Identification
- Summary
-
Ertapenemis a carbapenem antibiotic used for the treatment of moderate to severe bacterial infections caused by specific sensitive organisms.
- Brand Names
-
Invanz
- Generic Name
- Ertapenem
- DrugBank Accession Number
- DB00303
- Background
-
Ertapenem is a carbapenem antibiotic drug that is marketed under the trade name Invanz by Merck & Co. pharmaceutical company. It is structurally similar tomeropenemand possesses a 1-beta-methyl group.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
-
Structure for Ertapenem (DB00303)
- Weight
-
Average: 475.515
Monoisotopic: 475.141320859 - Chemical Formula
- C22H25N3O7S
- Synonyms
-
- (1R,5S,6S,8R,2'S,4'S)-2-(2-(3-carboxyphenylcarbamoyl)pyrrolidin-4-ylthio)-6-(1-hydroxyethyl)-1-methylcarbapenem-3-carboxylic acid
- (4R,5S,6S)-3-((3S,5S)-5-((3-carboxyphenyl)carbamoyl)pyrrolidin-3-ylthio)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-1-aza-bicyclo[3.2.0]hept-2-ene-2-carboxylic acid
- Ertapenem
Pharmacology
- Indication
-
For the treatment the following moderate to severe infections caused by susceptible isolates of the designated microorganisms: (1) complicated intra-abdominal infections due toEscherichia coli,Clostridium clostridioforme,Eubacterium lentum,Peptostreptococcusspecies,Bacteroides fragilis,Bacteroides distasonis,Bacteroides ovatus,Bacteroides thetaiotaomicron, orBacteroides uniformis, (2) complicated skin and skin structure infections, including diabetic foot infections without osteomyelitis due toStaphylococcus aureus(methicillin susceptible isolates only),Streptococcus agalactiae,Streptococcus pyogenes,Escherichia coli,Klebsiella pneumoniae,Proteus mirabilis,Bacteroides fragilis,Peptostreptococcusspecies,Porphyromonas asaccharolytica, orPrevotella bivia, (3) community acquired pneumonia due toStreptococcus pneumoniae(penicillin susceptible isolates only) including cases with concurrent bacteremia,Haemophilus influenzae(beta-lactamase negative isolates only), orMoraxella catarrhalis, (4) complicated urinary tract infections including pyelonephritis due toEscherichia coli, including cases with concurrent bacteremia, orKlebsiella pneumoniae, (5) acute pelvic infections including postpartum endomyometritis, septic abortion and post surgical gynecologic infections due toStreptococcus agalactiae,Escherichia coli,Bacteroides fragilis,Porphyromonas asaccharolytica,Peptostreptococcusspecies, orPrevotella bivia.
Reduce drug development failure ratesBuild, train, & validate machine-learning models
with evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets. - Associated Conditions
-
- Gynaecological infection
- Moderate, severe Community Acquired Pneumonia (CAP)
- Moderate, severe Complicated Intra-Abdominal Infections
- Moderate, severe Complicated Skin and Soft Tissue Infection
- Moderate, severe Complicated Urinary Tract Infection
- Moderate, severe Diabetic Foot Infection
- Moderate, severe Postpartum Endomyometritis
- Moderate, severe Septic Abortion
- Contraindications & Blackbox Warnings
-
Avoid life-threatening adverse drug eventsImprove clinical decision support with information oncontraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support. - Pharmacodynamics
-
Ertapenem has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria.
- Mechanism of action
-
The bactericidal activity of ertapenem results from the inhibition of cell wall synthesis and is mediated through ertapenem binding to penicillin binding proteins (PBPs). InEscherichia coli, it has strong affinity toward PBPs 1a, 1b, 2, 3, 4 and 5 with preference for PBPs 2 and 3. Ertapenem is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases. Ertapenem is hydrolyzed by metallo-beta-lactamases.
Target Actions Organism APenicillin-binding protein 2 inhibitorHaemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd) APenicillin-binding protein 2 inhibitorEscherichia coli (strain K12) APeptidoglycan synthase FtsI inhibitorHaemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd) APeptidoglycan synthase FtsI inhibitorEscherichia coli (strain K12) AD-alanyl-D-alanine carboxypeptidase DacB inhibitorEscherichia coli (strain K12) APenicillin-binding protein 1A inhibitorEscherichia coli (strain K12) APenicillin-binding protein 1B inhibitorEscherichia coli (strain K12) AD-alanyl-D-alanine carboxypeptidase DacC inhibitorEscherichia coli (strain K12) - Absorption
-
Ertapenem is almost completely absorbed following intramuscular administration. The bioavailability of a 1 g intramuscular dose approximated 92% in 26 healthy subjects [77% male; median (range) age, 29 (22–41) years]. Plasma concentrations of total ertapenem were similar whether given intramuscularly or intravenously.
- Volume of distribution
-
- 0.12 liter/kg [adults]
- 0.2 liter/kg [pediatric, 3 months to 12 years]
- 0.16 liter/kg [pediatric patients 13 to 17 years]
- Protein binding
-
Ertapenem is highly bound to human plasma proteins, primarily albumin, in a concentration-dependent manner. The protein binding of ertapenem decreases as plasma concentrations increase. At a plasma concentration of <100 µg/mL, approximately 95% of ertapenem is protein bound. Protein binding of ertapenem decreases to approximately 85% at an approximate plasma concentration of 300 µg/mL.
- Metabolism
-
The major metabolite is the inactive ring-opened derivative formed by hydrolysis of the β-lactam ring. Ertapenem did not inhibit metabolism mediated by cytochrome P450 (CYP) isoforms 1A2, 2C9, 2C19, 2D6, 2E1, or 3A4 when evaluated by in vitro studies in human liver microsomes. Ertapenem is neither a substrate nor an inhibitor of P-glycoprotein or cytochrome P450 enzymes; significant drug interactions between ertapenem and drugs handled by these systems are not expected [PMID: 15150180]
- Route of elimination
-
Of the 80% recovered in urine, approximately 38% is excreted as unchanged drug and approximately 37% as the ring-opened metabolite.
- Half-life
-
The mean plasma half-life is approximately 4 hours.
- Clearance
-
- 1.8 L/h
- Adverse Effects
-
Improve decision support & research outcomesWith structured adverse effects data, including:blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data. - Toxicity
-
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug InteractionsLearn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
-
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Ertapenem may decrease the excretion rate of Abacavir which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Ertapenem which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Ertapenem which could result in a higher serum level. Acenocoumarol The risk or severity of bleeding can be increased when Ertapenem is combined with Acenocoumarol. Acetaminophen Ertapenem may decrease the excretion rate of Acetaminophen which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Ertapenem which could result in a lower serum level and potentially a reduction in efficacy. Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Ertapenem which could result in a higher serum level. Aclidinium Ertapenem may decrease the excretion rate of Aclidinium which could result in a higher serum level. Acrivastine Ertapenem may decrease the excretion rate of Acrivastine which could result in a higher serum level. Acyclovir Acyclovir may decrease the excretion rate of Ertapenem which could result in a higher serum level. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- No interactions found.
Products
-
Drug product information from 10+ global regionsOur datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions. - Product Ingredients
-
Ingredient UNII CAS InChI Key Ertapenem sodium 2T90KE67L0 153773-82-1 ZXNAQFZBWUNWJM-HRXMHBOMSA-M - Brand Name Prescription Products
-
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Par Pharmaceutical Inc. 2018-11-01 Not applicable US 
Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Dr Reddy's Laboratories Ltd 2021-01-27 Not applicable Canada 
Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Auro Pharma Inc 2021-10-08 Not applicable Canada Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Hikma Canada Limited Not applicable Not applicable Canada Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Juno Pharmaceuticals Corp. 2020-02-10 Not applicable Canada Ertapenem for Injection Powder, for solution 1 g / vial Intramuscular; Intravenous Fresenius Kabi 2021-06-07 Not applicable Canada Invanz Injection, powder, lyophilized, for solution 1 g/1 Intravenous Merck Sharp & Dohme Llc 2001-11-21 2018-07-31 US Invanz 注射,粉的解决方案 1 g Intravenous Merck Sharp & Dohme B.V. 2016-09-08 Not applicable EU 
Invanz Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Merck Sharp & Dohme Llc 2001-11-21 Not applicable US Invanz Powder, for solution 1 g / vial Intramuscular; Intravenous Merck Ltd. 2003-08-27 Not applicable Canada - Generic Prescription Products
-
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Fosun Pharma USA Inc 2021-11-01 Not applicable US Ertapenem Injection 1 g/20mL Intramuscular; Intravenous Apotex Corp 2019-04-02 Not applicable US Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous WG Critical Care, LLC 2020-01-07 Not applicable US Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Gland Pharma Limited 2021-03-26 Not applicable US Ertapenem Injection 1 g/20mL Intramuscular; Intravenous Savior Lifetec Corporation 2019-03-19 Not applicable US Ertapenem Injection 1 g/20mL Intramuscular; Intravenous BluePoint Laboratories 2019-08-29 Not applicable US Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Fresenius Kabi USA, LLC 2019-10-10 Not applicable US Ertapenem Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Hospira, Inc. 2020-10-19 Not applicable US Ertapenem Injection 1 g/1 Intramuscular; Intravenous AuroMedics Pharma LLC 2018-06-25 Not applicable US Ertapenem Sodium Injection, powder, lyophilized, for solution 1 g/1 Intramuscular; Intravenous Dr.Reddys Laboratories Inc., 2021-04-29 Not applicable US
Categories
- ATC Codes
- J01DH03 — Ertapenem
- Drug Categories
- Chemical TaxonomyProvided byClassyfire
-
- Description
- This compound belongs to the class of organic compounds known as thienamycins. These are beta-lactam antibiotics that differ from penicillins in having the thiazolidine sulfur atom replaced by carbon, the sulfur then becoming the first atom in the side chain.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Lactams
- Sub Class
- Beta lactams
- Direct Parent
- Thienamycins
- Alternative Parents
- Acylaminobenzoic acid and derivatives/Proline and derivatives/Alpha amino acid amides/Anilides/Benzoic acids/Pyrroline carboxylic acids/Pyrrolidinecarboxamides/Benzoyl derivatives/N-arylamides/Azepines show 16 more
- Substituents
- Acylaminobenzoic acid or derivatives/Alcohol/Alpha-amino acid amide/Alpha-amino acid or derivatives/Amine/Amino acid/Amino acid or derivatives/Anilide/Aromatic heteropolycyclic compound/Azacycle show 37 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- pyrrolidinecarboxamide, carbapenemcarboxylic acid (CHEBI:404903)
- Affected organisms
-
- Enteric bacteria and other eubacteria
Chemical Identifiers
- UNII
- G32F6EID2H
- CAS number
- 153832-46-3
- InChI Key
- JUZNIMUFDBIJCM-ANEDZVCMSA-N
- InChI
-
InChI=1S/C22H25N3O7S/c1-9-16-15(10(2)26)20(28)25(16)17(22(31)32)18(9)33-13-7-14(23-8-13)19(27)24-12-5-3-4-11(6-12)21(29)30/h3-6,9-10,13-16,23,26H,7-8H2,1-2H3,(H,24,27)(H,29,30)(H,31,32)/t9-,10-,13+,14+,15-,16-/m1/s1
- IUPAC Name
-
(4R,5S,6S)-3-{[(3S,5S)-5-[(3-carboxyphenyl)carbamoyl]pyrrolidin-3-yl]sulfanyl}-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
- SMILES
-
[H][C@]12[C@@H](C)C(S[C@]3([H])CN[C@@]([H])(C3)C(=O)NC3=CC=CC(=C3)C(O)=O)=C(N1C(=O)[C@]2([H])[C@@H](C)O)C(O)=O
References
- Synthesis Reference
-
Ying Shi, Kun Li, Zan Xie, Xuebin Zhao, Jian Lv, Xiuqin Yu, "INTERMEDIATE OF ERTAPENEM, A COMPOSITION COMPRISING THE SAME AND PREPARATION METHODS THEREOF." U.S. Patent US20120095209, issued April 19, 2012.
US20120095209 - 一般引用
- External Links
-
- Human Metabolome Database
- HMDB0014448
- KEGG Drug
- D07908
- PubChem Compound
- 150610
- PubChem Substance
- 46506508
- ChemSpider
- 132758
- 325642
- ChEBI
- 404903
- ChEMBL
- CHEMBL1359
- ZINC
- ZINC000003918453
- Therapeutic Targets Database
- DAP000431
- PharmGKB
- PA164777032
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ertapenem
- FDA label
-
Download (140 KB)
Clinical Trials
- Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
-
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Patients With Urosepis and Received Ertapenem for Treatment 1 4 Completed Not Available Acute Renal Failure (ARF) 1 4 Completed Not Available Continuous ambulatory peritoneal dialysis therapy/End Stage Renal Disease (ESRD) 1 4 Completed Not Available Healthy Subjects (HS) 1 4 Completed Not Available Infection 1 4 Completed Prevention 良性Prostatic Hyperplasia (BPH) Requiring Surgical Resection 1 4 Completed Treatment Burn Patients 1 4 Completed Treatment Complicated Intra-Abdominal Infections (cIAIs) 1 4 Completed Treatment Diverticulosis, Colonic/Neoplasms, Colonic/Rectal Neoplasms 1 4 Completed Treatment Intraabdominal Infections 1
Pharmacoeconomics
- Manufacturers
-
- Merck and co inc
- Packagers
-
- Merck & Co.
- Dosage Forms
-
Form Route Strength Injection Intramuscular; Intravenous 1 g/20mL Injection Intramuscular; Intravenous 1 g/1 Injection, powder, lyophilized, for solution Intramuscular; Intravenous 1 g/1 注射,粉的解决方案 Parenteral 注射,粉的解决方案 Intravenous 1 g/vial 注射,粉的解决方案 注射,粉的解决方案 Intravenous Injection, powder, lyophilized, for solution Intravenous drip 1 G/VIAL Injection, powder, lyophilized, for solution Intravenous 1 g Powder Not applicable 1 kg/1kg Injection, powder, lyophilized, for solution Intramuscular; Intravenous 1 g 注射,粉的解决方案 1213 mg 注射,粉的解决方案 Intravenous 1 g 注射,粉的解决方案 Intravenous; Parenteral 1 G Injection, powder, lyophilized, for solution Intravenous 1 g/1 Powder, for solution Intramuscular; Intravenous 1 g / vial Injection Intramuscular; Intravenous 注射,粉的解决方案 Intramuscular; Intravenous 1 g Injection Intramuscular; Intravenous 1 g - Prices
-
Unit description Cost Unit Invanz 1 gm add-vantage vial 72.85USD vial Invanz 1 gm vial 69.4USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only. - Patents
-
Patent Number Pediatric Extension Approved Expires (estimated) Region US5652233 No 1997-07-29 2013-02-02 US CA2106370 No 2003-11-25 2013-02-02 Canada US5478820 Yes 1995-12-26 2016-05-21 US US5952323 Yes 1999-09-14 2017-11-15 US
Properties
- State
- Solid
- Experimental Properties
-
Property Value Source water solubility Soluble as sodium salt Not Available logP 0.3 Not Available - Predicted Properties
-
Property Value Source Water Solubility 0.286 mg/mL ALOGPS logP -0.2 ALOGPS logP -3.2 ChemAxon logS -3.2 ALOGPS pKa (Strongest Acidic) 3.22 ChemAxon pKa (Strongest Basic) 9.03 ChemAxon Physiological Charge -1 ChemAxon Hydrogen Acceptor Count 8 ChemAxon Hydrogen Donor Count 5 ChemAxon Polar Surface Area 156.27 Å2 ChemAxon Rotatable Bond Count 7 ChemAxon Refractivity 121.8 m3·mol-1 ChemAxon Polarizability 48.77 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like规则 Yes ChemAxon - Predicted ADMET Features
-
Property Value Probability Human Intestinal Absorption + 0.5982 Blood Brain Barrier - 0.9811 Caco-2 permeable - 0.7052 P-glycoprotein substrate Substrate 0.7716 P-glycoprotein inhibitor I Non-inhibitor 0.917 P-glycoprotein inhibitor II Non-inhibitor 0.9955 Renal organic cation transporter Non-inhibitor 0.9253 CYP450 2C9 substrate Non-substrate 0.7891 CYP450 2D6 substrate Non-substrate 0.8229 CYP450 3A4 substrate Non-substrate 0.5 CYP450 1A2 substrate Non-inhibitor 0.8677 CYP450 2C9 inhibitor Non-inhibitor 0.867 CYP450 2D6 inhibitor Non-inhibitor 0.8964 CYP450 2C19 inhibitor Non-inhibitor 0.8511 CYP450 3A4 inhibitor Non-inhibitor 0.9658 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9695 Ames test Non AMES toxic 0.6766 Carcinogenicity Non-carcinogens 0.8052 Biodegradation Not ready biodegradable 0.9821 Rat acute toxicity 2.0803 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9947 hERG inhibition (predictor II) Non-inhibitor 0.8848
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
-
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
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- Kind
- Protein
- Organism
- Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
- Pharmacological action
-
Yes
- Actions
-
Inhibitor
- General Function
- Penicillin binding
- Specific Function
- Cell wall formation; PBP-2 is responsible for the determination of the rod shape of the cell. Its synthesize cross-linked peptidoglycan from the lipid intermediates (By similarity).
- Gene Name
- mrdA
- Uniprot ID
- P44469
- Uniprot Name
- Penicillin-binding protein 2
- 分子量
- 73812.47 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- C im P,犯罪,迈耶:药物,他们的目标and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Odenholt I: Ertapenem: a new carbapenem. Expert Opin Investig Drugs. 2001 Jun;10(6):1157-66. [Article]
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
-
Yes
- Actions
-
Inhibitor
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Cell wall formation; PBP-2 is responsible for the determination of the rod shape of the cell. It synthesizes cross-linked peptidoglycan from lipid intermediates.
- Gene Name
- mrdA
- Uniprot ID
- P0AD65
- Uniprot Name
- Penicillin-binding protein 2
- 分子量
- 70856.1 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Kind
- Protein
- Organism
- Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
- Pharmacological action
-
Yes
- Actions
-
Inhibitor
- General Function
- Peptidoglycan glycosyltransferase activity
- Specific Function
- 重要的细胞分裂所需蛋白for the synthesis of peptidoglycan at the division septum. Catalyzes the synthesis of cross-linked peptidoglycan from the lipid-linked precursors.
- Gene Name
- ftsI
- Uniprot ID
- P45059
- Uniprot Name
- Peptidoglycan synthase FtsI
- 分子量
- 67165.845 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- C im P,犯罪,迈耶:药物,他们的目标and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
-
Yes
- Actions
-
Inhibitor
- General Function
- Peptidoglycan glycosyltransferase activity
- Specific Function
- 重要的细胞分裂所需蛋白for the synthesis of peptidoglycan at the division septum (PubMed:1103132, PubMed:9614966). Catalyzes the synthesis of cross-linked peptidoglycan fr...
- Gene Name
- ftsI
- Uniprot ID
- P0AD68
- Uniprot Name
- Peptidoglycan synthase FtsI
- 分子量
- 63876.925 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
-
Yes
- Actions
-
Inhibitor
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Not involved in transpeptidation but exclusively catalyzes a DD-carboxypeptidase and DD-endopeptidase reaction.
- Gene Name
- dacB
- Uniprot ID
- P24228
- Uniprot Name
- D-alanyl-D-alanine carboxypeptidase DacB
- 分子量
- 51797.85 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
-
Yes
- Actions
-
Inhibitor
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- 细胞壁的形成。合成交联peptidoglycan from the lipid intermediates. The enzyme has a penicillin-insensitive transglycosylase N-terminal domain (formation of linear glycan str...
- Gene Name
- mrcA
- Uniprot ID
- P02918
- Uniprot Name
- Penicillin-binding protein 1A
- 分子量
- 93635.545 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
-
Yes
- Actions
-
Inhibitor
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- 细胞壁的形成。合成交联peptidoglycan from the lipid intermediates. The enzyme has a penicillin-insensitive transglycosylase N-terminal domain (formation of linear glycan str...
- Gene Name
- mrcB
- Uniprot ID
- P02919
- Uniprot Name
- Penicillin-binding protein 1B
- 分子量
- 94291.875 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
-
Yes
- Actions
-
Inhibitor
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Removes C-terminal D-alanyl residues from sugar-peptide cell wall precursors.
- Gene Name
- dacC
- Uniprot ID
- P08506
- Uniprot Name
- D-alanyl-D-alanine carboxypeptidase DacC
- 分子量
- 43608.595 Da
References
- Kohler J, Dorso KL, Young K, Hammond GG, Rosen H, Kropp H, Silver LL: In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob Agents Chemother. 1999 May;43(5):1170-6. [Article]
Drug created at June 13, 2005 13:24 / Updated at November 01, 2022 16:25