Target Information

Target General Information

Top

Target ID

T72657 (Former ID: TTDS00219)

Target Name

Staphylococcus 30S ribosomal subunit (Stap-coc pbp2)

Synonyms

Penicillin-binding protein 2; Penicillin-binding protein; Penicillin binding protein PBP 2

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Gene Name

Stap-coc pbp2

Target Type

Successful target

[1]

Disease

[+] 8 Target-related Diseases

Acne vulgaris [ICD-11: ED80]

Acute/subacute hepatic failure [ICD-11: DB91]

Alcoholic liver disease [ICD-11: DB94]

Amoebiasis [ICD-11: 1A36]

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

Bronchitis [ICD-11: CA20]

Lyme borreliosis [ICD-11: 1C1G]

Skin and skin-structure infection [ICD-11: 1F28-1G0Z]

Function

Subunite of bacterial 70s ribosomes. Invovled in protein biosynthesis.

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UniProt ID

F4NA87_STAAU

Sequence

MTENKGSSQPKKNGNNGGKSNSKKNRNVKRTIIKIIGFMIIAFFVVLLLGILLFAYYAWK
APAFTEAKLQDPIPAKIYDKNGELVKTLDNGQRHEHVNLKDVPKSMKDAVLATEDNRFYE
HGALDYKRLFGAIGKNLTGGFGSEGASTLTQQVVKDAFLSQHKSIGRKAQEAYLSYRLEQ
EYSKDDIFQVYLNKIYYSDGVTGIKAAAKYYFNKDLKDLNLAEEAYLAGLPQVPNNYNIY
DHPKAAEDRKNTVLYLMHYHKRITDKQWEDAKKIDLKANLVNRTAEERQNIDTNQDSEYN
SYVNFVKSELMNNKAFKDENLGNVLQSGIKIYTNMDKDVQKTLQNDVDNGSFYKNKDQQV
GATILDSKTGGLVAISGGRDFKDVVNRNQATDPHPTGSSLKPFLAYGPAIENMKWATNHA
IQDESSYQVDGSTFRNYDVKSHGTVSIYDALRQSFNIPALKAWQSVKQNAGNDAPKKFAA
KLGLNYEGDIGPSEVLGGSASEFSPTQLASAFAAIANGGTYNNAHSIQKVVTRDGETIEY
DHTSHKAMSDYTAYMLAEMLKGTFKPYGSAYGHGVSGVNMGAKTGTGTYGAETYSQYNLP
DNAAKDVWINGFTPQYTMSVWMGFSKVKQYGENSFVGHSQQEYPQFLYENVMSKISSRDG
EDFKRPSSVSGSIPSINVSGSQDNNTTNRSTHGGSDTSANSSGTAQSNNNTRSQQSRNSG
GLTGIFN

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Drugs and Modes of Action

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Approved Drug(s)

[+] 15 Approved Drugs

Clomocycline

Drug Info

Approved

Bacterial infection

[4]

Demeclocycline

Drug Info

Approved

Bronchitis

[5]

Framycetin

Drug Info

Approved

Alcoholic cirrhosis of liver

[6], [7]

Lymecycline

Drug Info

Approved

Bacterial infection

[8]

Meclocycline

Drug Info

Approved

Bacterial infection

[9]

Methacycline

Drug Info

Approved

Bacterial infection

[10]

Minocycline

Drug Info

Approved

Bacterial infection

[11]

Netilmicin

Drug Info

Approved

Bacterial infection

[12]

Oxytetracycline

Drug Info

Approved

Bacterial infection

[13]

Paromomycin

Drug Info

Approved

Intestinal amebiasis

[14]

Rolitetracycline

Drug Info

Approved

Acne vulgaris

[5], [15]

Spectinomycin

Drug Info

Approved

Bacterial infection

[16]

Streptomycin

Drug Info

Approved

Bacterial infection

[17]

Tetracycline

Drug Info

Approved

Bacterial infection

[18]

Tigecycline

Drug Info

Approved

Skin infection

[19], [20], [21]

Mode of Action

[+] 1 Modes of Action

Binder

[+] 15 Binder drugs

Clomocycline

Drug Info

[4]

Demeclocycline

Drug Info

[22]

Framycetin

Drug Info

[23], [24]

Lymecycline

Drug Info

[25]

Meclocycline

Drug Info

[22]

Methacycline

Drug Info

[26]

Minocycline

Drug Info

[27]

Netilmicin

Drug Info

[28]

Oxytetracycline

Drug Info

[22]

Paromomycin

Drug Info

[29], [30]

Rolitetracycline

Drug Info

[15]

Spectinomycin

Drug Info

[31]

Streptomycin

Drug Info

[31], [32]

Tetracycline

Drug Info

[33]

Tigecycline

Drug Info

[19]

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Similarity Proteins

Different Human System Profiles of Target

Top

Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Similarity Proteins

There is no similarity protein (E value < 0.005) for this target

Drug Property Profile of Target

Top

(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

Co-Targets

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Co-Targets

Co-Targets Info

Target Profiles in Patients

Top

Drug Resistance
Mutation (DRM)

Drug Resistance Mutation Info

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

REF 1

Bacterial resistance to aminoglycosides and beta-lactams: the Tn1331 transposon paradigm. Front Biosci. 2000 Jan 1;5:D20-9.

REF 2

Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98.

REF 3

Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8.

REF 4

Molecular dynamics simulations of the 30S ribosomal subunit reveal a preferred tetracycline binding site. J Am Chem Soc. 2008 Jan 30;130(4):1114-5.

REF 5

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

REF 6

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 709).

REF 7

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 060304.

REF 8

Drug information of Lymecycline, 2008. eduDrugs.

REF 9

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 065094.

REF 10

Drug information of Methacycline, 2008. eduDrugs.

REF 11

Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.

REF 12

Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.

REF 13

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 060634.

REF 14

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 064171.

REF 15

Reversed-phase high-performance liquid chromatography coupled to ultraviolet and electrospray time-of-flight mass spectrometry on-line detection fo... J Chromatogr A. 2008 Jun 27;1195(1-2):107-16.

REF 16

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050347.

REF 17

Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22.

REF 18

How many modes of action should an antibiotic have Curr Opin Pharmacol. 2008 Oct;8(5):564-73.

REF 19

Tigecycline: first of a new class of antimicrobial agents. Pharmacotherapy. 2006 Aug;26(8):1099-110.

REF 20

2005 approvals: Safety first. Nature Reviews Drug Discovery 5, 92-93 (February 2006).

REF 21

Tigecycline (Tygacil): the first in the glycylcycline class of antibiotics. Proc (Bayl Univ Med Cent). 2006 Apr;19(2):155-61.

REF 22

Detection of tetracycline resistance genes by PCR methods. Methods Mol Biol. 2004;268:3-13.

REF 23

Characterization of a 30S ribosomal subunit assembly intermediate found in Escherichia coli cells growing with neomycin or paromomycin. Arch Microbiol. 2008 May;189(5):441-9.

REF 24

Antistaphylococcal activity of gentamicin. Minerva Med. 1975 Dec 8;66(84):4505-26.

REF 25

Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.

REF 26

Tetracyclines and pulmonary inflammation. Endocr Metab Immune Disord Drug Targets. 2007 Dec;7(4):232-6.

REF 27

Functional, biophysical, and structural bases for antibacterial activity of tigecycline. Antimicrob Agents Chemother. 2006 Jun;50(6):2156-66.

REF 28

Ribosomal resistance in the gentamicin producer organism Micromonospora purpurea. Antimicrob Agents Chemother. 1982 Aug;22(2):231-6.

REF 29

Aminoglycoside association pathways with the 30S ribosomal subunit. J Phys Chem B. 2009 May 21;113(20):7322-30.

REF 30

30S ribosomal subunit assembly is a target for inhibition by aminoglycosides in Escherichia coli. Antimicrob Agents Chemother. 2002 May;46(5):1546-9.

REF 31

Functional insights from the structure of the 30S ribosomal subunit and its interactions with antibiotics. Nature. 2000 Sep 21;407(6802):340-8.

REF 32

The interaction between streptomycin and ribosomal RNA. Biochimie. 1991 Dec;73(12):1431-8.

REF 33

The glycylcyclines: a comparative review with the tetracyclines. Drugs. 2004;64(1):63-88.

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