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Last update 23 Jan 2025

PDF

Last update 23 Jan 2025

Basic Info

Synonyms

PDF, PDF1A, peptide deformylase, mitochondrial

+ [1]

Introduction

Removes the formyl group from the N-terminal Met of newly synthesized proteins.

Drugs associated with PDF

PDF inhibitor(Imagene)

Target

PDF

Mechanism

PDF inhibitors

Active Org.

IMAGENE Co., Ltd.

Originator Org.

IMAGENE Co., Ltd.

Active Indication

Infectious Diseases

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

PDF inhibitors(Centre National de la Recherche Scientifique)

Target

PDF

Mechanism

PDF inhibitors

Active Org.

Centre National de la Recherche Scientifique

Originator Org.

Centre National de la Recherche Scientifique

Active Indication

Bacterial Infections

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with PDF

100 Translational Medicine associated with PDF

0 Patents (Medical) associated with PDF

558

Literatures (Medical) associated with PDF

01 Jan 2025·Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy

Synthesis and antibacterial evaluation of (5Z)-5-[(2-piperidinequinoline-3-yl)methyl]-2-chloroquinoline derivatives: Docking study on substituted N-alkylation and binding mechanisms with E. Coli PDF enzyme

Article

Author: Juddhawala, K V ; Parekh, N.M. ; Nagaraj, Karuppiah ; Alswieleh, Abdullah ; Juddhawala, K.V. ; Parekh, Nikhil M

A number of new substances were included into the (5Z)-5-[(2-piperidinequinoline-3-yl)methyl]-2-chloroquinoline structural framework. The condensation process 2-chloroquinoline, which served as a crucial reagent in the reaction with 3-carbaldehydes to produce 2,4-thiazolidinedione, allowed for the production of 1,3-thiazolidine-2,4-dione. The newly developed substances were described by means of their reactions with halide compounds, particularly those pertaining to substituted N-alkylation. Elemental analysis, Fourier-transform infrared spectroscopy (FT-IR), and proton nuclear magnetic resonance spectroscopy (¹H NMR) were used to identify the chemical. Furthermore, the antibacterial activity of the produced compounds was evaluated in vitro against a range of pathogens, including Bacillus subtilis, and Escherichia coli. Moreover, docking experiments were conducted using the PDF enzyme of E. coli to improve our understanding of the binding mechanism between the synthesized 5(A-N) compounds and the enzyme.

01 Dec 2024·Cell Reports

Molecular module for glucose production influences sex pheromone synthesis in Bactrocera dorsalis

Article

Author: Jiang, Yanling ; Wang, Zhenghao ; Cheng, Daifeng ; Teng, Hebo ; Li, Xinlian ; Ye, Long ; Chen, Huimin ; Lu, Yongyue ; Chen, Jingxiang ; Yang, Xiaorui

Some insects have evolved beneficial relationships with intestinal microbes for sex pheromone production to communicate with conspecifics effectively. However, it is not clear whether the sex pheromone synthesis activity of intestinal microbes can be controlled by the host, and the molecular mechanisms need to be further unraveled. In this study, we find that rectal gland Bacillus species of male Bactrocera dorsalis specifically produce sex pheromones in the evening, which is significantly associated with glucose levels. In vitro Bacillus culture assays show that glucose levels significantly influence the amount of sex pheromone produced. Comparative rectal gland transcriptome analysis reveals that the expressions of the alpha-galactosidase gene (GLA), a Bactrocera dorsalis transcription factor (BDTF), and a pigment-dispersing factor (PDF) are responsible for producing glucose. Our findings reveal that the PDF-BDTF-GLA module influences the intestinal-microbe-produced sex pheromone by regulating glucose levels and advance our understanding of interactions between insects and their intestinal microbes.

01 Sep 2024·Journal of Biomolecular Structure and Dynamics

Design, synthesis and antimicrobial activity of novel quinoline derivatives: an in silico and in vitro study

Article

Author: Mishra, Richa ; Rai, Shivangi ; Som, Anup ; Singh, Ramendra K ; Kumari, Priyanka ; Singh, Vishal K

A series of new quinoline derivatives has been designed, synthesized and evaluated as antibacterial and antifungal agents functioning as peptide deformylase enzyme (PDF) inhibitors and fungal cell wall disruptors on the basis of computational and experimental methods. The molecular docking and ADMET assessment aided in the synthesis of quinoline derivatives starting from 6-amino-4-methyl-1H-quinoline-2-one substituted with different types of sulfonyl/benzoyl/propargyl moieties. These newly synthesized compounds were evaluated for their in vitro antibacterial and antifungal activity. Antibacterial screening of all compounds showed excellent MIC value (MIC, 50 - 3.12 µg/mL) against bacterial strains, viz. Bacillus cerus, Staphylococcus, Pseudomonas and Escherichia coli. Compounds 2 and 6 showed better activity. Fractional inhibitory concentration (FIC) values of compounds were lowered by 1/2 to 1/128 of the original MIC values when a combinatorial screening with reference drugs was performed. Further, antifungal screening against fungal strains, viz. A. flavus, A. niger, F. oxysporum and C. albicans also showed that all compounds were potentially active and compound 6 being the most potent. Further, the cytotoxicity experiments revealed that compound 6 was the least toxic molecule. The molecular dynamics (MD) simulation investigations elucidated the conformational stability of compound 6-PDF complex with flexible binding pocket residues. The highest number of stable hydrogen bonds with the PDF residues during the entire simulation time illustrated strong binding affinity of compound 6 with PDF.Communicated by Ramaswamy H. Sarma.

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