Target Information

Target General Information

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Target ID

T82349

Target Name

Bacterial Cell membrane (Bact CM)

Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 3 Target-related Diseases

Antimicrobial drug resistance [ICD-11: MG50-MG52]

Bacterial infection [ICD-11: 1A00-1C4Z]

Clostridium difficile enterocolitis [ICD-11: 1A04]

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Approved Drug(s)

[+] 4 Approved Drugs

Amoxicillin

Drug Info

Approved

Bacterial infection

[2]

Delamanid

Drug Info

Approved

Multi-drug resistant tuberculosis

[3]

Diphtheria-tetanus vaccine

Drug Info

Approved

Clostridium infection

[4]

Teicoplanin

Drug Info

Approved

Bacterial infection

[5], [6]

Clinical Trial Drug(s)

[+] 7 Clinical Trial Drugs

D2A21

Drug Info

Phase 3

Burn and burn infection

[7]

Brilacidin

Drug Info

Phase 2

Infectious disease

[8]

DPK-060

Drug Info

Phase 2

Atopic dermatitis

[9]

LTX-109

Drug Info

Phase 2

Bacterial infection

[10]

Friulimicin

Drug Info

Phase 1

Bacterial infection

[11]

IDR-1018

Drug Info

Phase 1

Bacterial infection

[12]

Lotilibcin

Drug Info

Phase 1

Bacterial infection

[13]

Discontinued Drug(s)

[+] 4 Discontinued Drugs

EREMOMYCIN

Drug Info

Discontinued in Phase 2

Bacterial infection

[14]

CB-182804

Drug Info

Discontinued in Phase 1

Bacterial infection

[15]

BMS-181184

Drug Info

Terminated

Fungal infection

[16]

Ro-25-6833

Drug Info

Terminated

Bacterial infection

[17]

Mode of Action

[+] 4 Modes of Action

Modulator

[+] 7 Modulator drugs

Amoxicillin

Drug Info

[1]

D2A21

Drug Info

[19]

LTX-109

Drug Info

[22]

Lotilibcin

Drug Info

[25]

EREMOMYCIN

Drug Info

[26]

BMS-181184

Drug Info

[28]

Ro-25-6833

Drug Info

[29]

Inhibitor

[+] 4 Inhibitor drugs

Delamanid

Drug Info

[3]

Teicoplanin

Drug Info

[5], [18]

Friulimicin

Drug Info

[23]

CB-182804

Drug Info

[27]

Enhancer

[+] 2 Enhancer drugs

Brilacidin

Drug Info

[20]

DPK-060

Drug Info

[21]

Regulator

[+] 1 Regulator drugs

IDR-1018

Drug Info

[24]

Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

References

Top

REF 1

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

REF 2

Emerging therapies for the treatment and prevention of otitis media. Expert Opin Emerg Drugs. 2006 May;11(2):251-64.

REF 3

Compassionate use of delamanid in adults and children for drug-resistant tuberculosis: 5-year update. Eur Respir J. 2021 May 20;57(5):2002483.

REF 4

2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.

REF 5

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 6

ClinicalTrials.gov (NCT00719056) Teicoplanin Prophylaxis for Total Hip or Knee Arthroplasty. U.S. National Institutes of Health.

REF 7

Antimicrobial host defence peptides: functions and clinical potential. Nat Rev Drug Discov. 2020 May;19(5):311-332.

REF 8

ClinicalTrials.gov (NCT02324335) Phase 2 Study to Evaluate the Safety & Efficacy of Brilacidin Oral Rinse in Patients With Head and Neck Cancer. U.S. National Institutes of Health.

REF 9

ClinicalTrials.gov (NCT01447017) A Study of DPK-060 to Investigate Clinical Safety and Efficacy in Patients With Acute External Otitis. U.S. National Institutes of Health.

REF 10

ClinicalTrials.gov (NCT01223222) A Study to Evaluate Safety, Tolerability and Efficacy of Lytixar (LTX-109) on Uncomplicated, Gram-positive, Skin Infection. U.S. National Institutes of Health.

REF 11

ClinicalTrials.gov (NCT00492271) First Time in Man Trial for Friulimicin B. U.S. National Institutes of Health.

REF 12

A Screening Room for Cerebral Malaria Drugs. Sci Transl Med 4, 135ra64 (2012).

REF 13

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011609)

REF 14

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002322)

REF 15

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029693)

REF 16

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005328)

REF 17

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006319)

REF 18

2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.

REF 19

In Vitro Microbicidal Activities of Cecropin Peptides D2A21 and D4E1 and Gel Formulations Containing 0.1 to 2% D2A21 against Chlamydia trachomatis. Antimicrob Agents Chemother. 2002 January; 46(1): 34-41.

REF 20

Comparative mechanistic studies of brilacidin, daptomycin, and the antimicrobial peptide LL16. Antimicrob Agents Chemother. 2014 Sep;58(9):5136-45.

REF 21

The re-emergence of natural products for drug discovery in the genomics era. Nat Rev Drug Discov. 2015 Feb;14(2):111-29.

REF 22

A synthetic antimicrobial peptidomimetic (LTX 109): stereochemical impact on membrane disruption. J Med Chem. 2011 Aug 25;54(16):5786-95.

REF 23

Model membrane approaches to determine the role of calcium for the antimicrobial activity of friulimicin. Int J Antimicrob Agents. 2011 Mar;37(3):256-60.

REF 24

Innate Defense Regulator Peptide 1018 in Wound Healing and Wound Infection. PLoS One. 2012; 7(8): e39373.

REF 25

Bioactive natural products from Lysobacter. Nat Prod Rep. 2012 November 8; 29(11): 1277-1287.

REF 26

Role of the glycopeptide framework in the antibacterial activity of hydrophobic derivatives of glycopeptide antibiotics. J Med Chem. 2003 Mar 27;46(7):1204-9.

REF 27

Activity of polymyxin B and the novel polymyxin analogue CB-182,804 against contemporary Gram-negative pathogens in New York City. Microb Drug Resist. 2012 Apr;18(2):132-6.

REF 28

Antifungal Activity of the Pradimicin Derivative BMS 181184 in the Treatment of Experimental Pulmonary Aspergillosis in Persistently Neutropenic Rabbits. Antimicrob Agents Chemother. 1998 September; 42(9): 2399-2404.

REF 29

Animal pharmacokinetics and interspecies scaling of Ro 25-6833 and related (lactamylvinyl)cephalosporins. J Pharm Sci. 1998 Apr;87(4):496-500.

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