Target intelligence / Profile preview

Anti-Müllerian hormone receptor type 2 (AMHR2) (AMHR2)

Target
AMHR2
Molecular classification
Serine/threonine kinase receptor, TGF-beta receptor family, Receptor
01

Overview

Anti-Müllerian hormone receptor type 2 (AMHR2) is a transmembrane serine/threonine kinase receptor belonging to the transforming growth factor-beta (TGF-beta) receptor family [1]. It serves as the primary receptor for Anti-Müllerian hormone (AMH), a signaling protein essential for the regression of Müllerian ducts in male embryos [1, 4]. In adult females, AMHR2 is expressed in granulosa cells where it regulates the recruitment and maturation of ovarian follicles [4]. The receptor is notably overexpressed in approximately 70-90% of epithelial ovarian cancers and other gynecological malignancies, such as endometrial and cervical cancers [2, 4]. Because its expression in healthy adult tissues is highly restricted to the gonads, AMHR2 is considered a promising target for tumor-specific immunotherapy [2, 3]. The 4D12G1 epitope is a specific region on the extracellular domain (ED) of AMHR2 recognized by the monoclonal antibody clone 4D12G1 (also known as 12G1) [2]. Therapeutic agents targeting this epitope, such as the humanized antibody 3C23K and the glyco-engineered version GM102, primarily act through antibody-dependent cellular cytotoxicity (ADCC) to eliminate malignant cells [2, 3]. These drugs are designed to provide a targeted treatment option for patients with AMHR2-positive tumors, potentially minimizing the systemic toxicity associated with conventional chemotherapy [3]. Sources: [1] UniProt Consortium. "AMHR2 - Anti-Müllerian hormone type II receptor." UniProtKB - Q16671. [2] Kersual, N., et al. "The Anti-Müllerian Hormone Type II Receptor as a New Target for Ovarian Cancer Immunotherapy." Frontiers in Oncology, 2014. (PMID: 24714539). [3] GamaMabs Pharma. "Pipeline: AMHR2-targeting antibodies." Corporate Website. [4] Bakkum-Gamez, J. N., et al. "Müllerian inhibiting substance type II receptor (MISIIR): a novel target for therapy in gynecologic cancers." Gynecologic Oncology, 2008. (PMID: 18348157).

Other names
AMHRIIMISRIIMIS receptor type IIMüllerian inhibiting substance type II receptorAnti-Müllerian hormone receptor type II
02

Mechanism of action

Antibody-dependent cellular cytotoxicity (ADCC) and inhibition of AMH-mediated signaling

03

Biological functions

Signal transductionCell differentiationMüllerian duct regressionRegulation of folliculogenesis
04

Disease associations

Ovarian cancerEndometrial cancerPersistent Müllerian duct syndrome type II
05

Safety considerations

Potential effects on reproductive functionLimited expression in normal tissues minimizes systemic toxicity
06

Interacting drugs

3C23K

2 more in the full profile.

07

Biomarkers

AMHR2 expression (IHC)Anti-Müllerian hormone (AMH) levels

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