The pharmacological basis for nonpeptide agonism of the GLP-1 receptor by orforglipron

Sloop, K. W., Cox, A. L., Wainscott, D. B., White, A., Droz, B. A., Stutsman, C., Showalter, A. D., Suter, T. M., Dunbar, J. D., Snider, B. M., et al. (2024) · Science Translational Medicine

Diabetes Treatment and ManagementReceptor Mechanisms and Signaling

Cited by 52

Beyond Glucagon-like Peptide-1: Is G-Protein Coupled Receptor Polypharmacology the Path Forward to Treating Metabolic Diseases?

Sloop, K. W., Briere, D. A., Emmerson, P. J., & Willard, F. S. (2018) · ACS Pharmacology & Translational Science

Diabetes Treatment and ManagementReceptor Mechanisms and Signaling

Cited by 31

679-P: The Novel GIP, GLP-1, and Glucagon Triple Receptor Agonist LY3437943 Exhibits Robust Efficacy in Preclinical Models of Obesity and Diabetes

COSKUN, T., MOYERS, J. S., ROELL, W. C., O’FARRELL, L., REGMI, A., RUAN, X., SHOWALTER, A. D., SLOOP, K., WAINSCOTT, D. B., WILLARD, F. S., et al. (2021) · Diabetes

Diabetes Treatment and ManagementRegulation of Appetite and Obesity

Cited by 10