Last update 01 Nov 2024

PDF

Last update 01 Nov 2024

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

548

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 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.

01 Aug 2024·Psychological Medicine

Uncovering novel drug targets for bipolar disorder: a Mendelian randomization analysis of brain, cerebrospinal fluid, and plasma proteomes

Article

Author: Qin, Fengqin ; Han, Feng ; Zhang, Chengcheng ; Li, Yongjun ; Hu, Shiyi ; Chen, Peixi ; He, Yongji ; Jia, Tingting ; Liu, Tiancheng

AbstractBackgroundThere is a clear demand for innovative therapeutics for bipolar disorder (BD).MethodsWe integrated the largest BD genome-wide association study (GWAS) dataset (NCase = 41 917, NControl = 371 549) with protein quantitative trait loci from brain, cerebrospinal fluid, and plasma. Using a range of integrative analyses, including Mendelian randomization (MR), Steiger filter analysis, Bayesian colocalization, and phenome-wide MR analysis, we prioritized novel drug targets for BD. Additionally, we incorporated data from the UK Biobank (NCase = 1064, NControl = 365 476) and the FinnGen study (NCase = 7006, NControl = 329 192) for robust biological validation.ResultsThrough MR analysis, we found that in the brain, downregulation of DNM3, MCTP1, ABCB8 and elevation of DFNA5 and PDF were risk factors for BD. In cerebrospinal fluid, increased BD risk was associated with increased levels of FRZB, AGRP, and IL36A and decreased CTSF and LRP8. Plasma analysis revealed that decreased LMAN2L, CX3CL1, PI3, NCAM1, and TIMP4 correlated with increased BD risk, but ITIH1 did not. All these proteins passed Steiger filtering, and Bayesian colocalization confirmed that 12 proteins were colocalized with BD. Phenome-wide MR analysis revealed no significant side effects for potential drug targets, except for LRP8. External validation further underscored the concordance between the primary and validation cohorts, confirming MCTP1, DNM3, PDF, CTSF, AGRP, FRZB, LMAN2L, NCAM1, and TIMP4 are intriguing targets for BD.ConclusionsOur study identified druggable proteins for BD, including MCTP1, DNM3, and PDF in the brain; CTSF, AGRP, and FRZB in cerebrospinal fluid; and LMAN2L, NCAM1, and TIMP4 in plasma, delineating promising avenues to development of novel therapies.

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