MRGPRX2
Escient Presentations
MRGPRX2 Small Molecule Antagonists Potently Inhibit Agonist-Induced Skin Mast Cell Degranulation
EAACI 2023 Annual Meeting
Joshua Wollam, Michelle Solomon, Christiane Villescaz, Samantha Anderson, David Freeman, Alexis Vasquez, Corinne Pisacane, Alan Vest, Jim Napora, Brittney Charlot, Christine Cavarlez, Lisa Dvorak, Andrew Kim, Marion Lanier, Brandon Selfridge, Liming Huang, Marcos Sainz, Jennifer Brooks, Andres Nevarez, Harry Dedman, Gregg Timony, Esther Martinborough, Veena Viswanath, Marcus Boehm
MRPGRX2 Antagonist EP262 Prevents Inflammation and Disease in a Mouse Model of Atopic Dermatitis
American Academy of Dermatology (AAD) 2023 Annual Meeting
Joshua Wollam, Michelle Solomon, Christiane Villescaz, Brittney Charlot, Alan Vest, Jim Napora, Christine Cavarlez, Lisa Dvorak, Andres Nevarez, Veena Viswanath, Marcus Boehm
MRGPRX2 Antagonist EP262 Potently Inhibits Agonist-Induced Mast Cell Degranulation In Vitro and In Vivo
American Academy of Allergy, Asthma and Immunology (AAAAI) 2023 Annual Meeting
Joshua Wollam, Michelle Solomon, Christiane Villescaz, Marion Lanier, Jennifer Brooks, Andrew Kim, Samantha Anderson, Corinne Pisacane, David Freeman, Alexis Vasquez, Brittney Charlot, Alan Vest, Jim Napora, Christine Cavarlez, Lisa Dvorak, Brandon Selfridge, Liming Huang, Marcos Sainz, Andres Nevarez, Harry Dedman, Gregg Timony, Esther Martinborough, Veena Viswanath, Marcus Boehm
Treatment with MRGPRX2 Antagonist EP262 Potently Inhibits Mast Cell Degranulation
6th GA2LEN Global Urticaria Forum, December 2022
Wollam J, Solomon M, Villescaz C, Lanier M, Brooks J, Kim A, Anderson S, Pisacane C, Freeman D, Vasquez A, Charlot B, Vest A, Napora J, Cavarlez C, Dvorak L, Selfridge B, Huang L, Sainz M, Nevarez A, Timony G, Martinborough E, Viswanath V, Boehm M
Key Publications
Structure, Function and Pharmacology of Human Itch GPCRs
Cao. et al. Nature, 600:170–175, November 2021.
MRGPRX2 Activation Causes Increased Skin Reactivity in Patients with Chronic Spontaneous Urticaria
Shtessel. et al. Journal of Investigative Dermatology, 141:678-681, March 2021.
House Dust Mites Activate Nociceptor–mast Cell Clusters to Drive Type 2 Skin Inflammation
Serhan. et al. Nature Immunology, 20:1435–1443, October 2019.
A Mast-Cell-Specific Receptor Mediates Neurogenic Inflammation and Pain
Green. et al. Neuron, 101:412–420.e3, February 2019.
Upregulation of Mas-related G Protein-coupled Receptor X2 in Asthmatic Lung Mast Cells and its Activation by the Novel Neuropeptide Hemokinin-1
Manorak et al. Respiratory Research 2019:1, January 2019.
Naturally Occurring Missense MRGPRX2 Variants Display Loss of Function Phenotype for Mast Cell Degranulation in Response to Substance P, Hemokinin-1, Human β-Defensin-3, and Icatibant
Alkanfari. et al. J Immunol, 201:343-349, July 2018.
The Genetics of Chronic Itch: Gene Expression in the Skin of Patients with Atopic Dermatitis and Psoriasis with Severe Itch
Nattkemper. et al. Journal of Investigative Dermatology, 138:1311 -1317, June 2018.
Identification of a Mast-cell-specific Receptor Crucial for Pseudo-allergic Drug Reactions
McNeil. et al. Nature, 519:237–241, March 2015.
Substance P Is Upregulated in the Serum of Patients with Chronic Spontaneous Urticaria
Metz. et al. Journal of Investigative Dermatology, 134:2833–2836, November 2014.
Expression of Mas-related Gene X2 on Mast Cells is Upregulated in the Skin of Patients with Severe Chronic Urticaria
Fujisawa. et al. Journal of Allergy and Clinical Immunology, 134:622-633.E9, September 2014.
MRGPRX4
Escient Presentations
Pharmacokinetic Modeling of EP547 and Simulations of Exposure in Hepatic Impairment
ASCPT 2022
Brooks J, Kim T, Chang C, Bentley D. Pharmacokinetic Modeling of EP547 and Simulations of Exposure in Hepatic Impairment. Clin. Pharmacol. Ther. 2022;111(S1):S10. Abstract P-019
Rationale for MRGPRX4 Antagonism as a Treatment for Cholestatic and Uremic Pruritus
AASLD: The Liver Meeting, November 2021
MRGPRX4 Antagonism as a Treatment for Cholestatic and Uremic Pruritis. Hepatology. 2021;74(S1):779A-780A. Abstract 1297.
Development of EP547: A Potent, Highly Selective MRGPRX4 Inverse Agonist for the Treatment of Cholestatic and Uremic Pruritus
AASLD: The Liver Meeting, November 2021
Taylor K, Brooks B, Hemming J, Malloy J, Ferguson B, Baron A, Roberts S, Gane E. Development of EP547: A Potent, Highly Selective MRGPRX4 Inverse Agonist for the Treatment of Cholestatic and Uremic Pruritis. Hepatology. 2021;74(S1):757A. Abstract 1262.
First-in-Human Study of EP547, a Potent and Highly Selective MRGPRX4 Inverse Agonist in Development for Treatment of Cholestatic Pruritus
AASLD: The Liver Meeting, November 2021
Yeager A, Selfridge B, Sainz M, Huang L, Dvorak L, Pisacane C, Solomon M, Pittner R, Timony G, Martinborough E, Boehm M. First-in-Human Study of EP547, a Potent and Highly Selective MRGPRX4 Inverse Agonist in Development for Treatment of Cholestatic Pruritus. Hepatology. 2021;74(S1):764A-765A. Abstract 1272.
Key Publications
MRGPRX4 is a Bile Acid Receptor for Human Cholestatic Itch
Yu. et al. eLife 2019;8:e48431, September 2019.
Identification of a Bilirubin Receptor that may Mediate a Component of Cholestatic Itch
Meixiong. et. al. eLife 2019;8:e44116, January 2019.
MRGPRX4 is a G Protein-coupled Receptor Activated by Bile Acids that may Contribute to Cholestatic Pruritus
Meixiong. et al. PNAS, 116, 10525-10530, May 2019.
Prevalence of Chronic Kidney Disease-associated Pruritus Among Adult Dialysis Patients
Hu. et al. Medicine 21:e10633, May 2018.
Cholestatic Itch Management
Mittal, A. Curr Probl Dermatol, 50:142-8, 2016.