Identification

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Name
Patupilone
Accession Number
DB03010  (EXPT01349)
Type
Small Molecule
Groups
Experimental, Investigational
Description

Epothilone B is a 16-membered macrolide that mimics the biological effects of taxol.

Structure
Thumb
Synonyms
  • (−)-epothilone B
  • Epo B
  • Epothilone B
  • patupilona
External IDs
EPO 906 / EPO 906A / EPO-906 / EPO-906A
Categories
UNII
UEC0H0URSE
CAS number
152044-54-7
Weight
Average: 507.683
Monoisotopic: 507.265458739
Chemical Formula
C27H41NO6S
InChI Key
QXRSDHAAWVKZLJ-PVYNADRNSA-N
InChI
InChI=1S/C27H41NO6S/c1-15-9-8-10-27(7)22(34-27)12-20(16(2)11-19-14-35-18(4)28-19)33-23(30)13-21(29)26(5,6)25(32)17(3)24(15)31/h11,14-15,17,20-22,24,29,31H,8-10,12-13H2,1-7H3/b16-11+/t15-,17+,20-,21-,22-,24-,27+/m0/s1
IUPAC Name
(1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-[(1E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione
SMILES
[H]\C(=C(\C)[C@]1([H])C[C@]2([H])O[C@]2(C)CCC[C@]([H])(C)[C@]([H])(O)[C@@]([H])(C)C(=O)C(C)(C)[C@@]([H])(O)CC(=O)O1)C1=CSC(C)=N1

Pharmacology

Indication

Investigated for use/treatment in ovarian cancer, lung cancer, brain cancer, breast cancer, and gastric cancer.

Pharmacodynamics
Not Available
Mechanism of action

The principal mechanism of the epothilone class is inhibition of microtubule function. Microtubules are essential to cell division, and epothilones therefore stop cells from properly dividing. Epothilone B possess the same biological effects as taxol both in vitro and in cultured cells. This is because they share the same binding site, as well as binding affinity to the microtubule. Like taxol, epothilone B binds to the αβ-tubulin heterodimer subunit. Once bound, the rate of αβ-tubulin dissociation decreases, thus stabilizing the microtubules. Furthermore, epothilone B has also been shown to induce tubulin polymerization into microtubules without the presence of GTP. This is caused by formation of microtubule bundles throughout the cytoplasm. Finally, epothilone B also causes cell cycle arrest at the G2-M transition phase, thus leading to cytotoxicity and eventually cell apoptosis.

TargetActionsOrganism
UTubulin alpha-3C/D chainNot AvailableHumans
UTubulin beta chainNot AvailableHumans
UTubulin beta-1 chainNot AvailableHumans
UTubulin beta-4B chainNot AvailableHumans
UTubulin beta-4A chainNot AvailableHumans
UTubulin alpha-4A chainNot AvailableHumans
UTubulin beta-3 chainNot AvailableHumans
UTubulin alpha-1C chainNot AvailableHumans
UTubulin alpha-8 chainNot AvailableHumans
UTubulin alpha-1B chainNot AvailableHumans
UTubulin alpha-1A chainNot AvailableHumans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
(R)-warfarinThe serum concentration of (R)-warfarin can be increased when it is combined with Patupilone.
(S)-WarfarinThe serum concentration of (S)-Warfarin can be increased when it is combined with Patupilone.
3-isobutyl-1-methyl-7H-xanthineThe metabolism of 3-isobutyl-1-methyl-7H-xanthine can be decreased when combined with Patupilone.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Patupilone.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Patupilone.
7-DeazaguanineThe metabolism of 7-Deazaguanine can be decreased when combined with Patupilone.
7,9-DimethylguanineThe metabolism of 7,9-Dimethylguanine can be decreased when combined with Patupilone.
8-azaguanineThe metabolism of 8-azaguanine can be decreased when combined with Patupilone.
8-chlorotheophyllineThe metabolism of 8-chlorotheophylline can be decreased when combined with Patupilone.
9-aminocamptothecinThe metabolism of 9-aminocamptothecin can be decreased when combined with Patupilone.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

References

Synthesis Reference

Richard Taylor, "Derivatives of epothilone B and D and synthesis thereof." U.S. Patent US20030176473, issued September 18, 2003.

US20030176473
General References
Not Available
External Links
KEGG Compound
C12154
PubChem Compound
448013
PubChem Substance
46505629
ChemSpider
10213816
BindingDB
50103627
ChEBI
31550
ChEMBL
CHEMBL94657
Therapeutic Targets Database
DNC000616
HET
EPB
PDB Entries
1q5d / 5mlv / 6s8m

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentAdult Solid Neoplasm1
1Active Not RecruitingTreatmentMale Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer1
1CompletedTreatmentAdvanced Malignancies1
1CompletedTreatmentAdvanced Malignancies / Tumors2
1CompletedTreatmentAdvanced Malignancies / Tumors, Solid1
1CompletedTreatmentAdvanced Solid Tumors1
1CompletedTreatmentCentral Nervous System Neoplasms / Neoplasms, Head and Neck1
1CompletedTreatmentMalignant Neoplasm of Colon1
1CompletedTreatmentRefractory Malignancy1
1CompletedTreatmentTumors1
1CompletedTreatmentTumors, Solid1
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
1TerminatedTreatmentAdvanced Malignancies1
1TerminatedTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
1WithdrawnTreatmentTumors, Solid1
1, 2Active Not RecruitingTreatmentColorectal Cancers / Malignant Neoplasm of Colon1
1, 2CompletedTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
1, 2CompletedTreatmentAdult Anaplastic Astrocytoma / Adult Giant Cell Glioblastoma / Adult Gliosarcoma / Recurrent Adult Brain Tumor1
1, 2CompletedTreatmentFallopian Tube Cancer / Female Reproductive Cancer / Recurrent Breast Cancer / Recurrent Ovarian Epithelial Cancer / Stage III Ovarian Epithelial Cancer / Stage IV Breast Cancer / Stage IV Ovarian Epithelial Cancer1
1, 2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2CompletedTreatmentRecurrent Glioblastoma Planned for Reoperation1
2Active Not RecruitingTreatmentBilateral Breast Carcinoma / Cancer, Breast / HER2/Neu Negative / Invasive Breast Carcinoma1
2Active Not RecruitingTreatmentEndometrial Adenocarcinomas / Endometrial Adenosquamous Carcinoma / Endometrial Clear Cell Adenocarcinoma / Endometrial Serous Adenocarcinoma / Recurrent Uterine Corpus Carcinoma / Stage IIIA Uterine Corpus Cancer / Stage IIIA Uterine Corpus Cancer AJCC v7 / Stage IIIB Uterine Corpus Cancer / Stage IIIB Uterine Corpus Cancer AJCC v7 / Stage IIIC Uterine Corpus Cancer / Stage IIIC Uterine Corpus Cancer AJCC v7 / Stage IVA Uterine Corpus Cancer / Stage IVA Uterine Corpus Cancer AJCC v7 / Stage IVB Uterine Corpus Cancer / Stage IVB Uterine Corpus Cancer AJCC v71
2CompletedTreatmentAbdominal wall neoplasm / Fallopian Tube Neoplasms / Neoplasms, Ovarian1
2CompletedTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage IV Prostate Cancer2
2CompletedTreatmentAdult Rhabdomyosarcoma / Adult Synovial Sarcoma / Alveolar Childhood Rhabdomyosarcoma / Childhood Synovial Sarcoma / Embryonal Childhood Rhabdomyosarcoma / Previously Treated Childhood Rhabdomyosarcoma / Recurrent Adult Soft Tissue Sarcoma / Recurrent Childhood Rhabdomyosarcoma / Recurrent Childhood Soft Tissue Sarcoma / Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Recurrent Neuroblastoma / Recurrent Osteosarcoma / Recurrent Wilms Tumor and Other Childhood Kidney Tumors1
2CompletedTreatmentAnaplastic Large Cell Lymphoma / Recurrent Adult Burkitt Lymphoma / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Adult Diffuse Mixed Cell Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Mantle Cell Lymphoma1
2CompletedTreatmentBrain Metastasis / Lung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentCancer, Breast / Metastatic Cancers1
2CompletedTreatmentCarcinoids / Neuroendocrine Tumors1
2CompletedTreatmentClear Cell Renal Cell Carcinoma / Renal Cell Cancer, Recurrent / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer1
2CompletedTreatmentColonic Neoplasms / Neoplasms, Colorectal1
2CompletedTreatmentDistal Urethral Cancer / Metastatic Bladder Cancer / Metastatic Transitional Cell Cancer of the Renal Pelvis and Ureter / Proximal Urethral Cancer / Recurrent Bladder Cancer / Recurrent Transitional Cell Cancer of the Renal Pelvis and Ureter / Recurrent Urethral Cancer / Regional Transitional Cell Cancer of the Renal Pelvis and Ureter / Stage III Bladder Cancer / Transitional Cell Carcinoma of the Bladder / Urethral Cancer Associated With Invasive Bladder Cancer1
2CompletedTreatmentEndometrial Adenocarcinomas / Recurrent Endometrial Carcinoma / Stage IV Endometrial Carcinoma1
2CompletedTreatmentHepatocellular,Carcinoma1
2CompletedTreatmentHer2-Positive Breast Cancer / Male Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer1
2CompletedTreatmentHormone Refractory Prostate Cancer1
2CompletedTreatmentMelanoma1
2CompletedTreatmentMetastatic Hormone Refractory Prostate Cancer1
2CompletedTreatmentMetastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma / Recurrent Metastatic Squamous Neck Cancer With Occult Primary / Recurrent Salivary Gland Cancer / Recurrent Squamous Cell Carcinoma of the Hypopharynx / Recurrent Squamous Cell Carcinoma of the Larynx / Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity / Recurrent Squamous Cell Carcinoma of the Oropharynx / Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Recurrent Verrucous Carcinoma of the Larynx / Recurrent Verrucous Carcinoma of the Oral Cavity / Salivary Gland Squamous Cell Carcinoma / Stage IV Squamous Cell Carcinoma of the Hypopharynx / Stage IVA Salivary Gland Cancer / Stage IVA Squamous Cell Carcinoma of the Larynx / Stage IVA Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IVA Squamous Cell Carcinoma of the Oropharynx / Stage IVA Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IVA Verrucous Carcinoma of the Larynx / Stage IVA Verrucous Carcinoma of the Oral Cavity / Stage IVB Salivary Gland Cancer / Stage IVB Squamous Cell Carcinoma of the Larynx / Stage IVB Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IVB Squamous Cell Carcinoma of the Oropharynx / Stage IVB Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IVB Verrucous Carcinoma of the Larynx / Stage IVB Verrucous Carcinoma of the Oral Cavity / Stage IVC Salivary Gland Cancer / Stage IVC Squamous Cell Carcinoma of the Larynx / Stage IVC Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IVC Squamous Cell Carcinoma of the Oropharynx / Stage IVC Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IVC Verrucous Carcinoma of the Larynx / Stage IVC Verrucous Carcinoma of the Oral Cavity / Tongue Cancer1
2CompletedTreatmentNeoplasms, Breast1
2CompletedTreatmentNeoplasms, Kidney1
2CompletedTreatmentPrimary Peritoneal Cavity Cancer / Recurrent Ovarian Epithelial Cancer1
2CompletedTreatmentProstatic Neoplasms1
2CompletedTreatmentRecurrent Melanoma / Stage IV Melanoma1
2CompletedTreatmentRecurrent Uterine Corpus Sarcoma / Recurrent Uterine Sarcoma / Uterine Carcinosarcoma1
2TerminatedTreatmentAdult Primary Cholangiocellular Carcinoma / Adult Primary Hepatocellular Carcinoma / Advanced Adult Primary Liver Cancer / Cholangiocarcinoma of the Extrahepatic Bile Duct / Cholangiocarcinoma of the Gallbladder / Localized Extrahepatic Bile Duct Cancer / Localized Gallbladder Cancer / Localized Resectable Adult Primary Liver Cancer / Localized Unresectable Adult Primary Liver Cancer / Recurrent Adult Primary Liver Cancer / Recurrent Extrahepatic Bile Duct Cancer / Recurrent Gallbladder Cancer / Unresectable Extrahepatic Bile Duct Cancer / Unresectable Gallbladder Cancer1
2TerminatedTreatmentHer2-Positive Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer1
2TerminatedTreatmentRecurrent Adult Soft Tissue Sarcoma / Stage III Adult Soft Tissue Sarcoma / Stage IV Adult Soft Tissue Sarcoma1
3Active Not RecruitingTreatmentEstrogen Receptor Negative / Estrogen Receptor Positive / HER2/Neu Negative / HER2/Neu Positive / Male Breast Carcinoma / Progesterone Receptor Negative / Progesterone Receptor Positive / Recurrent Breast Carcinoma / Stage IIIC Breast Cancer AJCC v6 / Stage IV Breast Cancer / Stage IV Breast Cancer AJCC v6 and v71
3CompletedTreatmentAbdominal wall neoplasm / Cancer of the Ovary / Fallopian Tube Cancer1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00342 mg/mLALOGPS
logP3.7ALOGPS
logP4.12ChemAxon
logS-5.2ALOGPS
pKa (Strongest Acidic)14.09ChemAxon
pKa (Strongest Basic)2.73ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area109.25 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity134.76 m3·mol-1ChemAxon
Polarizability56.11 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8471
Blood Brain Barrier+0.6791
Caco-2 permeable-0.5935
P-glycoprotein substrateSubstrate0.7384
P-glycoprotein inhibitor INon-inhibitor0.8232
P-glycoprotein inhibitor IINon-inhibitor0.9779
Renal organic cation transporterNon-inhibitor0.9193
CYP450 2C9 substrateNon-substrate0.84
CYP450 2D6 substrateNon-substrate0.8309
CYP450 3A4 substrateSubstrate0.622
CYP450 1A2 substrateInhibitor0.5065
CYP450 2C9 inhibitorNon-inhibitor0.7468
CYP450 2D6 inhibitorNon-inhibitor0.9114
CYP450 2C19 inhibitorNon-inhibitor0.6114
CYP450 3A4 inhibitorNon-inhibitor0.7163
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8841
Ames testNon AMES toxic0.5816
CarcinogenicityNon-carcinogens0.933
BiodegradationReady biodegradable0.5
Rat acute toxicity2.7983 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9924
hERG inhibition (predictor II)Non-inhibitor0.935
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as epothilones and analogues. These are macrolides consisting of a 16-member lactone ring conjugated at the carbon 16 with a 1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl group. Some epothilone analogues containing a lactam ring instead of the lactone ring.
Kingdom
Organic compounds
Super Class
Phenylpropanoids and polyketides
Class
Macrolides and analogues
Sub Class
Epothilones and analogues
Direct Parent
Epothilones and analogues
Alternative Parents
2,4-disubstituted thiazoles / Heteroaromatic compounds / Secondary alcohols / Lactones / Cyclic ketones / Carboxylic acid esters / Oxacyclic compounds / Monocarboxylic acids and derivatives / Epoxides / Dialkyl ethers
show 5 more
Substituents
Epothilone / 2,4-disubstituted 1,3-thiazole / Azole / Heteroaromatic compound / Thiazole / Carboxylic acid ester / Ketone / Lactone / Secondary alcohol / Cyclic ketone
show 18 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
1,3-thiazole, oxabicycloalkane (CHEBI:42432) / Macrolides and lactone polyketides (C12154) / Macrolides and lactone polyketides (LMPK04000041)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Structural constituent of cytoskeleton
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Gene Name
TUBA3C
Uniprot ID
Q13748
Uniprot Name
Tubulin alpha-3C/D chain
Molecular Weight
49959.145 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Ubiquitin protein ligase binding
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Gene Name
TUBB
Uniprot ID
P07437
Uniprot Name
Tubulin beta chain
Molecular Weight
49670.515 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Structural constituent of cytoskeleton
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain (By similarity).
Gene Name
TUBB1
Uniprot ID
Q9H4B7
Uniprot Name
Tubulin beta-1 chain
Molecular Weight
50326.56 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Unfolded protein binding
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Gene Name
TUBB4B
Uniprot ID
P68371
Uniprot Name
Tubulin beta-4B chain
Molecular Weight
49830.72 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Structural constituent of cytoskeleton
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Gene Name
TUBB4A
Uniprot ID
P04350
Uniprot Name
Tubulin beta-4A chain
Molecular Weight
49585.475 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Structural constituent of cytoskeleton
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Gene Name
TUBA4A
Uniprot ID
P68366
Uniprot Name
Tubulin alpha-4A chain
Molecular Weight
49923.995 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Structural constituent of cytoskeleton
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain. TUBB3 plays a criti...
Gene Name
TUBB3
Uniprot ID
Q13509
Uniprot Name
Tubulin beta-3 chain
Molecular Weight
50432.355 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Structural molecule activity
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Gene Name
TUBA1C
Uniprot ID
Q9BQE3
Uniprot Name
Tubulin alpha-1C chain
Molecular Weight
49894.93 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Specific Function
Gtp binding
Gene Name
TUBA8
Uniprot ID
Q9NY65
Uniprot Name
Tubulin alpha-8 chain
Molecular Weight
50093.12 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Ubiquitin protein ligase binding
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Gene Name
TUBA1B
Uniprot ID
P68363
Uniprot Name
Tubulin alpha-1B chain
Molecular Weight
50151.24 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Specific Function
Gtp binding
Gene Name
TUBA1A
Uniprot ID
Q71U36
Uniprot Name
Tubulin alpha-1A chain
Molecular Weight
50135.25 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Kuper JI, D'Aprile M: Drug-Drug interactions of clinical significance in the treatment of patients with Mycobacterium avium complex disease. Clin Pharmacokinet. 2000 Sep;39(3):203-14. [PubMed:11020135]

Drug created on June 13, 2005 07:24 / Updated on November 02, 2019 01:21