ro 28-2653 profile

Ro 28-2653: a synthetic matrix metalloproteinase inhibitor reduces tumor growth and prolongs survival in a prostate cancer standard rat model [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	9832179
CHEMBL ID	456911
SCHEMBL ID	726759
SCHEMBL ID	8471189
MeSH ID	M0423293

Synonym
ro 28-2653
ro-28-2653
5-[4-(4-nitrophenyl)piperazin-1-yl]-5-(4-phenylphenyl)-1,3-diazinane-2,4,6-trione
CHEMBL456911 ,
bdbm50363130
SCHEMBL726759
SCHEMBL8471189
5-biphenyl-4-yl-5-[4-(4-nitro-phenyl)-piperazin-1-yl]-pyrimidine-2,4,6-trione
5-(4-biphenylyl)-5-[4-(4-nitrophenyl)piperazin-1-yl]barbituric acid
261956-22-3
5-([1,1'-biphenyl]-4-yl)-5-(4-(4-nitrophenyl)piperazin-1-yl)pyrimidine-2,4,6(1h,3h,5h)-trione
ro28-2653
EX-A2614
ro 28 2653; ro 282653; ro-28-2653; ro282653;ro28-2653
BCP30790
(2,4,6(1h,3h,5h)-pyrimidinetrione, 5-[1,1'-biphenyl]-4-yl-5-[4-(4-nitrophenyl)-1-piperazinyl]-)
A902961
AKOS040747405

Research Excerpts

Pharmacokinetics

Excerpt	Reference	Relevance
" The area under curve (AUC) and the peak serum concentration (Cmax) were approximately 10 times higher than those obtained with the suspension, while the time (Tmax) to reach Cmax was reduced."	( Pharmacokinetic study of a new synthetic MMP inhibitor (Ro 28-2653) after IV and oral administration of cyclodextrin solutions. Bertholet, P; Castagne, D; Chiap, P; Delattre, L; Evrard, B; Foidart, JM; Frankenne, F; Piel, G; Piette, M, 2006)	0.58

Compound-Compound Interactions

The proliferation rate was only inhibited by etoposide while that effect was increased in combination with Ro 28-2653 and estramustine.

Excerpt	Reference	Relevance
" Based on these results we investigated Ro 28-2653 in combination with estramustine on the G subline of the Dunning tumor."	( Matrix metalloproteinase inhibitor Ro 28-2653 in combination with estramustine: tumor-reducing effects on hormone-sensitive prostate cancer in rats. Abramjuk, C; Juchem, R; Jung, K; Krell, HW; Lein, M; Loening, SA; Peters, R; Schnorr, J; Staack, A; Stephan, C; Taymoorian, K, 2005)	0.87
" We hypothesized that the inhibitor effect of Ro 28-2653 on the tumor growth could be improved by combination with chemotherapeutic drugs and examined therefore the effect of Ro 28-2653 alone and in combination with etoposide or estramustine in the MatLyLu Dunning R-3327 rat tumor model characteristic for the androgen-independent prostate cancer (PCa)."	( Enhanced inhibitory effect of the matrix metalloproteinase inhibitor Ro 28-2653 in combination with estramustine and etoposide on the prostate carcinoma in the rat Dunning orthotopic tumor model. Abramjuk, C; Jung, K; Krell, HW; Lein, M; Loening, SA; Rothaug, W, 2007)	0.83
"The proliferation rate was only inhibited by etoposide while that effect was increased in combination with Ro 28-2653 and estramustine."	( Enhanced inhibitory effect of the matrix metalloproteinase inhibitor Ro 28-2653 in combination with estramustine and etoposide on the prostate carcinoma in the rat Dunning orthotopic tumor model. Abramjuk, C; Jung, K; Krell, HW; Lein, M; Loening, SA; Rothaug, W, 2007)	0.79

Bioavailability

Excerpt	Reference	Relevance
"Ro-28-2653, a selective and orally bioavailable MMPI with inhibitory activity against MMPs expressed by tumor and/or stromal cells, is a potent antitumor and antiangiogenic agent."	( Anti-invasive, antitumoral, and antiangiogenic efficacy of a pyrimidine-2,4,6-trione derivative, an orally active and selective matrix metalloproteinases inhibitor. Devy, L; Foidart, JM; Frankenne, F; Grams, F; Krell, HW; Maquoi, E; Noël, A; Olivier, F; Sounni, NE, 2004)	0.32
" The aim of this study is to demonstrate that an increase in Ro 28-2653 solubility, via ternary complex formation, can lead to an increase in the oral bioavailability of this drug."	( Pharmacokinetic study of a new synthetic MMP inhibitor (Ro 28-2653) after IV and oral administration of cyclodextrin solutions. Bertholet, P; Castagne, D; Chiap, P; Delattre, L; Evrard, B; Foidart, JM; Frankenne, F; Piel, G; Piette, M, 2006)	0.82

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
72 kDa type IV collagenase	Homo sapiens (human)	IC50 (µMol)	0.0230	0.0000	1.2848	10.0000	AID643325
Matrix metalloproteinase-9	Homo sapiens (human)	IC50 (µMol)	0.0070	0.0000	0.7053	10.0000	AID643327
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
angiogenesis	72 kDa type IV collagenase	Homo sapiens (human)
ovarian follicle development	72 kDa type IV collagenase	Homo sapiens (human)
ovulation from ovarian follicle	72 kDa type IV collagenase	Homo sapiens (human)
luteinization	72 kDa type IV collagenase	Homo sapiens (human)
blood vessel maturation	72 kDa type IV collagenase	Homo sapiens (human)
intramembranous ossification	72 kDa type IV collagenase	Homo sapiens (human)
proteolysis	72 kDa type IV collagenase	Homo sapiens (human)
negative regulation of cell adhesion	72 kDa type IV collagenase	Homo sapiens (human)
heart development	72 kDa type IV collagenase	Homo sapiens (human)
embryo implantation	72 kDa type IV collagenase	Homo sapiens (human)
parturition	72 kDa type IV collagenase	Homo sapiens (human)
response to xenobiotic stimulus	72 kDa type IV collagenase	Homo sapiens (human)
response to mechanical stimulus	72 kDa type IV collagenase	Homo sapiens (human)
peripheral nervous system axon regeneration	72 kDa type IV collagenase	Homo sapiens (human)
response to activity	72 kDa type IV collagenase	Homo sapiens (human)
protein metabolic process	72 kDa type IV collagenase	Homo sapiens (human)
extracellular matrix disassembly	72 kDa type IV collagenase	Homo sapiens (human)
protein catabolic process	72 kDa type IV collagenase	Homo sapiens (human)
positive regulation of cell migration	72 kDa type IV collagenase	Homo sapiens (human)
collagen catabolic process	72 kDa type IV collagenase	Homo sapiens (human)
response to retinoic acid	72 kDa type IV collagenase	Homo sapiens (human)
cellular response to reactive oxygen species	72 kDa type IV collagenase	Homo sapiens (human)
response to nicotine	72 kDa type IV collagenase	Homo sapiens (human)
endodermal cell differentiation	72 kDa type IV collagenase	Homo sapiens (human)
response to hydrogen peroxide	72 kDa type IV collagenase	Homo sapiens (human)
response to estrogen	72 kDa type IV collagenase	Homo sapiens (human)
negative regulation of vasoconstriction	72 kDa type IV collagenase	Homo sapiens (human)
ephrin receptor signaling pathway	72 kDa type IV collagenase	Homo sapiens (human)
macrophage chemotaxis	72 kDa type IV collagenase	Homo sapiens (human)
response to electrical stimulus	72 kDa type IV collagenase	Homo sapiens (human)
response to hyperoxia	72 kDa type IV collagenase	Homo sapiens (human)
face morphogenesis	72 kDa type IV collagenase	Homo sapiens (human)
bone trabecula formation	72 kDa type IV collagenase	Homo sapiens (human)
prostate gland epithelium morphogenesis	72 kDa type IV collagenase	Homo sapiens (human)
cellular response to amino acid stimulus	72 kDa type IV collagenase	Homo sapiens (human)
cellular response to interleukin-1	72 kDa type IV collagenase	Homo sapiens (human)
cellular response to estradiol stimulus	72 kDa type IV collagenase	Homo sapiens (human)
cellular response to UV-A	72 kDa type IV collagenase	Homo sapiens (human)
cellular response to fluid shear stress	72 kDa type IV collagenase	Homo sapiens (human)
positive regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathway	72 kDa type IV collagenase	Homo sapiens (human)
response to amyloid-beta	72 kDa type IV collagenase	Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation	72 kDa type IV collagenase	Homo sapiens (human)
extracellular matrix organization	72 kDa type IV collagenase	Homo sapiens (human)
response to hypoxia	72 kDa type IV collagenase	Homo sapiens (human)
tissue remodeling	72 kDa type IV collagenase	Homo sapiens (human)
skeletal system development	Matrix metalloproteinase-9	Homo sapiens (human)
positive regulation of protein phosphorylation	Matrix metalloproteinase-9	Homo sapiens (human)
proteolysis	Matrix metalloproteinase-9	Homo sapiens (human)
apoptotic process	Matrix metalloproteinase-9	Homo sapiens (human)
embryo implantation	Matrix metalloproteinase-9	Homo sapiens (human)
cell migration	Matrix metalloproteinase-9	Homo sapiens (human)
extracellular matrix disassembly	Matrix metalloproteinase-9	Homo sapiens (human)
macrophage differentiation	Matrix metalloproteinase-9	Homo sapiens (human)
collagen catabolic process	Matrix metalloproteinase-9	Homo sapiens (human)
cellular response to reactive oxygen species	Matrix metalloproteinase-9	Homo sapiens (human)
endodermal cell differentiation	Matrix metalloproteinase-9	Homo sapiens (human)
positive regulation of apoptotic process	Matrix metalloproteinase-9	Homo sapiens (human)
negative regulation of apoptotic process	Matrix metalloproteinase-9	Homo sapiens (human)
positive regulation of DNA binding	Matrix metalloproteinase-9	Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathway	Matrix metalloproteinase-9	Homo sapiens (human)
ephrin receptor signaling pathway	Matrix metalloproteinase-9	Homo sapiens (human)
positive regulation of keratinocyte migration	Matrix metalloproteinase-9	Homo sapiens (human)
cellular response to lipopolysaccharide	Matrix metalloproteinase-9	Homo sapiens (human)
cellular response to cadmium ion	Matrix metalloproteinase-9	Homo sapiens (human)
cellular response to UV-A	Matrix metalloproteinase-9	Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondria	Matrix metalloproteinase-9	Homo sapiens (human)
regulation of neuroinflammatory response	Matrix metalloproteinase-9	Homo sapiens (human)
positive regulation of receptor binding	Matrix metalloproteinase-9	Homo sapiens (human)
response to amyloid-beta	Matrix metalloproteinase-9	Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation	Matrix metalloproteinase-9	Homo sapiens (human)
negative regulation of epithelial cell differentiation involved in kidney development	Matrix metalloproteinase-9	Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway	Matrix metalloproteinase-9	Homo sapiens (human)
negative regulation of cation channel activity	Matrix metalloproteinase-9	Homo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic signaling pathway	Matrix metalloproteinase-9	Homo sapiens (human)
extracellular matrix organization	Matrix metalloproteinase-9	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
fibronectin binding	72 kDa type IV collagenase	Homo sapiens (human)
endopeptidase activity	72 kDa type IV collagenase	Homo sapiens (human)
metalloendopeptidase activity	72 kDa type IV collagenase	Homo sapiens (human)
serine-type endopeptidase activity	72 kDa type IV collagenase	Homo sapiens (human)
protein binding	72 kDa type IV collagenase	Homo sapiens (human)
metallopeptidase activity	72 kDa type IV collagenase	Homo sapiens (human)
zinc ion binding	72 kDa type IV collagenase	Homo sapiens (human)
endopeptidase activity	Matrix metalloproteinase-9	Homo sapiens (human)
metalloendopeptidase activity	Matrix metalloproteinase-9	Homo sapiens (human)
serine-type endopeptidase activity	Matrix metalloproteinase-9	Homo sapiens (human)
protein binding	Matrix metalloproteinase-9	Homo sapiens (human)
collagen binding	Matrix metalloproteinase-9	Homo sapiens (human)
peptidase activity	Matrix metalloproteinase-9	Homo sapiens (human)
metallopeptidase activity	Matrix metalloproteinase-9	Homo sapiens (human)
zinc ion binding	Matrix metalloproteinase-9	Homo sapiens (human)
identical protein binding	Matrix metalloproteinase-9	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
collagen-containing extracellular matrix	72 kDa type IV collagenase	Homo sapiens (human)
extracellular region	72 kDa type IV collagenase	Homo sapiens (human)
extracellular space	72 kDa type IV collagenase	Homo sapiens (human)
nucleus	72 kDa type IV collagenase	Homo sapiens (human)
mitochondrion	72 kDa type IV collagenase	Homo sapiens (human)
plasma membrane	72 kDa type IV collagenase	Homo sapiens (human)
sarcomere	72 kDa type IV collagenase	Homo sapiens (human)
collagen-containing extracellular matrix	72 kDa type IV collagenase	Homo sapiens (human)
extracellular space	72 kDa type IV collagenase	Homo sapiens (human)
extracellular region	Matrix metalloproteinase-9	Homo sapiens (human)
extracellular space	Matrix metalloproteinase-9	Homo sapiens (human)
collagen-containing extracellular matrix	Matrix metalloproteinase-9	Homo sapiens (human)
extracellular exosome	Matrix metalloproteinase-9	Homo sapiens (human)
tertiary granule lumen	Matrix metalloproteinase-9	Homo sapiens (human)
ficolin-1-rich granule lumen	Matrix metalloproteinase-9	Homo sapiens (human)
extracellular space	Matrix metalloproteinase-9	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID643327	Inhibition of MMP9 using (7-methoxycoumarin-4-yl)acetyl-Pro-Leu-Gly-Leu-(3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)Ala-Arg-NH2 as substrate preincubated for 30 mins measured after 10 mins by fluorescence analysis	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	A new generation of radiofluorinated pyrimidine-2,4,6-triones as MMP-targeted radiotracers for positron emission tomography.
AID396059	Antiinvasive activity in human HT1080 cells assessed as number of cells migrated at 1 uM after 24 hrs by Boyden chamber invasion assay	2008	European journal of medicinal chemistry, Dec, Volume: 43, Issue:12	6-Substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives in a new approach of the treatment of cancer cell invasion and metastasis.
AID643324	Octanol-water partition coefficient, log D of the compound at pH 7.4 by gamma counter	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	A new generation of radiofluorinated pyrimidine-2,4,6-triones as MMP-targeted radiotracers for positron emission tomography.
AID643325	Inhibition of MMP2 using (7-methoxycoumarin-4-yl)acetyl-Pro-Leu-Gly-Leu-(3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)Ala-Arg-NH2 as substrate preincubated for 30 mins measured after 10 mins by fluorescence analysis	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	A new generation of radiofluorinated pyrimidine-2,4,6-triones as MMP-targeted radiotracers for positron emission tomography.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	19 (79.17)	29.6817
2010's	5 (20.83)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	24 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
aa 861 2,3,5-trimethyl-6-(12-hydroxy-5,10-dodecadiynyl)-1,4-benzoquinone: structure given in first source. docebenone : A member of the class of benzoquinones that is p-benzoquinone in which the hydrogens are substituted by three methyl groups and a 12-hydroxydodeca-5,10-diyn-1-yl group.	2.02	1	1,4-benzoquinones; acetylenic compound; primary alcohol	EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; ferroptosis inhibitor
alachlor alachlor : An aromatic amide that is N-(2,6-diethylphenyl)acetamide substituted by a methoxymethyl group at at the nitrogen atom while one of the hydrogens of the methyl group has been replaced by a chlorine atom.	7.02	1	aromatic amide; monocarboxylic acid amide; organochlorine compound	environmental contaminant; herbicide; xenobiotic
fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.	2.01	1	nucleobase analogue; organofluorine compound	antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic
thymidine [no description available]	2.02	1	pyrimidine 2'-deoxyribonucleoside	Escherichia coli metabolite; human metabolite; metabolite; mouse metabolite
lysine Lysine: An essential amino acid. It is often added to animal feed.. lysine : A diamino acid that is caproic (hexanoic) acid bearing two amino substituents at positions 2 and 6.. L-lysine : An L-alpha-amino acid; the L-isomer of lysine.	2.03	1	aspartate family amino acid; L-alpha-amino acid zwitterion; L-alpha-amino acid; lysine; organic molecular entity; proteinogenic amino acid	algal metabolite; anticonvulsant; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite
phenylalanine Phenylalanine: An essential aromatic amino acid that is a precursor of MELANIN; DOPAMINE; noradrenalin (NOREPINEPHRINE), and THYROXINE.. L-phenylalanine : The L-enantiomer of phenylalanine.. phenylalanine : An aromatic amino acid that is alanine in which one of the methyl hydrogens is substituted by a phenyl group.	2.42	2	amino acid zwitterion; erythrose 4-phosphate/phosphoenolpyruvate family amino acid; L-alpha-amino acid; phenylalanine; proteinogenic amino acid	algal metabolite; EC 3.1.3.1 (alkaline phosphatase) inhibitor; Escherichia coli metabolite; human xenobiotic metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite
thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.	2.42	2	mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound	non-polar solvent
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	2.01	1	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
etoposide [no description available]	7.03	1	beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound	antineoplastic agent; DNA synthesis inhibitor
nitrosobis(2-oxopropyl)amine nitrosobis(2-oxopropyl)amine: structure. nitrosobis(2-oxopropyl)amine : A nitrosamine that is iminodiacetone that is substituted by a nitroso group at the N-atom. It induces pancreatic ductal adenocarcinomas in Syrian golden hamsters (other rodents are not susceptible).	2.03	1	ketone; nitrosamine	carcinogenic agent
nicotine (S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.	2.02	1	3-(1-methylpyrrolidin-2-yl)pyridine	anxiolytic drug; biomarker; immunomodulator; mitogen; neurotoxin; nicotinic acetylcholine receptor agonist; peripheral nervous system drug; phytogenic insecticide; plant metabolite; psychotropic drug; teratogenic agent; xenobiotic
estramustine Estramustine: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.. estramustine : A carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid.	2.43	2	17beta-hydroxy steroid; carbamate ester; organochlorine compound	alkylating agent; antineoplastic agent; radiation protective agent
betadex beta-Cyclodextrins: Cyclic GLUCANS consisting of seven (7) glucopyranose units linked by 1,4-glycosidic bonds.	2.03	1	cyclodextrin
prinomastat prinomastat: a diazepine-based hydroxamic acid inhibitor; matrix metalloproteinase (MMP) inhibitor; angiogenesis inhibitor;. prinomastat : A hydroxamic acid that is (3S)-N-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide in which the hydrogen attached to the thiomorpholine nitrogen has been replaced by a [4-(pyridin-4-yloxy)phenyl]sulfonyl group. It is a selective inhibitor with of matrix metalloproteinases (MMPs) 2, 3, 9, 13, and 14.	2.05	1	aromatic ether; hydroxamic acid; pyridines; sulfonamide; thiomorpholines	antineoplastic agent; EC 3.4.24.35 (gelatinase B) inhibitor; matrix metalloproteinase inhibitor
sphingosine sphing-4-enine : A sphingenine in which the C=C double bond is located at the 4-position.. sphingenine : A 2-aminooctadecene-1,3-diol having (2S,3R)-configuration.. sphingoid : Sphinganine, its homologs and stereoisomers, and the hydroxy and unsaturated derivatives of these compounds.. 2-aminooctadec-4-ene-1,3-diol : A 2-aminooctadecene-1,3-diol having its double bond at position 4.	2.02	1	sphing-4-enine	human metabolite; mouse metabolite
sphingosine 1-phosphate sphingosine 1-phosphate: RN given refers to (R-(R,S-(E)))-isomer; RN for cpd without isomeric designation not available 8/89. sphingosine 1-phosphate : A phosphosphingolipid that consists of sphingosine having a phospho group attached at position 1	2.02	1	sphingoid 1-phosphate	mouse metabolite; signalling molecule; sphingosine-1-phosphate receptor agonist; T-cell proliferation inhibitor; vasodilator agent
batimastat batimastat: structure given in first source; a synthetic matrix metalloproteinase inhibitor. batimastat : A secondary carboxamide resulting from the formal condensation of the carboxy group of (2S,3R)-5-methyl-3-{[(2S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]carbamoyl}-2-[(thiophen-2-ylsulfanyl)methyl]hexanoic acid with the amino group of hydroxylamine. It a broad-spectrum matrix metalloprotease inhibitor.	2.42	2	hydroxamic acid; L-phenylalanine derivative; organic sulfide; secondary carboxamide; thiophenes; triamide	angiogenesis inhibitor; antineoplastic agent; matrix metalloproteinase inhibitor
gw 4869 GW 4869: inhibits neutral sphingomyelinase; structure in first source	2.06	1
glycolipids [no description available]	2.02	1

Condition	Relationship Strength	Studies
Metastase [description not available]	2.04	1
Invasiveness, Neoplasm [description not available]	2.95	4
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	2.04	1
Toxoplasmosis, Animal Acquired infection of non-human animals by organisms of the genus TOXOPLASMA.	2.05	1
Carcinoma, Epidermoid [description not available]	2.05	1
Cancer of Skin [description not available]	2.05	1
Carcinoma, Squamous Cell A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)	2.05	1
Skin Neoplasms Tumors or cancer of the SKIN.	2.05	1
Cerebral Infarction, Middle Cerebral Artery [description not available]	2.06	1
Apoplexy [description not available]	2.06	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	3.42	7
Anasarca [description not available]	2.06	1
Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.	2.06	1
Infarction, Middle Cerebral Artery NECROSIS occurring in the MIDDLE CEREBRAL ARTERY distribution system which brings blood to the entire lateral aspects of each CEREBRAL HEMISPHERE. Clinical signs include impaired cognition; APHASIA; AGRAPHIA; weak and numbness in the face and arms, contralaterally or bilaterally depending on the infarction.	2.06	1
Stroke A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)	7.06	1
Neointima The new and thickened layer of scar tissue that forms on a PROSTHESIS, or as a result of vessel injury especially following ANGIOPLASTY or stent placement.	2.06	1
Constriction, Pathological [description not available]	2.06	1
Constriction, Pathologic The condition of an anatomical structure's being constricted beyond normal dimensions.	2.06	1
Hyperplasia An increase in the number of cells in a tissue or organ without tumor formation. It differs from HYPERTROPHY, which is an increase in bulk without an increase in the number of cells.	2.06	1
Vascular Diseases Pathological processes involving any of the BLOOD VESSELS in the cardiac or peripheral circulation. They include diseases of ARTERIES; VEINS; and rest of the vasculature system in the body.	2.06	1
Breast Cancer [description not available]	2.42	2
Carcinoma, Anaplastic [description not available]	2.01	1
Cancer of Colon [description not available]	2.42	2
Cancer of Liver [description not available]	2.42	2
Cancer of Lung [description not available]	2.01	1
Benign Neoplasms [description not available]	2.01	1
Cancer of Pancreas [description not available]	2.42	2
Breast Neoplasms Tumors or cancer of the human BREAST.	2.42	2
Carcinoma A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.	2.01	1
Colonic Neoplasms Tumors or cancer of the COLON.	2.42	2
Liver Neoplasms Tumors or cancer of the LIVER.	2.42	2
Lung Neoplasms Tumors or cancer of the LUNG.	2.01	1
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	2.01	1
Pancreatic Neoplasms Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).	2.42	2
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	2.01	1
Disease Exacerbation [description not available]	2.42	2
Cancer of Prostate [description not available]	3.11	5
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	3.11	5
Adenocarcinoma, Basal Cell [description not available]	2.02	1
Angiogenesis, Pathologic [description not available]	2.02	1
Adenocarcinoma A malignant epithelial tumor with a glandular organization.	2.02	1
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	2.43	2
Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).	2.02	1
Hormone-Dependent Neoplasms [description not available]	2.02	1
Cancer of Nose [description not available]	2.02	1
ALS - Amyotrophic Lateral Sclerosis [description not available]	2.43	2
Amyotrophic Lateral Sclerosis A degenerative disorder affecting upper MOTOR NEURONS in the brain and lower motor neurons in the brain stem and SPINAL CORD. Disease onset is usually after the age of 50 and the process is usually fatal within 3 to 6 years. Clinical manifestations include progressive weakness, atrophy, FASCICULATION, hyperreflexia, DYSARTHRIA, dysphagia, and eventual paralysis of respiratory function. Pathologic features include the replacement of motor neurons with fibrous ASTROCYTES and atrophy of anterior SPINAL NERVE ROOTS and corticospinal tracts. (From Adams et al., Principles of Neurology, 6th ed, pp1089-94)	2.43	2
Carcinoma, Ductal, Pancreatic [description not available]	2.03	1
Carcinoma, Pancreatic Ductal Carcinoma that arises from the PANCREATIC DUCTS. It accounts for the majority of cancers derived from the PANCREAS.	2.03	1

ro 28-2653

Description

Cross-References

Synonyms (18)

Research Excerpts

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Protein Targets (2)

Inhibition Measurements

Biological Processes (64)

Molecular Functions (10)

Ceullar Components (10)

Bioassays (4)

Research

Studies (24)

Market Indicators

Research Demand Index: 11.04

Study Types

ro 28-2653

Description

Cross-References

Synonyms (18)

Research Excerpts

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Protein Targets (2)

Inhibition Measurements

Biological Processes (64)

Molecular Functions (10)

Ceullar Components (10)

Bioassays (4)

Research

Studies (24)

Market Indicators

Research Demand Index: 11.04

Study Types

Related Drugs (19)

Related Conditions (49)