Target type: biologicalprocess
An intracellular signaling cassette in which a small monomeric GTPase of the Rac subfamily relays a signal. [GOC:bf]
Rac proteins are small GTPases that play a critical role in regulating a wide range of cellular processes, including actin cytoskeleton organization, cell migration, proliferation, and gene expression. Rac proteins cycle between an inactive GDP-bound state and an active GTP-bound state, with their activity tightly regulated by guanine nucleotide exchange factors (GEFs) that promote GTP binding and GTPase-activating proteins (GAPs) that stimulate GTP hydrolysis.
In the inactive state, Rac proteins are bound to GDP and are associated with regulatory proteins that keep them in an inactive conformation. Upon receiving an upstream signal, GEFs bind to Rac and promote the exchange of GDP for GTP. This conformational change activates Rac, allowing it to interact with downstream effector proteins that mediate its biological effects.
One of the primary downstream targets of activated Rac is the WAVE regulatory complex (WRC). Rac binds to the WRC, triggering its activation and promoting the formation of actin filaments. Actin polymerization drives a variety of cellular processes, including cell movement, adhesion, and engulfment.
In addition to regulating actin dynamics, Rac also influences other cellular processes, such as the activation of the JNK and p38 MAP kinase pathways, which regulate gene expression and cell survival. Rac also plays a role in regulating the assembly and function of focal adhesions, which are specialized structures that connect the cell to the extracellular matrix.
Rac signaling is tightly regulated to ensure proper cellular function. Dysregulation of Rac activity has been implicated in a variety of diseases, including cancer, cardiovascular disease, and inflammatory disorders. Therefore, understanding the mechanisms that govern Rac signaling is crucial for developing new therapeutic strategies to target these diseases.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Ras-related C3 botulinum toxin substrate 1 | A Ras-related C3 botulinum toxin substrate 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P63000] | Homo sapiens (human) |
| Nischarin | A nischarin that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9Y2I1] | Homo sapiens (human) |
| GTPase KRas | A GTPase KRas that is encoded in the genome of human. [PRO:DNx, UniProtKB:P01116] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| cirazoline | cirazoline: posseses agonist properties at alpha-adrenoreceptor sites; RN given refers to parent cpd | aromatic ether | |
| clonidine | clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group. Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION. | clonidine; imidazoline | |
| guanfacine | Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. | acetamides | |
| fasudil | fasudil : An isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia. fasudil: intracellular calcium antagonist; structure in first source | isoquinolines; N-sulfonyldiazepane | antihypertensive agent; calcium channel blocker; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; geroprotector; neuroprotective agent; nootropic agent; vasodilator agent |
| ketorolac | 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid : A member of the class of pyrrolizines that is 2,3-dihydro-1H-pyrrolizine which is substituted at positions 1 and 5 by carboxy and benzoyl groups, respectively. ketorolac : A racemate comprising equimolar amounts of (R)-(+)- and (S)-(-)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(-) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure. Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed) | amino acid; aromatic ketone; monocarboxylic acid; pyrrolizines; racemate | analgesic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| naphazoline | Naphazoline: An adrenergic vasoconstrictor agent used as a decongestant. | naphthalenes | |
| ondansetron | Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. | carbazoles | |
| oxymetazoline | oxymetazoline : A member of the class of phenols that is 2,4-dimethylphenol which is substituted at positions 3 and 6 by 4,5-dihydro-1H-imidazol-2-ylmethyl and tert-butyl groups, respectively. A direct-acting sympathomimetic with marked alpha-adrenergic activity, it is a vasoconstrictor that is used (generally as the hydrochloride salt) to relieve nasal congestion. Oxymetazoline: A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251) | carboxamidine; imidazolines; phenols | alpha-adrenergic agonist; nasal decongestant; sympathomimetic agent; vasoconstrictor agent |
| 4-iodoclonidine | 4-iodoclonidine: structure given in first source | ||
| moxonidine | moxonidine: structure given in first source | organohalogen compound; pyrimidines | |
| tizanidine | tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites. tizanidine: RN given refers to parent cpd; structure | benzothiadiazole; imidazoles | alpha-adrenergic agonist; muscle relaxant |
| phentolamine | phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension. Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease. | imidazoles; phenols; substituted aniline; tertiary amino compound | alpha-adrenergic antagonist; vasodilator agent |
| benzimidazole | 1H-benzimidazole : The 1H-tautomer of benzimidazole. | benzimidazole; polycyclic heteroarene | |
| bisphenol a | 4,4'-isopropylidene diphenol: stimulates proliferative responses and cytokine productions of murine spleen cells and thymus cells in vitro bisphenol : By usage, the methylenediphenols, HOC6H4CH2C6H4OH, commonly p,p-methylenediphenol, and their substitution products (generally derived from condensation of two equivalent amounts of a phenol with an aldehyde or ketone). The term also includes analogues in the the methylene (or substituted methylene) group has been replaced by a heteroatom. bisphenol A : A bisphenol that is 4,4'-methanediyldiphenol in which the methylene hydrogens are replaced by two methyl groups. | bisphenol | endocrine disruptor; environmental contaminant; xenobiotic; xenoestrogen |
| idazoxan | idazoxan : A benzodioxine that is 2,3-dihydro-1,4-benzodioxine in which one of the hydrogens at position 2 has been replaced by a 4,5-dihydro-1H-imidazol-2-yl group. Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity. | benzodioxine; imidazolines | alpha-adrenergic antagonist |
| sanguinarine chloride | |||
| rilmenidine | Rilmenidine: Oxazole derivative that acts as an agonist for ALPHA-2 ADRENERGIC RECEPTORS and IMIDAZOLINE RECEPTORS. It is used in the treatment of HYPERTENSION. | isourea | |
| efaroxan | efaroxan: RN given refers to parent cpd | 1-benzofurans | |
| chelerythrine chloride | |||
| tryptoline | tryptoline: neurotoxic factor that may be involved in development of Parkinson's disease; enzymatic prep from human brain converts tryptamine to tryptoline; RN given refers to parent cpd; structure | beta-carbolines | |
| 293b cpd | 6-cyano-4-(N-ethylsulfonyl-N-methylamino)-3-hydroxy-2,2-dimethylchromane: RN given for (trans-(+-))-isomer | 1-benzopyran | |
| 4-chloro-2-(2-imidazolin-2-ylamino)isoindoline | 4-chloro-2-(2-imidazolin-2-ylamino)isoindoline: acts as partial agonist at the postsynaptic alpha-adrenoreceptors of the rat anococcygeus muscle & as antagonist at the presynaptic alpha-adrenoreceptors of the rat vas deferens | ||
| perifosine | ammonium betaine; phospholipid | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | |
| ruboxistaurin | ruboxistaurin: inhibits protein kinase C beta; structure in first source | ||
| harmalan | harmalan: structure given in first source | harmala alkaloid | |
| n(1)-guanyl-1,7-diaminoheptane | 2-(7-aminoheptyl)guanidine : A member of the class of guanidines in which the imino hydrogen of guanidine itself has been replaced by a 7-aminoheptyl group. It is an inhibitor of deoxyhypusine synthase activity (GO:0034038). N(1)-guanyl-1,7-diaminoheptane: inhibits deoxyhypusine synthase | guanidines; primary amino compound | antineoplastic agent; EC 2.5.1.46 (deoxyhypusine synthase) inhibitor |
| bms 214662 | 7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine: a farnesyltransferase inhibitor; structure in first source BMS-214662 : A member of the class of benzodiazepines that is 2,3,4,5-tetrahydro-1H-1,4-benzodiazepine substituted by (1H-imidazol-5-yl)methyl, benzyl, (thiophen-2-yl)sulfonyl, and cyano groups at positions 1, 3R, 4 and 7, respectively. It is a potent inhibitor of farnesyltransferase (IC50 = 1.35nM) which was under clinical development for the treatment of solid tumors. | benzenes; benzodiazepine; imidazoles; nitrile; sulfonamide; thiophenes | antineoplastic agent; apoptosis inducer; EC 2.5.1.58 (protein farnesyltransferase) inhibitor |
| s 1033 | (trifluoromethyl)benzenes; imidazoles; pyridines; pyrimidines; secondary amino compound; secondary carboxamide | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor | |
| 2-(2-benzofuranyl)-2-imidazoline | 2-(2-benzofuranyl)-2-imidazoline: structure given in first source | benzofurans | |
| harmine | harmine : A harmala alkaloid in which the harman skeleton is methoxy-substituted at C-7. Harmine: Alkaloid isolated from seeds of PEGANUM HARMALA; ZYGOPHYLLACEAE. It is identical to banisterine, or telepathine, from Banisteria caapi and is one of the active ingredients of hallucinogenic drinks made in the western Amazon region from related plants. It has no therapeutic use, but (as banisterine) was hailed as a cure for postencephalitic PARKINSON DISEASE in the 1920's. | harmala alkaloid | anti-HIV agent; EC 1.4.3.4 (monoamine oxidase) inhibitor; metabolite |
| guanabenz | Guanabenz: An alpha-2 selective adrenergic agonist used as an antihypertensive agent. | dichlorobenzene | |
| manumycin | manumycin A : A polyketide with formula C31H38N2O7 initially isolated from Streptomyces parvulus as a result of a random screening program for farnesyl transferase (FTase) inhibitors. It is a natural product that exhibits anticancer and antibiotic properties. manumycin: an NSAID; RN given for (1S-(1alpha,3(2E,4E,6S*),5alpha,5(1E,3E,5E),6alpha))-isomer; a farnesyl protein transferase inhibitor; from Streptomyces parvulus; MF C31-H38-N2-O7; structure given in first source | enamide; epoxide; organic heterobicyclic compound; polyketide; secondary carboxamide; tertiary alcohol | antiatherosclerotic agent; antimicrobial agent; antineoplastic agent; apoptosis inducer; bacterial metabolite; EC 1.8.1.9 (thioredoxin reductase) inhibitor; EC 2.5.1.58 (protein farnesyltransferase) inhibitor; marine metabolite |
| tracizoline | tracizoline: RN given for (R-(R*,R*))-2,3-dihydroxybutanedionate (1:1); ligand for imidazoline receptor; structure in first source | ||
| 6-cyano-4-(n-ethylsulfonyl-n-methylamino)-3-hydroxy-2,2-dimethylchromane, (trans-(+))-isomer | |||
| cilansetron | cilansetron: structure given in first source; binds to 5-HT(3) receptors | ||
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | |||
| sotrastaurin | sotrastaurin : A member of the class of maleimides that is maleimide which is substituted at position 3 by an indol-3-yl group and at position 4 by a quinazolin-4-yl group, which in turn is substituted at position 2 by a 4-methylpiperazin-1-yl group. It is a potent and selective inhibitor of protein kinase C and has been investigated as an immunosuppresant in renal transplant patients. sotrastaurin: a potent protein kinase C-selective inhibitor; structure in first source | indoles; maleimides; N-alkylpiperazine; N-arylpiperazine; quinazolines | anticoronaviral agent; EC 2.7.11.13 (protein kinase C) inhibitor; immunosuppressive agent |
| sch 54292 | SCH 54292: structure in first source | ||
| gdc-0973 | cobimetinib : A member of the class of N-acylazetidines obtained by selective formal condensation of the carboxy group of 3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzoic acid with the secondary amino group from the azetidine ring of 3-[(2S)-piperidin-2-yl]azetidin-3-ol. An inhibitor of mitogen-activated protein kinase that is used (as its fumarate salt) in combination with vemurafenib for the treatment of patients with unresectable or metastatic melanoma. cobimetinib: has antineoplastic activity; structure in first source | aromatic amine; difluorobenzene; N-acylazetidine; organoiodine compound; piperidines; secondary amino compound; tertiary alcohol | antineoplastic agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor |
| azd5438 | sulfonamide | ||
| nsc 23766 | NSC 23766 trihydrochloride : A hydrochloride resulting from the formal reaction of NSC 23766 with 3 mol eq. of hydrogen chloride. An inhibitor of the signalling G-protein known as RAC1 (Ras-related C3 botulinum toxin substrate 1). Rac1 inhibitor : Any inhibitor of Rac1. | hydrochloride | antiviral agent; apoptosis inducer; EC 3.6.5.2 (small monomeric GTPase) inhibitor; muscarinic antagonist |
| at13148 | |||
| poziotinib | HM781-36B: antitumor irreversible Pan-HER inhibitor for treatment of gastric cancer | acrylamides; aromatic ether; dichlorobenzene; diether; monofluorobenzenes; N-acylpiperidine; quinazolines; secondary amino compound; substituted aniline | antineoplastic agent; apoptosis inducer; epidermal growth factor receptor antagonist |
| plx4032 | aromatic ketone; difluorobenzene; monochlorobenzenes; pyrrolopyridine; sulfonamide | antineoplastic agent; B-Raf inhibitor | |
| bay 869766 | |||
| dabrafenib | 1,3-thiazoles; aminopyrimidine; organofluorine compound; sulfonamide | anticoronaviral agent; antineoplastic agent; B-Raf inhibitor | |
| gilteritinib | gilteritinib : A member of the class of pyrazines that is pyrazine-2-carboxamide which is substituted by {3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}nitrilo, (oxan-4-yl)nitrilo and ethyl groups at positions 3,5 and 6, respectively. It is a potent inhibitor of FLT3 and AXL tyrosine kinase receptors (IC50 = 0.29 nM and 0.73 nM, respectively). Approved by the FDA for the treatment of acute myeloid leukemia in patients who have a FLT3 gene mutation. gilteritinib: an FLT3/AXL protein tyrosine kinase inhibitor | aromatic amine; monomethoxybenzene; N-methylpiperazine; oxanes; piperidines; primary carboxamide; pyrazines; secondary amino compound | antineoplastic agent; apoptosis inducer; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor |
| glpg0634 | |||
| bix 02565 | |||
| ly3009120 | LY3009120 : A member of the class of pyridopyrimidines that is pyrido[2,3-d]pyrimidine substituted by methylamino, 5-{[(3,3-dimethylbutyl)carbamoyl]amino}-4-fluoro-2-methylphenyl, and methyl groups at positions 2, 6 and 7, respectively. It is a potent pan RAF inhibitor which inhibits BRAF(V600E), BRAF(WT) and CRAF(WT) (IC50 = 5.8, 9.1 and 15 nM, respectively). It also inhibits RAF homo- and heterodimers and exhibits anti-cancer properties. LY3009120: a pan-RAF inhibitor; structure in first source | aminotoluene; aromatic amine; biaryl; monofluorobenzenes; phenylureas; pyridopyrimidine; secondary amino compound | antineoplastic agent; apoptosis inducer; autophagy inducer; B-Raf inhibitor; necroptosis inhibitor |
| ARS-1620 | ARS-1620 : A qinazoline derivative carrying chloro and fluoro substituents at positions 6 and 8 respectively, a 2-fluoro-6-hydroxyphenyl group at position 7, and a 4-(prop-2-enoyl)piperazin-1-yl group at position 4. A potent, selective, and orally bioavailable covalent KRAS-G12C inhibitor, it inhibits the protein coding gene KRAS (Kirsten rat sarcoma virus) with high potency in cells and animals. ARS-1620: covalent S-IIP G12C inhibitor for targeting of KRAS G12C mutant tumors | quinazolines | antineoplastic agent; antiviral agent; inhibitor |
| sotorasib | sotorasib : A pyridopyrimidine that is pyrido[2,3-d]pyrimidin-2(1H)-one substituted by 4-methyl-2-(propan-2-yl)pyridin-3-yl, (2S)-2-methyl-4-(prop-2-enoyl)piperazin-1-yl, fluoro and 2-fluoro-6-hydroxyphenyl groups at positions 1, 4, 6 and 7, respectively. It is approved for the treatment of patients with non-small cell lung cancer having KRAS(G12C) mutations. sotorasib: a KRAS(G12C) inhibitor | acrylamides; methylpyridines; monofluorobenzenes; N-acylpiperazine; phenols; pyridopyrimidine; tertiary amino compound; tertiary carboxamide | antineoplastic agent |