Last update 01 Nov 2024

bacterial DHPS

Last update 01 Nov 2024

Basic Info

Synonyms

dhpS, Dihydropteroate pyrophosphorylase, Dihydropteroate synthase

Introduction

Catalyzes the condensation of para-aminobenzoate (pABA) with 6-hydroxymethyl-7,8-dihydropterin diphosphate (DHPt-PP) to form 7,8-dihydropteroate (H2Pte), the immediate precursor of folate derivatives.

Drugs associated with bacterial DHPS

Sulfamethoxazole/Potassium glycyrrhizinate/Aminocaproic Acid/Taurine

Target

11β-HSD1 x GluN2B x Plasminogen activators x bacterial DHPS

Mechanism

11β-HSD1 inhibitors [+4]

Active Org.

OPTUS Pharmaceutical Co., Ltd.

Originator Org.

OPTUS Pharmaceutical Co., Ltd.

Active Indication

Blepharitis [+2]

Inactive Indication-

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date17 Oct 2024

Sulfadoxine

Target

bacterial DHPS

Mechanism

bacterial DHPS inhibitors

Active Org.

Chengdu First Pharmaceutical Co. Ltd.

Originator Org.

F. Hoffmann-La Roche Ltd.

Active Indication

Bacterial Infections

Inactive Indication-

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date31 Dec 1989

Sulfanilamide

Target

bacterial DHPS

Mechanism

bacterial DHPS inhibitors

Active Org.

Shijiazhuang Heping Pharmaceutical Factory

Originator Org.

Mylan Specialty LP

Active Indication

Bacterial Infections

Inactive Indication

Candidiasis, Vulvovaginal

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date05 Jun 1965

126

Clinical Trials associated with bacterial DHPS

NCT06360068 / Not yet recruitingPhase 2IIT

A Prospective, Single Arm, Open Label, Proof of Concept Clinical Study of Sulfasalazine in the Treatment of Active Systemic Lupus Erythematosus

The goal of this clinical trial is to learn if sulfasalazine is safe and feasible in the treatment of active lupus erythematosus (SLE). The main questions it aims to answer are:
Does drug sulfasalazine with stable background treatment help lower the disease activity (SLEDAI) at week 16? How many patients can reach SRI-4 at week 16? Can this regimen help lower the prednisone dosage the patients need at week 16? What about the change of the type I interferon related genes expression at week 16?
Participants will:
Take sulfasalazine 750mg/dose, twice a day for 16 weeks. The dosage will be increased to 1000mg/dose within one month, twice a day if the patient could tolerate.
Visit the clinic once every 4 weeks for checkups and tests.

Start Date06 May 2024

Sponsor / Collaborator-

CTR20240762 / CompletedPhase 1

注射用HR20013对地高辛和柳氮磺吡啶在健康受试者中的药代动力学影响研究

[Translation] Effect of HR20013 for injection on the pharmacokinetics of digoxin and sulfasalazine in healthy subjects

在健康受试者中评价注射用HR20013对转运体P-gp底物地高辛和BCRP底物柳氮磺吡啶的药代动力学的影响及联合用药的安全性。

[Translation]

To evaluate the effect of HR20013 for injection on the pharmacokinetics of digoxin (a substrate of P-gp) and sulfasalazine (a substrate of BCRP) and the safety of their combined use in healthy subjects.

Start Date07 Apr 2024

Sponsor / Collaborator

Fujian Suncadia Pharmaceuticals Co Ltd.

CTRI/2024/02/062916 / Not yet recruitingPhase 2

A single-centric, double-blinded randomized parallel group non-inferiority study to the therapeutic potential of Sulfasalazine in alleviating ultrasonography detected synovitis in patients with osteoarthrities knee - NIL

Start Date26 Feb 2024

Sponsor / Collaborator-

100 Clinical Results associated with bacterial DHPS

100 Translational Medicine associated with bacterial DHPS

0 Patents (Medical) associated with bacterial DHPS

Literatures (Medical) associated with bacterial DHPS

01 Dec 2023·Journal of Genetic Engineering and Biotechnology

Polymorphism and mutational diversity of virulence (vcgCPI/vcgCPE) and resistance determinants (aac(3)-IIa, (aacC2, strA, Sul 1, and 11) among human pathogenic Vibrio species recovered from surface waters in South-Western districts of Uganda

Article

Author: Onohuean, Hope ; Nwodo, Uchechukwu U

AbstractBackgroundVibrio species are among the autochthonous bacterial populations found in surface waters and associated with various life-threatening extraintestinal diseases, especially in human populations with underlying illnesses and wound infections. Presently, very diminutive information exists regarding these species’ mutational diversity of virulence and resistance genes. This study evaluated variations in endonucleases and mutational diversity of the virulence and resistance genes of Vibrio isolates, harboring virulence-correlated gene (vcgCPI), dihydropteroate synthase type 1 and type II genes (Sul 1 and 11), (aadA) aminoglycoside (3′′) (9) adenylyltransferase gene, (aac(3)-IIa, (aacC2)a, aminoglycoside N(3)-acetyltransferase III, and (strA) aminoglycoside 3′-phosphotransferase resistance genes.MethodsUsing combinations of molecular biology techniques, bioinformatics tools, and sequence analysis.ResultsOur result revealed various nucleotide variations in virulence determinants of V. vulnificus (vcgCPI) at nucleotide positions (codon) 73–75 (A → G) and 300–302 (N → S). The aminoglycosides resistance gene (aadA) of Vibrio species depicts a nucleotide difference at position 482 (A → G), while the aminoglycosides resistance gene (sul 1 and 11) showed two variable regions of nucleotide polymorphism (102 and 140). The amino acid differences exist with the nucleotide polymorphism at position 140 (A → E). The banding patterns produced by the restriction enzymes HinP1I, MwoI, and StyD4I showed significant variations. Also, the restriction enzyme digestion of protein dihydropteroate synthase type 1 and type II genes (Sul 1 and 11) differed significantly, while enzymes DpnI and Hinf1 indicate no significant differences. The restriction enzyme NlaIV showed no band compared to reference isolates from the GenBank. However, the resistant determinants show significant point nucleotide mutation, which does not produce any amino acid change with diverse polymorphic regions, as revealed in the restriction digest profile.ConclusionThe described virulence and resistance determinants possess specific polymorphic locus relevant to pathogenomics studies, pharmacogenomic, and control of such water-associated strains.

01 Oct 2003·The Journal of Infectious DiseasesQ2 · MEDICINE

Association between a SpecificPneumocystis jiroveciDihydropteroate Synthase Mutation and Failure of Pyrimethamine/Sulfadoxine Prophylaxis in Human Immunodeficiency Virus–Positive and –Negative Patients

Q2 · MEDICINE

Article

Author: Jacques Bille ; Philippe M. Hauser ; Giorgio Zanetti ; Isabelle Meneau ; Meja Rabodonirina ; Aimable Nahimana ; Patrick Francioli

To investigate the possible association between different prophylactic sulfa drugs and the genotype of the Pneumocystis jiroveci dihydropteroate synthase (DHPS) gene, we examined DHPS polymorphisms in clinical specimens from 158 immunosuppressed patients (38 HIV-negative and 120 HIV-positive), using polymerase chain reaction-single-strand conformation polymorphism. Fifty-seven (36.1%) of 158 patients were infected with a mutant DHPS genotype. All patients who developed P. jiroveci pneumonia (PcP) while receiving pyrimethamine/sulfadoxine (PM/SD) prophylaxis (n=14) had a strain harboring DHPS with an amino acid change at position 57 (Pro-->Ser). This mutation was only present in 20 (14%) of 144 patients not receiving prophylaxis (P<.001). Hospitalization in a specific hospital was an independent risk factor for having P. jiroveci harboring the same DHPS mutation, which indirectly supports that interhuman transmission may affect the dissemination of the mutant strains.

Advances and Applications in Bioinformatics and Chemistry

Antibacterial, Docking, DFT and ADMET Properties Evaluation of Chalcone-Sulfonamide Derivatives Prepared Using ZnO Nanoparticle Catalysis

Article

Author: Mulugeta, Endale ; Melaku, Yadessa ; Weyesa, Abdanne ; Eswaramoorthy, Rajalakshmanan

INTRODUCTIONIn the present work, two novel compounds were synthesized using zinc oxide nanoparticles through green synthesis protocol. The zinc oxide nanoparticles catalyzed reactions were afforded good to excellent yields of the target compounds 76.3-98.6%.METHODOLOGYThe synthesized compounds were characterized by UV-Vis, IR and NMR. The antibacterial activity of the synthesized compounds was screened against two Gram-positive bacteria (Bacillus cereus and Staphylococcus aureus) and two Gram-negative bacteria (Escherichia coli and Salmonella typhimurium).RESULTS AND DISCUSSIONThe synthesized compounds displayed potent activity against the bacterial strains. Among them, compound 8 showed strong activity against Bacillus cereus relative to the standard drug. On the other hand, compound 9 exhibited strong activity against Escherichia coli. The molecular docking study of the synthesized compounds was conducted to investigate their binding pattern with DNA gyrase and E. coli dihydropteroate synthase and all of them were found to have minimum binding energy ranging from -6.0 to -7.3 kcal/mol, and the best result achieved with compound 8 and 9.CONCLUSIONThe findings of the in vitro antibacterial and molecular docking analysis demonstrated that the synthesized compounds have potential of antibacterial activity and can be further optimized to serve as a lead compound.

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bacterial DHPS

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