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Drug-Target Interaction

Drug

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PubChem ID:60937
Structure:
Synonyms:
(((p-Chlorophenyl)thio)methylene)diphosphonic acid
149845-07-8
149845-07-8 (disodium)
89987-06-4
96538-83-9
AC1L1U70
AC1Q3OOE
Acide tiludronique
Acide tiludronique [INN-French]
Acido tiludronico
Acido tiludronico [INN-Spanish]
Acidum tiludronicum
Acidum tiludronicum [INN-Latin]
acpmd
BIDD:GT0814
C08141
CHEMBL1350
D08599
DB01133
LS-183988
SR 41319
SR-41319
Tiludronate
Tiludronate disodium
Tiludronic acid
Tiludronic acid (INN)
Tiludronic Acid Disodium Salt
Tiludronic acid [BAN:INN]
Tiludronic acid [INN:BAN]
UNII-6PNS59HP4Y
[(4-chlorophenyl)sulfanyl-phosphonomethyl]phosphonic acid
ATC-Codes:
Side-Effects:
Side-EffectFrequency
headache0
nausea0
tooth disorder0
hyperparathyroidism0
pain0
peripheral edema0
vomiting0
bronchitis0
diarrhea0
vertigo0
chest pain0
anxiety0
syncope0
flushing0
infection0
somnolence0
paresthesia0
upper respiratory tract infection0
anorexia0
arthralgia0
cataract0
arthrosis0
conjunctivitis0
dyspepsia0
insomnia0
increased sweating0
flatulence0
cough0
vitamin d deficiency0
sinusitis0
rhinitis0
constipation0
back pain0
pathological fracture0
rash0
hypertension0
nervousness0
urinary tract infection0
glaucoma0
fatigue0
pharyngitis0
dry mouth0
abdominal pain0
asthenia0
influenza0
pruritus0
dizziness0
edema0
gastritis0

Target

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Uniprot ID:B8LXH5_TALSN
Synonyms:
Protein kinase c
EC-Numbers:2.7.11.13
Organism:Penicillium stipitatum
strain ATCC 10500 / CBS 375.48 / QM 6759 / NRRL 1006
Talaromyces stipitatus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

15922088
Tiludronate inhibits prostaglandin F2alpha-induced vascular endothelial growth factor synthesis in osteoblasts.. Minoru Yoshida; Haruhiko Tokuda; Akira Ishisaki; Yosuke Kanno; Atsushi Harada; Katsuji Shimuzu; Osamu Kozawa (2005) Molecular and cellular endocrinology display abstract
We have previously reported that prostaglandin F2alpha (PGF2alpha) activates p44/p42 mitogen-activated protein (MAP) kinase through protein kinase C (PKC), resulting in the synthesis of vascular endothelial growth factor (VEGF) in osteoblast-like MC3T3-E1 cells, and that incadronate, a bisphosphonate, amplifies the VEGF synthesis. In the present study, we investigated the effects of tiludronate and etidronate, other bisphosphonates, on the PGF2alpha-stimulated VEGF synthesis in these cells. Tiludronate reduced the synthesis of VEGF induced by PGF2alpha. The PGF(2alpha)-stimulated phosphorylation of p44/p42 MAP kinase was suppressed by tiludronate. On the other hand, etidronate affected neither the VEGF synthesis nor the phosphorylation of p44/p42 MAP kinase elicited by PGF2alpha. Tiludronate attenuated the phosphorylation of both Raf-1 and MEK1/2 induced by PGF2alpha. The VEGF synthesis stimulated by 12-O-tetradecanoylphorbol-13-acetate (TPA), a direct activator of PKC, was suppressed by tiludronate. The TPA-induced phosphorylations of Raf-1, MEK1/2 and p44/p42 MAP kinase were inhibited by tiludronate. These results strongly suggest that tiludronate but not etidronate suppresses the PGF2alpha-stimulated VEGF synthesis in osteoblasts, and that the effect of tiludronate is exerted at the point between PKC and Raf-1.