HPN Membrane Protein Introduction

Introduction of HPN

Serine protease hepsin, also known as transmembrane protease serine 1 or HPN, is a cell surface-expressed trypsin-like serine protease which is predominantly expressed in normal human liver. HPN in human is encoded by the HPN gene. And it belongs to the type II transmembrane serine protease (TTSP) family. Specifically, HPN contains an N-terminal cytoplasmic domain, a transmembrane domain, and an extracellular portion composed of a scavenger receptor-like cysteine-rich domain (SRCR domain) and a C-terminal protease domain with a trypsin-like fold (S1 domain).

Basic Information of HPN
Protein Name	Serine protease hepsin
Gene Name	HPN
Aliases	Transmembrane protease serine 1
Organism	Homo sapiens (Human)
UniProt ID	P05981
TransmHPNrane Times	1
Length (aa)	417
Sequence	MAQKEGGRTVPCCSRPKVAALTAGTLLLLTAIGAASWAIVAVLLRSDQEPLYPVQVSSADARLMVFDKTEGTWRLLCSSRSNARVAGLSCEEMGFLRALTHSELDVRTAGANGTSGFFCVDEGRLPHTQRLLEVISVCDCPRGRFLAAICQDCGRRKLPVDRIVGGRDTSLGRWPWQVSLRYDGAHLCGGSLLSGDWVLTAAHCFPERNRVLSRWRVFAGAVAQASPHGLQLGVQAVVYHGGYLPFRDPNSEENSNDIALVHLSSPLPLTEYIQPVCLPAAGQALVDGKICTVTGWGNTQYYGQQAGVLQEARVPIISNDVCNGADFYGNQIKPKMFCAGYPEGGIDACQGDSGGPFVCEDSISRTPRWRLCGIVSWGTGCALAQKPGVYTKVSDFREWIFQAIKTHSEASGMVTQL

Function of HPN Membrane Protein

Serine protease hepsin plays a role in cell growth and maintenance of cell morphology. And it is involved in the proteolytic processing of ACE2. It has been also shown that hepsin may mediate the proteolytic cleavage of urinary UMOD which is required for UMOD polymerization. Hepsin is prominently expressed in the human liver and several types of tumors, including prostate cancer, endometrial cancer, and renal cell carcinoma. It has been identified as one of the most highly up-regulated proteases in prostate cancer and immunohistochemical staining indicates its strong expression in late-stage tumors and metastatic bone lesions. Overexpression of hepsin in the prostate epithelium weakens the epithelial-stromal adhesion and disrupts the basement membrane. In preclinical studies using prostate cancer models, it has been shown that hepsin may play a role in invasive cancer growth, cancer progression. Hepsin has been also supposed to promote primary prostate cancer metastasis.

Fig.1 Structure of Serine Protease Hepsin.

Application of HPN Membrane Protein in Literature

Lee S.G., et al. RIPL peptide-conjugated nanostructured lipid carriers for enhanced intracellular drug delivery to hepsin-expressing cancer cells. Int J Nanomedicine. 2018, 13: 3263-3278. PubMed ID: 29910614

Authors in this article considered the RIPL-NLCs as good candidates for Hpn-selective drug targeting with a high loading capacity of hydrophobic drug molecules.
Pant S.M., et al. Analyzing the Type II Transmembrane Serine Protease Hepsin-Dependent Basement Membrane Remodeling in 3D Cell Culture. Methods Mol Biol. 2018, 1731: 169-178. PubMed ID: 29318553

Authors in this article described how to establish a 3D mammary epithelial culture in an exogenous basement membrane-free egg white matrix and provided a protocol for quantitative analysis of the impact of hepsin on laminin-332 and its hemidesmosomal receptor α6-integrin by means of confocal microscopy imaging.
Pant S.M., et al. Design, Synthesis, and Testing of Potent, Selective Hepsin Inhibitors via Application of an Automated Closed-Loop Optimization Platform. J Med Chem. 2018, 61(10): 4335-4347. PubMed ID: 29701962

This article focused on rapidly developing potent and selective inhibitors of hepsin, using integrated design, synthesis, and screening platform.
Nassan M., et al. Exploring hepsin functional genetic variation association with disease specific protein expression in bipolar disorder: Applications of a proteomic informed genomic approach. J Psychiatr Res. 2017, 95: 208-212. PubMed ID: 22753192

This article attempted to study the potential functional role of serum Growth Differentiation Factor 15 (GDF15), Hepsin (HPN), and Matrix Metalloproteinase-7 (MMP7) in bipolar disorder (BP).
Kwon H., et al. Recent Advances of Hepsin-Targeted Inhibitors. Curr Med Chem. 2017, 24(21): 2294-2311. PubMed ID: 28245763

This article discussed design strategy, structure-activity relationship (SAR), and binding mode of the four classes of hepsin inhibitors.

HPN Preparation Options

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