Delving into the Latest Updates on HEP1 with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Gepon

Target-

Mechanism

Immunomodulators

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication

HIV Infections

Inactive Indication-

Originator Organization

Immapharma LLC

Active Organization

Immapharma LLC

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

RU (01 Jan 2001),

HIV Infections

Regulation-

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Structure

Molecular FormulaC74H132N26O27

InChIKeyHTQONPPEZULJKY-XRBNWYQFSA-N

CAS Registry174641-44-2

Gene Sequence

Sequence Code 24498

Source: *****

Currently, SARS-CoV-2 the novel member of the corona virus family, affecting the world leading to COVID-19 disease. It can result life-threatening condition by developing severe acute respiratory distress syndrome (ARDS). Based on previous evidence a group of patients with severe COVID-19 develop a cytokine storm syndrome which leads to hyper-inflammation lung tissue damage. Supportive care is the current management of COVID-19 is and management of ARDS as a main cause of mortality has been remained challenging. Therefore, an urgent effective treatment of COVID-19 regarding hyper-inflammation mechanism is required. Currently, development of novel anti-viral agents and vaccines are the main issues. However, it needs long time, from months to years, until suitable new medications and vaccines have been developed. An immune-modulatory tetra deca peptide (14-mer peptide) named Human Ezrin Peptide 1 (HEP-1) (trade name Gepon) was introduced by the group of Ataullakhanov in Russia. Regarding its proved anti-viral and anti-inflammatory effect, Russian authorities approved Gepon for treatment of ulcerative colitis treatment and Hepatitis -C.
In this regard, it seems that Hep-1 is a very safe immune-modulatory agent which can be effective in the management of COVID-19 infection without any adverse effect for the patient.

Start Date20 Dec 2020

Sponsor / Collaborator

Shahid Beheshti University of Medical Sciences

100 Clinical Results associated with HEP1

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100 Translational Medicine associated with HEP1

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100 Patents (Medical) associated with HEP1

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14

Literatures (Medical) associated with HEP1

01 Jul 2023·International Journal of Biological Macromolecules

Structural characterization of Hericium erinaceus polysaccharides and the mechanism of anti-T2DM by modulating the gut microbiota and metabolites

Article

Author: Jia, Le ; Li, Xueping ; Song, Xinling ; Zhang, Chen ; Cui, Weijun

A low molecular weight polysaccharides of HEP-1, with molecular weights of 1.67 × 10⁴ Da and composition of →6)-β-D-Glcp-(1→, →3)-β-D-Glcp-(1→, β-D-Glcp-(1→ and →3,6)-β-D-Glcp-(1→, was isolated and characterized from the fruiting body of Hericium erinaceus. The results indicated that HEP-1 showed potential effects against T2DM-induced imbalance of glucose and lipid metabolism by promoting the serum glucose uptake by hepatic glycogen synthesis via activating the IRS/PI3K/AKT signaling pathway, and inhibiting fatty acid synthesis and reducing hepatic lipid accumulation via activating the AMPK/SREBP-1c signaling pathways. Besides, HEP-1 promoted the production of beneficial bacteria in the gut, and increased the beneficial metabolites in liver through the gut-liver axis, consequently, resisting the occurrence of T2DM.

01 Oct 2020·PeptidesQ3 · MEDICINE

Pharmaceutical grade synthetic peptide Thr-Glu-Lys-Lys-Arg-Arg-Glu-Thr-Val-Glu-Arg-Glu-Lys-Glu ameliorates DSS-induced murine colitis by reducing the number and pro-inflammatory activity of colon tissue-infiltrating Ly6G+ granulocytes and Ly6C+ monocytes

Q3 · MEDICINE

Article

Author: Pichugin, A V ; Ataullakhanov, R I ; Chulkina, M M

A pharmaceutical grade synthetic tetradecapeptide Thr-Glu-Lys-Lys-Arg-Arg-Glu-Thr-Val-Glu-Arg-Glu-Lys-Glu (GEPON) that mimics the ezrin protein hinge region was studied in dextran sodium sulphate-induced murine experimental colitis (DSS colitis). We report that GEPON intraperitoneal injections significantly attenuated DSS-induced pathological manifestations in the large intestine, bloody diarrhoea, and body weight loss in C57BL/6 mice. GEPON markedly inhibited the transcription rate of pro-inflammatory Il1b, Il6, and Nos2 genes in the colon tissue, in contrast with those encoding anti-inflammatory factors, such as Tgfb1, I10, and Arg1, whose transcription rate did not change significantly. Using flow cytometry, we found that GEPON treatment significantly reduced the accumulation of Ly6G⁺ granulocytes and Ly6C⁺ monocytes in the colon infiltrate of DSS colitis mice. Analysis of the mRNA level in myeloid cells sorted from the colon tissue revealed that GEPON had decreased the expression of pro-inflammatory genes in both colon-infiltrating Ly6G⁺ granulocytes and Ly6C⁺ monocytes, but not in Ly6C^-CD64⁺ macrophages of DSS-treated mice. The direct anti-inflammatory impact of GEPON was shown in an in vitro culture of Ly6C⁺ monocytes, as evidenced by an inhibition of IL-1 beta and IL-6 mRNA expression. Taken together, our results demonstrated that GEPON had a pronounced therapeutic effect on ulcerative colitis in a laboratory mice model and provided evidence of its curative efficacy via inhibition of colon tissue inflammation by decreasing Ly6G⁺ granulocyte and Ly6C⁺ monocyte infiltration and by reducing their pro-inflammatory activities.

01 Sep 2017·European Journal of PharmacologyQ3 · MEDICINE

Synthetic peptide TEKKRRETVEREKE derived from ezrin induces differentiation of NIH/3T3 fibroblasts

Q3 · MEDICINE

Article

Author: Lebedeva, Ekaterina ; Ataullakhanov, Ravshan ; Negmadjanov, Ulugbek ; Pichugin, Aleksey ; Holmuhamedov, Ekhson ; Chulkina, Marina ; Mazurov, Dmitriy

Synthetic 14 AA peptide (Gepon) derived from the hinge region of ezrin, a protein that links cell surface molecules to intracellular actin filaments, accelerates and facilitates wound and ulcer healing in clinical applications. However, the molecular mechanisms underlying this phenomenon and involved in enhanced healing of wounds with Gepon are not yet understood. The purpose of current study was to investigate intracellular signaling pathways involved in the effect of this peptide on wild type and genetically modified (CD44 KO) NIH/3T3 embryonic mouse fibroblasts. Gepon treatment of NIH/3T3 cells resulted in morphological and biochemical changes, characteristic of differentiated fibroblasts. While treatment of NIH/3T3 cells with TGF-β1 triggered the activation of both canonical and non-canonical signaling pathways, exposure of fibroblasts to Gepon activated only the ERK1/2 dependent pathway without modulating SMAD dependent signaling pathway. Knocking out hyaluronic acid CD44 receptor did not change Gepon or TGF-β1 dependent activation of intracellular signaling pathways and assembling of α-SMA-positive filaments. Gepon dependent differentiation of NIH/3T3 fibroblasts is based on activation of ERK1/2 kinase, non-canonical intracellular signaling pathway. Our data suggest that the treatment of fibroblasts with Gepon triggers activation of the non-canonical (SMAD independent) intracellular signaling pathway that involves ERK1/2kinase phosphorylation. Activation of the MAPK signaling pathway and the increase in formation of α-SMA containing stress filaments induced by Gepon were independent on presence of CD44 receptor in NIH/3T3 fibroblasts. Thus, our observation designates the significance and sufficiency of MAPK pathway mediated activation of fibroblasts with Gepon for healing of erosion, ulcers and wounds.

100 Deals associated with HEP1

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