Last update 01 Nov 2024

pantetheinase

Last update 01 Nov 2024

Basic Info

Synonyms

Pantetheinase, Pantetheine hydrolase, Tiff66

+ [4]

Introduction

Amidohydrolase that hydrolyzes specifically one of the carboamide linkages in D-pantetheine thus recycling pantothenic acid (vitamin B5) and releasing cysteamine.

Drugs associated with pantetheinase

MY-009212A

Target

pantetheinase

Mechanism

pantetheinase inhibitors

Active Org.

Shanghai Meiyue Biotech Development Co. Ltd.

Originator Org.

Shanghai Meiyue Biotech Development Co. Ltd.

Active Indication

Inflammatory Bowel Diseases

Inactive Indication-

Drug Highest PhasePhase 1

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

pantetheinase inhibitors(Pfizer)

Target

pantetheinase

Mechanism

pantetheinase inhibitors

Active Org.

Pfizer Inc.

Originator Org.

Pfizer Inc.

Active Indication

Inflammatory Bowel Diseases

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with pantetheinase

CTR20223094 / CompletedPhase 1

一项评估MY009212A片多次给药在健康成年志愿者中的安全性、耐受性和药代动力学特征的随机、双盲、安慰剂对照、剂量递增I期临床试验

[Translation] A randomized, double-blind, placebo-controlled, dose-escalation phase I clinical trial to evaluate the safety, tolerability and pharmacokinetic characteristics of multiple-dose MY009212A tablets in healthy adult volunteers

主要目的：评估MY009212A片多次给药在健康成年志愿者中的安全性和耐受性；次要目的：评估MY009212A片多次给药在健康成年志愿者中的PK特征；探索性目的：初步探索MY009212A片多次给药在健康成年志愿者中的PD特征；初步开展人体中药物代谢探索性研究，尝试对主要代谢产物进行定量研究。

[Translation]

Primary objective: To evaluate the safety and tolerability of multiple doses of MY009212A tablets in healthy adult volunteers; Secondary objective: To evaluate the PK characteristics of multiple doses of MY009212A tablets in healthy adult volunteers; Exploratory objective: To preliminarily explore the PD characteristics of multiple doses of MY009212A tablets in healthy adult volunteers; To preliminarily conduct exploratory studies on drug metabolism in humans and attempt to conduct quantitative studies on major metabolites.

Start Date13 Dec 2022

Sponsor / Collaborator

Shanghai Meiyue Biotech Development Co. Ltd.

CTR20222327 / CompletedPhase 1

一项在健康成年受试者中评价食物对MY009212A片的药代动力学特征影响的开放、随机、单剂量、两交叉研究

[Translation] An open-label, randomized, single-dose, two-crossover study to evaluate the effect of food on the pharmacokinetic profile of MY009212A tablets in healthy adult subjects

主要目的：评估食物对健康成年受试者单次口服MY009212A片的药代动力学（PK）特征的影响；次要目的：评估食物对健康成年受试者单次口服MY009212A片安全性的影响。

[Translation]

The primary objective was to evaluate the effect of food on the pharmacokinetic (PK) characteristics of a single oral dose of MY009212A tablets in healthy adult subjects. The secondary objective was to evaluate the effect of food on the safety of a single oral dose of MY009212A tablets in healthy adult subjects.

Start Date25 Sep 2022

Sponsor / Collaborator

Shanghai Meiyue Biotech Development Co. Ltd.

ChiCTR2200061203 / SuspendedPhase 1IIT

A phase I clinical trial to evaluate the safety, tolerability and pharmacokinetic profiles of single-dose MY009212A in healthy adult volunteers

Start Date01 Jun 2022

Sponsor / Collaborator

The Second Affiliated Hospital of Anhui Medical University

100 Clinical Results associated with pantetheinase

100 Translational Medicine associated with pantetheinase

0 Patents (Medical) associated with pantetheinase

277

Literatures (Medical) associated with pantetheinase

01 Dec 2024·European Journal of Medicinal Chemistry

Chemical synthesis and enzymatic late-stage diversification of novel pantothenate analogues with antiplasmodial activity

Article

Author: Thistlethwaite, Sian ; Liu, Xiangning ; Auclair, Karine ; Pierscianowski, Jacob ; Kholiya, Rohit ; Saliba, Kevin J. ; Saliba, Kevin J

The emergence of resistance to nearly every therapeutic agent directed against malaria-causing Plasmodium parasites emphasises the dire need for new antimalarials. Despite their high potency and low cytotoxicity in vitro, the clinical use of pantothenamides is hindered by pantetheinase-mediated hydrolysis in human serum. We herein report the chemical synthesis and biological activity of a new series of pantothenamide analogues in which the labile amide group is replaced with an isoxazole ring. In addition, we utilised, for the first time, enzymatic late-stage diversification to generate additional isoxazole-containing pantothenamide-mimics. Thirteen novel isoxazole-containing pantothenamide-mimics were generated, several of which display nanomolar antiplasmodial activity against Plasmodium falciparum and are non-toxic to human cells in vitro. Although the derivatives generated via late-stage diversification are less potent than the parent compounds, the most potent still exerted its activity via a mechanism that interferes with the pantothenate-utilising process and appears to be nontoxic to human cells. This increases the appeal of using late-stage diversification to modify pantothenamide-mimics, potentially leading to compounds with improved antiplasmodial and/or pharmacological properties.

25 Oct 2024·ACS Sensors

Development of an Activity-Based Ratiometric Electrochemical Switch for Direct, Real-Time Sensing of Pantetheinase in Live Cells, Blood, and Urine Samples

Article

Author: Kumaragurubaran, Namasivayam ; Wei, Yi-Cheng ; Huang, Sheng-Tung ; Morkvenaite-Vilkonciene, Inga ; Lin, Hsin-Yi ; Huang, Yan-Zhi ; Mockaitis, Tomas ; Arul, Ponnusamy

Pantetheinase is a key biomarker for the diagnosis of acute kidney injury and the monitoring of malaria progression. Currently, existing methods for sensing pantetheinase, also known as Vanin-1, show considerable potential but come with certain limitations, including their inability to directly sense analytes in turbid biofluid samples without tedious sample pretreatment. Here, we describe the first activity-based electrochemical probe, termed VaninLP, for convenient and specific direct targeting of pantetheinase activity in turbid liquid biopsy samples. The probe was designed such that cleavage of the pantetheinase amide linkage, triggered by a self-immolative reaction, simultaneously ejects an amino ferrocene reporter. Among the distinctive properties of the VaninLP probe for sensing pantetheinase are its high selectivity, sensitivity, and enzyme affinity, a wide linear concentration range (8-300 ng/mL), and low limit of detection (2.47 ng/mL). The designed probe precisely targeted pantetheinase and was free of interference by other electroactive biological species. We further successfully applied the VaninLP probe to monitor and quantify the activity of pantetheinase on the surfaces of HepG2 tumor cells, blood, and urine samples. Collectively, our findings indicate that VaninLP holds significant promise as a point-of-care tool for diagnosing early-stage kidney injury, as well as monitoring the progression of malaria.

01 Aug 2024·Vascular Medicine

Urinary vanin-1 as a novel biomarker for survival in peripheral artery disease

Article

Author: Bojic, Marija ; Zierfuss, Bernhard ; Karlinger, Anna ; Schernthaner, Gerit-Holger ; Koppensteiner, Renate ; Höbaus, Clemens

Background: Chronic kidney disease is associated with increased rates of incidence, morbidity, and mortality in lower-extremity peripheral artery disease (PAD). No specific marker for a functional risk assessment of kidney disease in PAD is known, especially at the early stages. Thus, we speculated that urinary vanin-1 (uVNN1), a marker of oxidative stress even in early kidney injury, could further stratify outcome assessment in patients with PAD. Methods: Patients with stable PAD ( n = 304) of the Vienna medical cohort were followed up for up to 10 years and the outcome was assessed by central death database queries. uVNN1 was measured by enzyme-linked immunosorbent assay (ELISA) at study inclusion and normalized to urinary creatinine (uVNN1/Cr). During the observation time (9.3, 7.0–9.8 years), 104 patients died, 54.8% of which were due to cardiovascular causes. Results: uVNN1/Cr was associated with a urine albumin–creatinine ratio (UACR) ( R = 0.166, p = 0.004) but not with an estimated glomerular filtration rate ( R = 0.102, p = 0.077). Levels of uVNN1/Cr did not differ between asymptomatic and symptomatic PAD ( p = 0.406). Kaplan–Meier curves showed a clear-cut association with higher all-cause (log-rank p = 0.034) and cardiovascular mortality (log-rank p = 0.032) with higher uVNN1/Cr levels. Similarly, significant associations for all-cause (hazard ratio [HR] 1.34, 95% CI [1.08–1.67], p = 0.009) and cardiovascular mortality (HR 1.45, 95% CI [1.06–1.99], p = 0.020) could be seen in multivariable Cox regression models. Conclusions: uVNN1/Cr showed an independent association with both all-cause and cardiovascular mortality in patients with PAD and was associated with early kidney disease. Thus, uVNN1 could be a useful marker for risk stratification of kidney disease in PAD.

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