Activin receptor type-1C (ACVR1C)

Activin receptor type-1C (ACVR1C), also known as ALK7, is a type I receptor belonging to the transforming growth factor-beta (TGF-beta) superfamily of serine/threonine kinase receptors [1]. It plays a pivotal role in regulating energy homeostasis, adipocyte differentiation, and insulin secretion by transducing signals from ligands such as Nodal, Activin B, and GDF3 [1, 3]. Upon ligand binding, ACVR1C forms a heteromeric complex with type II receptors, leading to the phosphorylation of SMAD2 and SMAD3 proteins which then regulate gene expression in the nucleus [1, 4]. In humans, ACVR1C is predominantly expressed in adipose tissue and the pancreas, and genetic studies have linked specific variants to reduced abdominal fat and protection against type 2 diabetes [3, 4]. Beyond its metabolic functions, ACVR1C is involved in controlling cell proliferation and apoptosis, with its expression being altered in various cancers including breast and pancreatic cancer [5]. In some oncogenic contexts, it acts as a tumor suppressor by inducing apoptosis, while in others, it may facilitate tumor progression [5]. Currently, ACVR1C is being investigated as a therapeutic target for obesity and metabolic disorders, with research focusing on small molecule inhibitors and neutralizing antibodies to modulate its signaling [3, 6]. While no drugs targeting ACVR1C are currently FDA-approved, several research compounds like SB-431542 are used to study its inhibition in preclinical models [6].

Other names

ALK7Activin receptor-like kinase 7ACVRLK7

Kinase inhibition