Sloop, Kyle W.

LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept

Coskun, T., Sloop, K. W., Loghin, C., Alsina-Fernandez, J., Urva, S., Bokvist, K. B., Cui, X., Briere, D. A., Cabrera, O., Roell, W. C., et al. (2018) · Molecular Metabolism

Diabetes Treatment and ManagementDiabetes Management and Research

Cited by 882

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

How May GIP Enhance the Therapeutic Efficacy of GLP-1?

Samms, R. J., Coghlan, M. P., & Sloop, K. W. (2020) · Trends in Endocrinology & Metabolism

Diabetes Treatment and ManagementRegulation of Appetite and Obesity

Cited by 419

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

GIPR agonism mediates weight-independent insulin sensitization by tirzepatide in obese mice

Samms, R. J., Christe, M. E., Collins, K. A. L., Pirro, V., Droz, B. A., Holland, A. K., Friedrich, J. L., Wojnicki, S., Konkol, D. L., Cosgrove, R., et al. (2021) · Journal of Clinical Investigation

Diabetes Treatment and ManagementAdipokines, Inflammation, and Metabolic Diseases

Cited by 256

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

GIP mediates the incretin effect and glucose tolerance by dual actions on α cells and β cells

El, K., Gray, S. M., Capozzi, M. E., Knuth, E. R., Jin, E., Svendsen, B., Clifford, A., Brown, J. L., Encisco, S. E., Chazotte, B. M., et al. (2021) · Science Advances

Pancreatic function and diabetesDiabetes Treatment and Management

Cited by 132

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

GLP-1 Receptor in Pancreatic α-Cells Regulates Glucagon Secretion in a Glucose-Dependent Bidirectional Manner

Zhang, Y., Parajuli, K. R., Fava, G. E., Gupta, R., Xu, W., Nguyen, L. U., Zakaria, A. F., Fonseca, V. A., Wang, H., Mauvais-Jarvis, F., et al. (2019) · Diabetes

Pancreatic function and diabetesDiabetes Treatment and Management

Cited by 104

Tirzepatide induces a thermogenic-like amino acid signature in brown adipose tissue

Samms, R. J., Zhang, G., He, W., Ilkayeva, O., Droz, B. A., Bauer, S. M., Stutsman, C., Pirro, V., Collins, K. A., Furber, E. C., et al. (2022) · Molecular Metabolism

Adipose Tissue and MetabolismAdipokines, Inflammation, and Metabolic Diseases

Cited by 93

Orforglipron ( LY3502970 ), a novel, oral non‐peptide glucagon‐like peptide‐1 receptor agonist: A Phase 1a, blinded, placebo‐controlled, randomized, single‐ and multiple‐ascending‐dose study in healthy participants

Pratt, E., Ma, X., Liu, R., Robins, D., Haupt, A., Coskun, T., Sloop, K. W., & Benson, C. (2023) · Diabetes, Obesity and Metabolism

Diabetes Treatment and ManagementPharmacology and Obesity Treatment

Cited by 62

Absence of Glucagon and Insulin Action Reveals a Role for the GLP-1 Receptor in Endogenous Glucose Production

Jun, L. S., Millican, R. L., Hawkins, E. D., Konkol, D. L., Showalter, A. D., Christe, M. E., Michael, M. D., & Sloop, K. W. (2015) · Diabetes

Diabetes Treatment and ManagementPancreatic function and diabetes

Cited by 60

Orforglipron ( LY3502970 ), a novel, oral non‐peptide glucagon‐like peptide‐1 receptor agonist: A Phase 1b, multicentre, blinded, placebo‐controlled, randomized, multiple‐ascending‐dose study in people with type 2 diabetes

Pratt, E., Ma, X., Liu, R., Robins, D., Coskun, T., Sloop, K. W., Haupt, A., & Benson, C. (2023) · Diabetes, Obesity and Metabolism

Diabetes Treatment and ManagementPharmacology and Obesity Treatment

Cited by 60

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

GIPR Function in the Central Nervous System: Implications and Novel Perspectives for GIP-Based Therapies in Treating Metabolic Disorders

Samms, R. J., Sloop, K. W., Gribble, F. M., Reimann, F., & Adriaenssens, A. E. (2021) · Diabetes

Regulation of Appetite and ObesityDiabetes Treatment and Management

Cited by 49

Is Glucagon Receptor Activation the Thermogenic Solution for Treating Obesity?

Conceição-Furber, E., Coskun, T., Sloop, K. W., & Samms, R. J. (2022) · Frontiers in Endocrinology

Regulation of Appetite and ObesityPharmacology and Obesity Treatment

Cited by 48

Effect of Food Consumption on the Pharmacokinetics, Safety, and Tolerability of Once-Daily Orally Administered Orforglipron (LY3502970), a Non-peptide GLP-1 Receptor Agonist

Ma, X., Liu, R., Pratt, E. J., Benson, C. T., Bhattachar, S. N., & Sloop, K. W. (2024) · Diabetes Therapy

Diabetes Treatment and ManagementPharmacology and Obesity Treatment

Cited by 38

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