PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 20405922-4 2010 This article will detail the structure-activity relationships (SAR) leading to a novel second generation series of highly potent spirocyclic hydantoin antagonists of LFA-1. Hydantoins 141-150 integrin subunit alpha L Homo sapiens 166-171 20573163-10 2010 Also discussed here are the formaldehyde-releasers MDM hydantoin, methenamine, N-methylolchloracetamide, paraformaldehyde, and Preventol D2. Hydantoins 55-64 secreted LY6/PLAUR domain containing 1 Homo sapiens 51-54 20014751-11 2010 These results, when coupled with the known diastereomeric preference for excision of hydantoin lesions by the hNEIL1 enzyme, show the importance of defining both levels of lesion formation and diastereomeric preference of formation with regard to their potential impact on chromate carcinogenesis. Hydantoins 85-94 nei like DNA glycosylase 1 Homo sapiens 110-116 20172725-1 2010 We disclose inhibitors of TNF-alpha converting enzyme (TACE) designed around a hydantoin zinc binding moiety. Hydantoins 79-88 ADAM metallopeptidase domain 17 Homo sapiens 26-53 20172725-1 2010 We disclose inhibitors of TNF-alpha converting enzyme (TACE) designed around a hydantoin zinc binding moiety. Hydantoins 79-88 ADAM metallopeptidase domain 17 Homo sapiens 55-59 20172725-2 2010 Crystal structures of inhibitors bound to TACE revealed monodentate coordination of the hydantoin to the zinc. Hydantoins 88-97 ADAM metallopeptidase domain 17 Homo sapiens 42-46 20172725-4 2010 To our knowledge, these are the first reported X-ray structures of TACE with a hydantoin zinc ligand. Hydantoins 79-88 ADAM metallopeptidase domain 17 Homo sapiens 67-71 20099873-0 2010 Mutation versus repair: NEIL1 removal of hydantoin lesions in single-stranded, bulge, bubble, and duplex DNA contexts. Hydantoins 41-50 nei like DNA glycosylase 1 Homo sapiens 24-29 20182585-10 2010 Both hydantoins lowered beta-catenin, as reported previously. Hydantoins 5-15 catenin beta 1 Homo sapiens 24-36 17188861-5 2007 The preceding paper described a novel series of potent and TACE-selective hydantoins and we previously described pyrimidinetrione (barbiturate) inhibitors of TACE, both of which contain the same P1" group as IK682. Hydantoins 74-84 ADAM metallopeptidase domain 17 Homo sapiens 59-63 19556138-0 2009 Anti-tumor and anti-angiogenic activity of novel hydantoin derivatives: Inhibition of VEGF secretion in liver metastatic osteosarcoma cells. Hydantoins 49-58 vascular endothelial growth factor A Mus musculus 86-90 18543945-3 2008 In order to provide insight into the role of repair, the excision efficiency by hNEIL1 of these hydantoin lesions relative to other known substrates was determined. Hydantoins 96-105 nei like DNA glycosylase 1 Homo sapiens 80-86 18543945-4 2008 Most notably, quantitative examination of the substrate specificity with hNEIL1 revealed that the hydantoin lesions are excised much more efficiently (>100-fold faster) than the reported standard substrates thymine glycol (Tg) and 5-hydroxycytosine (5-OHC). Hydantoins 98-107 nei like DNA glycosylase 1 Homo sapiens 73-79 19597814-3 2009 The reaction proceeds via a three-step pathway: (a) the ring-opening cleavage of the hydantoin ring by a D-: hydantoinase (encoded by hyuH), (b) conversion of the resultant D-: N-carbamylamino acid to the corresponding amino acid by a D-: N-carbamoylase (encoded by hyuC), and (c) chemical or enzymatic racemization of the un-reacted hydantoin substrate. Hydantoins 85-94 AWN88_RS03840 Agrobacterium tumefaciens 109-121 18607541-4 2009 From the SAR studies, it reveals that, the substitution at N-terminal in hydantoin ring plays key role in the antiproliferative activity. Hydantoins 73-82 sarcosine dehydrogenase Homo sapiens 9-12 18543945-0 2008 Superior removal of hydantoin lesions relative to other oxidized bases by the human DNA glycosylase hNEIL1. Hydantoins 20-29 nei like DNA glycosylase 1 Homo sapiens 100-106 18543945-2 2008 Of these, the hydantoin lesions, guanidinohydantoin (Gh) and the two diastereomers of spiroiminodihydantoin (Sp1 and Sp2), have garnered much recent attention due to their unusual structures, high mutagenic potential, and detection in cells. Hydantoins 14-23 Sp2 transcription factor Homo sapiens 117-120 18270691-4 2008 The fifth SARM is a muscle-tissue specific agonist with a bicyclic hydantoin structure (BMS-564929). Hydantoins 67-76 sterile alpha and TIR motif containing 1 Homo sapiens 10-14 17368021-0 2007 Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). Hydantoins 0-10 ADAM metallopeptidase domain 17 Homo sapiens 85-130 17368021-0 2007 Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). Hydantoins 0-10 ADAM metallopeptidase domain 17 Homo sapiens 132-136 17368021-1 2007 We have discovered selective and potent inhibitors of TACE that replace the common hydroxamate zinc binding group with a hydantoin, triazolone, and imidazolone heterocycle. Hydantoins 121-130 ADAM metallopeptidase domain 17 Homo sapiens 54-58 17368021-2 2007 These novel heterocyclic inhibitors of a zinc metalloprotease were designed using a pharmacophore model that we previously described while developing hydantoin and pyrimidinetrione (barbiturate) inhibitors of TACE. Hydantoins 150-159 ADAM metallopeptidase domain 17 Homo sapiens 209-213 17368021-3 2007 The potency and binding orientation of these inhibitors is discussed and they are modeled into the X-ray crystal structure of TACE and compared to hydroxamate and earlier hydantoin TACE inhibitors which share the same 4-[(2-methyl-4-quinolinyl)methoxy]benzoyl P1" group. Hydantoins 171-180 ADAM metallopeptidase domain 17 Homo sapiens 181-185 17188863-1 2007 A series of novel hydantoins was designed and synthesized as structural alternatives to hydroxamate inhibitors of TACE. Hydantoins 18-28 ADAM metallopeptidase domain 17 Homo sapiens 114-118 17188863-0 2007 Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). Hydantoins 19-29 ADAM metallopeptidase domain 17 Homo sapiens 73-118 17188863-0 2007 Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). Hydantoins 19-29 ADAM metallopeptidase domain 17 Homo sapiens 120-124 16959487-0 2006 Synthesis and SAR of novel hydantoin derivatives as selective androgen receptor modulators. Hydantoins 27-36 sarcosine dehydrogenase Homo sapiens 14-17 17125246-2 2006 This letter describes the discovery and preliminary SAR of spirocyclic hydantoin based LFA-1 antagonists that culminated in the identification of analog 8 as a clinical candidate. Hydantoins 71-80 integrin subunit alpha L Homo sapiens 87-92 15686933-0 2005 De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold. Hydantoins 94-103 integrin subunit alpha L Homo sapiens 52-57 17003340-1 2006 Previously studied inhibitors of aldose reductase were largely from two chemical classes, spirosuccinamide/hydantoins and carboxylic acids. Hydantoins 107-117 aldo-keto reductase family 1 member B Homo sapiens 33-49 16190759-0 2005 A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners. Hydantoins 43-52 aldo-keto reductase family 1 member B1 Rattus norvegicus 67-83 16190759-1 2005 Discovery of a highly selective, potent, and safe non-carboxylic acid, non-hydantoin inhibitor of aldose reductase (AR) capable of potently blocking the excess glucose flux through the polyol pathway that prevails under diabetic conditions has been a long-standing challenge. Hydantoins 75-84 aldo-keto reductase family 1 member B1 Rattus norvegicus 98-114 16190759-1 2005 Discovery of a highly selective, potent, and safe non-carboxylic acid, non-hydantoin inhibitor of aldose reductase (AR) capable of potently blocking the excess glucose flux through the polyol pathway that prevails under diabetic conditions has been a long-standing challenge. Hydantoins 75-84 aldo-keto reductase family 1 member B1 Rattus norvegicus 116-118 15686933-4 2005 This paper describes the de novo design, synthesis and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold. Hydantoins 118-127 integrin subunit alpha L Homo sapiens 76-81 15288804-0 2004 Active-site characteristics of CYP2C19 and CYP2C9 probed with hydantoin and barbiturate inhibitors. Hydantoins 62-71 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 31-38 15288804-0 2004 Active-site characteristics of CYP2C19 and CYP2C9 probed with hydantoin and barbiturate inhibitors. Hydantoins 62-71 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 43-49 12504329-2 2003 Binding of hydantoins to the I domain of LFA-1 is observed by size exclusion chromatography/mass spectrometry (SEC/MS) and by direct electrospray ionization mass spectrometry (ESI/MS). Hydantoins 11-21 integrin subunit alpha L Homo sapiens 41-46 12773033-0 2003 A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one. Hydantoins 24-33 aldo-keto reductase family 1 member B1 Rattus norvegicus 68-84 12773033-1 2003 We report here on the discovery path that led to a structurally unprecedented non-hydantoin, non-carboxylic acid aldose reductase inhibitor, 24, which shows remarkably potent oral activity in normalizing elevated sorbitol levels and, more significantly, fructose levels in the sciatic nerve of chronically diabetic rats, with ED(90) values of 0.8 and 3 mpk, respectively. Hydantoins 82-91 aldo-keto reductase family 1 member B1 Rattus norvegicus 113-129 15181632-3 2004 More basic conditions were required to form the bis-protected t-Boc hydantoin with the same reagent. Hydantoins 68-77 BOC cell adhesion associated, oncogene regulated Homo sapiens 64-67 15039302-3 2004 The aim of this study was to determine the structure-activity relationships for hPXR-mediated transactivation by barbiturates, hydantoins, and macrolide antibiotics. Hydantoins 127-137 nuclear receptor subfamily 1 group I member 2 Homo sapiens 80-84 15039302-8 2004 In the case of hydantoins, only mephenytoin and ethotoin, which have an alkylchain at the R1-position, strongly activated hPXR at 300 microM. Hydantoins 15-25 nuclear receptor subfamily 1 group I member 2 Homo sapiens 122-126 15039302-10 2004 These results suggest that the presence of an alkyl-chain at the R1-position and the presence of bulky and hydrophobic moieties at both R2- and R3-positions are important factors for activation of hPXR by hydantoins. Hydantoins 205-215 nuclear receptor subfamily 1 group I member 2 Homo sapiens 197-201 12504329-3 2003 A photoactive hydantoin analog specifically labels an amino acid residue of LFA-1 I domain. Hydantoins 14-23 integrin subunit alpha L Homo sapiens 76-81 12504329-6 2003 The results demonstrate specific, stoichiometric, reversible binding of the hydantoins to LFA-1. Hydantoins 76-86 integrin subunit alpha L Homo sapiens 90-95 11720851-0 2001 Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection. Hydantoins 47-57 C-C motif chemokine receptor 5 Homo sapiens 19-23 11720851-1 2001 A series of hydantoin derivatives has been discovered as highly potent nonpeptide antagonists for the human CCR5 receptor. Hydantoins 12-21 C-C motif chemokine receptor 5 Homo sapiens 108-112 11720852-1 2001 Replacement of the large hydantoin-indole moiety from our previous work with a variety of smaller heterocyclic analogues gave rise to potent CCR5 antagonists having binding affinity comparable to the hydantoin analogues. Hydantoins 25-34 C-C motif chemokine receptor 5 Homo sapiens 141-145 8825077-1 1995 A lower microsomal epoxide hydrolase (mEH) activity has been associated with increased likelihood of fetal hydantoin syndrome. Hydantoins 107-116 epoxide hydrolase 1, microsomal Mus musculus 8-36 11403595-0 2001 Binding site elucidation of hydantoin-based antagonists of LFA-1 using multidisciplinary technologies: evidence for the allosteric inhibition of a protein--protein interaction. Hydantoins 28-37 integrin subunit alpha L Homo sapiens 59-64 11403595-1 2001 The binding site on the lymphocyte function-associated antigen-1 (LFA-1) of a class of hydantoin-based antagonists of leukocyte cell adhesion has been identified. Hydantoins 87-96 integrin subunit alpha L Homo sapiens 24-64 11403595-1 2001 The binding site on the lymphocyte function-associated antigen-1 (LFA-1) of a class of hydantoin-based antagonists of leukocyte cell adhesion has been identified. Hydantoins 87-96 integrin subunit alpha L Homo sapiens 66-71 11312916-0 2001 Discovery of an orally active non-peptide fibrinogen receptor antagonist based on the hydantoin scaffold. Hydantoins 86-95 fibrinogen beta chain Homo sapiens 42-52 8767112-2 1996 It has been shown that the investigated derivatives are recognized by 5-HT1A and 5-HT2A receptors due to the presence of a 1-arylpiperazine fragment however, the terminal hydantoin moiety plays an important role in stabilization of the receptor-ligand complex. Hydantoins 171-180 5-hydroxytryptamine receptor 1A Homo sapiens 70-82 8767112-2 1996 It has been shown that the investigated derivatives are recognized by 5-HT1A and 5-HT2A receptors due to the presence of a 1-arylpiperazine fragment however, the terminal hydantoin moiety plays an important role in stabilization of the receptor-ligand complex. Hydantoins 171-180 5-hydroxytryptamine receptor 2A Homo sapiens 83-87 11693932-3 2001 Hydantoinase and N-carbamoylamino acid amidohydrolase (NCAAH) activities are induced when cells are grown in the presence of hydantoin or an hydantoin analogue, and in complete medium, enzyme activity can be detected only in early stationary growth phase. Hydantoins 125-134 AWN88_RS03840 Agrobacterium tumefaciens 0-12 11693932-3 2001 Hydantoinase and N-carbamoylamino acid amidohydrolase (NCAAH) activities are induced when cells are grown in the presence of hydantoin or an hydantoin analogue, and in complete medium, enzyme activity can be detected only in early stationary growth phase. Hydantoins 141-150 AWN88_RS03840 Agrobacterium tumefaciens 0-12 11300910-2 2001 The rate-surfactant profiles for the HO(-)- and AcO(-)-catalyzed ring closure of two ethyl hydantoates, E2 and E3, to hydantoins with three cetyltrimethylammonium salts (CTAX, X = Br(-), Cl(-), or AcO(-)) are measured in 0.02 and 0.2 M acetate buffers 50% base with starting pH 4.65. Hydantoins 118-128 cystatin 12, pseudogene Homo sapiens 104-113 10328974-6 1999 Aldose reductase inhibitors possessing either hydantoin or carboxylic acid groups prevented protein modification induced by naphthalene-1, 2-dihydrodiol but not protein modification induced by 1, 2-dihydroxynaphthalene or 1,2-naphthoquinone. Hydantoins 46-55 aldo-keto reductase family 1 member B1 Rattus norvegicus 0-16 9579068-1 1998 D-Amino acids, important intermediates in the production of semisynthetic penicillins and cephalosporins, are currently prepared from the corresponding hydantoins using bacterial biomass containing two enzymes, hydantoinase and carbamylase. Hydantoins 152-162 AWN88_RS03840 Agrobacterium tumefaciens 211-223 8825077-1 1995 A lower microsomal epoxide hydrolase (mEH) activity has been associated with increased likelihood of fetal hydantoin syndrome. Hydantoins 107-116 epoxide hydrolase 1, microsomal Mus musculus 38-41 7562906-2 1995 Variation of substituents on the hydantoin ring leads to potent and selective Ang II antagonists with nanomolar IC50 values at the AT1 receptor and negligible affinity for the AT2 receptor. Hydantoins 33-42 angiotensinogen Rattus norvegicus 78-84 7578956-1 1995 The crystal structure of the hydantoin 1-[(S)-1"-aminoethylmalonyl benzyl ester]-(S)-4-methylimidazolidin-2,5-dione (1) derived from the peptide H-Ala-gAla-mGly-OBzl, having the retro-inverso modification of the Ala-Gly bond, has been determined by x-ray diffraction analysis. Hydantoins 29-38 galactosidase alpha Homo sapiens 151-155 7562906-2 1995 Variation of substituents on the hydantoin ring leads to potent and selective Ang II antagonists with nanomolar IC50 values at the AT1 receptor and negligible affinity for the AT2 receptor. Hydantoins 33-42 angiotensin II receptor, type 1a Rattus norvegicus 131-134 2079641-2 1990 Derivatives of hydantoin have been found to inactivate human leukocyte elastase irreversibly. Hydantoins 15-24 elastase, neutrophil expressed Homo sapiens 61-79 8035330-3 1994 The serum concentrations associated with half-maximal hepatic CYP2B induction (EC50 values) were 6 to 11 microM and 15 to 18 microM for the diphenyl-substituted barbiturate and hydantoin, respectively, based on measurement of pentoxy- or benzyloxyresorufin O-dealkylation activities, or immunoreactive CYP2B1 protein. Hydantoins 177-186 cytochrome P450, family 2, subfamily b, polypeptide 1 Rattus norvegicus 302-308 1613744-2 1992 The hypothesis that clinical side effects of the aldose reductase inhibitor (ARI) sorbinil were related to its hydantoin ring led to a bioisosteric analysis and replacement of the hydantoin by a spiro hydroxy acetic acid moiety as in 40. Hydantoins 111-120 aldo-keto reductase family 1 member B1 Rattus norvegicus 49-65 1613744-2 1992 The hypothesis that clinical side effects of the aldose reductase inhibitor (ARI) sorbinil were related to its hydantoin ring led to a bioisosteric analysis and replacement of the hydantoin by a spiro hydroxy acetic acid moiety as in 40. Hydantoins 180-189 aldo-keto reductase family 1 member B1 Rattus norvegicus 49-65 2128352-0 1990 Effects of novel hydantoin derivatives with aldose reductase inhibiting activity on galactose-induced cataract in rats. Hydantoins 17-26 aldo-keto reductase family 1 member B1 Rattus norvegicus 44-60 2113948-1 1990 A series of spiro hydantoins derived from 8-azachromanones (2,3-dihydro-4H-pyrano[2,3-b]pyridin-4-ones) has been prepared and tested for aldose reductase inhibitory activity. Hydantoins 18-28 aldo-keto reductase family 1 member B Homo sapiens 137-153 7658443-2 1995 Structural modifications of N- and C-linked (principally hydantoin) analogues at the 5-position were synthesized and their pharmacological activities were utilized to deduce significant steric and electrostatic requirements of the 5-HT1D and 5-HT2A receptor subtypes. Hydantoins 57-66 5-hydroxytryptamine receptor 1D Homo sapiens 231-237 7658443-2 1995 Structural modifications of N- and C-linked (principally hydantoin) analogues at the 5-position were synthesized and their pharmacological activities were utilized to deduce significant steric and electrostatic requirements of the 5-HT1D and 5-HT2A receptor subtypes. Hydantoins 57-66 5-hydroxytryptamine receptor 2A Homo sapiens 242-248 3378426-8 1988 Aqueous solutions of (D)MDM hydantoin in concentrations as used in cosmetic products therefore contain enough free formaldehyde to cause dermatitis in a patch test system in some formaldehyde-allergic patients: 12 such patients applied a cream containing 1% DMDM hydantoin to the flexor aspect of the lower arm twice daily for 1 week; 4 (33%) developed dermatitis. Hydantoins 28-37 secreted LY6/PLAUR domain containing 1 Homo sapiens 24-27 34648230-0 2021 Structure-Activity Relationship Studies of Hydantoin-Cored Ligands for Smoothened Receptor. Hydantoins 43-52 smoothened, frizzled class receptor Homo sapiens 71-90 3425630-0 1987 Elevated glucocorticoid receptor levels in lymphocytes of children with the fetal hydantoin syndrome (FHS). Hydantoins 82-91 nuclear receptor subfamily 3 group C member 1 Homo sapiens 9-32 3121857-2 1988 Spiro hydantoins derived from five- and six-membered ketones fused to an aromatic ring or ring system inhibit aldose reductase isolated from calf lens. Hydantoins 6-16 aldose reductase Bos taurus 110-126 3115267-0 1987 Development of potent aldose reductase inhibitors having a hydantoin structure. Hydantoins 59-68 aldo-keto reductase family 1 member B1 Rattus norvegicus 22-38 3115267-1 1987 Seventeen hydantoin derivatives were tested as inhibitors of aldose reductase, an enzyme believed to participate in the initiation of diabetic complications. Hydantoins 10-19 aldo-keto reductase family 1 member B1 Rattus norvegicus 61-77 32505850-6 2020 Hydantoin derivatives (5-7) were significantly more effective than the reference inhibitor verapamil (up to 2.6-fold at a 10-fold lower concentration) modulating ABCB1-efflux pump, also possessing a good drug-drug interaction profile. Hydantoins 0-9 ATP binding cassette subfamily B member 1 Homo sapiens 162-167 3989820-1 1985 Selectively substituted hydantoins 1 (15 examples), 4-hydroxy-2-imidazolidinones 2 (13 examples), 2-imidazolones 3 (10 examples), 2-imidazolidinones 4 (four examples), vicinal diamines 5 (two examples), and simple amino acid derivatives 6 (four examples) have been prepared and evaluated in the maximal electroshock seizure (MES), subcutaneous pentylenetetrazole seizure threshold (sc Met), and rotorod (Tox) tests. Hydantoins 24-34 thymocyte selection associated high mobility group box Homo sapiens 404-407 6087417-8 1984 The hydantoin acts at the platelet PGD2 receptor. Hydantoins 4-13 prostaglandin D2 receptor Homo sapiens 35-48 6302737-0 1983 Pharmacological and cardiovascular properties of a hydantoin derivative, BW 245 C, with high affinity and selectivity for PGD2 receptors. Hydantoins 51-60 prostaglandin D2 synthase Homo sapiens 122-126 90139-4 1979 The most pronounced changes in IgA levels were seen in patients in whom the hydantoin medication also changed. Hydantoins 76-85 CD79a molecule Homo sapiens 31-34 650410-2 1978 Binding of some salicylates and hydantoin derivatives to bovine serum albumin by fluorescent probe technique (author"s transl)]. Hydantoins 32-41 albumin Homo sapiens 64-77 1244103-2 1975 Under the treatment with antiepileptic drugs, especially with hydantoin and succinimide a depression of the activity of EGOT and the level of pyridoxal-phosphate in serum followed. Hydantoins 62-71 eosinophil granule ontogeny transcript Homo sapiens 120-124 4369857-2 1974 The hydantoins released on hydrolysis of HCN oligomers. Hydantoins 4-14 metastasis associated lung adenocarcinoma transcript 1 Homo sapiens 41-44 33719441-4 2021 We describe the discovery of GLPG1972/S201086, a potent and selective ADAMTS-5 inhibitor obtained by optimization of a promising hydantoin series following an HTS. Hydantoins 129-138 ADAM metallopeptidase with thrombospondin type 1 motif 5 Homo sapiens 70-78 4150990-0 1974 The role of dihydropyrimidinase in the metabolism of some hydantoin and succinimide drugs. Hydantoins 58-67 dihydropyrimidinase Homo sapiens 12-31 32069022-5 2020 The 2"-F-hydantoins in duplex DNA were found to be highly resistant to the glycosylase activity of Fpg and NEIL1 compared to the unmodified lesion substrates. Hydantoins 4-19 nei like DNA glycosylase 1 Homo sapiens 107-112 32302101-0 2020 Inhibition of Excison of Oxidatively Generated Hydantoin DNA Lesions by NEIL1 by the Competitive Binding of the Nucleotide Excision Repair Factor XPC-RAD23B. Hydantoins 47-56 nei like DNA glycosylase 1 Homo sapiens 72-77 32302101-0 2020 Inhibition of Excison of Oxidatively Generated Hydantoin DNA Lesions by NEIL1 by the Competitive Binding of the Nucleotide Excision Repair Factor XPC-RAD23B. Hydantoins 47-56 XPC complex subunit, DNA damage recognition and repair factor Homo sapiens 146-156 31944122-0 2020 Ullmann-type C-Se cross-coupling in the hydantoin family: Synthesis, mechanistic studies, and tests of biological activity. Hydantoins 40-49 choreoathetosis/spasticity, episodic (paroxysmal choreoathetosis/spasticity) Homo sapiens 13-17 32105280-0 2020 Interaction of hydantoin with solar wind minority ions: O6+ and He2. Hydantoins 15-24 sperm associated antigen 11A Homo sapiens 64-67 30969473-6 2019 To explore the relationships between molecular structures and corresponding binding abilities to aid the new AR modulator design, multiple linear regressions (MLR) are employed to analyze a series of hydantoin analogues, which can bind to androgen receptor acting as AR modulators. Hydantoins 200-209 androgen receptor Homo sapiens 109-111 31744675-3 2020 The present study examined the AR inhibitory effects of novel synthetic hydantoins and their structural relatives, some of which were obtained from chemically engineered extracts of natural plants, and discovered several novel AR inhibitors with moderate inhibitory activity. Hydantoins 72-82 aldo-keto reductase family 1 member B Homo sapiens 31-33 31744675-3 2020 The present study examined the AR inhibitory effects of novel synthetic hydantoins and their structural relatives, some of which were obtained from chemically engineered extracts of natural plants, and discovered several novel AR inhibitors with moderate inhibitory activity. Hydantoins 72-82 aldo-keto reductase family 1 member B Homo sapiens 227-229 30969473-6 2019 To explore the relationships between molecular structures and corresponding binding abilities to aid the new AR modulator design, multiple linear regressions (MLR) are employed to analyze a series of hydantoin analogues, which can bind to androgen receptor acting as AR modulators. Hydantoins 200-209 androgen receptor Homo sapiens 239-256 30969473-6 2019 To explore the relationships between molecular structures and corresponding binding abilities to aid the new AR modulator design, multiple linear regressions (MLR) are employed to analyze a series of hydantoin analogues, which can bind to androgen receptor acting as AR modulators. Hydantoins 200-209 androgen receptor Homo sapiens 267-269 31840594-6 2019 The cell migration index and expression level of tumor invasion-promoting metalloproteinase- 9 (MMP-9) gene were significantly decreased after treatment with the tested hydantoin derivatives implicating their inhibitory role in colon cancer cell motility and invasion processes. Hydantoins 169-178 matrix metallopeptidase 9 Homo sapiens 96-101 31413795-0 2019 Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. Hydantoins 48-68 histone deacetylase 6 Homo sapiens 84-89 31413795-2 2019 Herein, we reported a series of 2,4-imidazolinedione derivatives as novel HDAC6 isoform-selective inhibitors based on structure-based drug design. Hydantoins 32-52 histone deacetylase 6 Homo sapiens 74-79 30614708-4 2019 This synthetic strategy is user friendly as CBX is a bench-stable easy-to-handle crystalline reagent and avoids conventional multistep protocols, thus allowing the facile synthesis of a library of chiral hydantoins. Hydantoins 204-214 chromobox 1 Homo sapiens 44-47 29126741-1 2017 A series of novel hydantoin-bridged analogues of combretastatin A-4 (CA-4) were designed, synthesized and evaluated for antiproliferative activities in vitro and in vivo. Hydantoins 18-27 carbonic anhydrase 4 Homo sapiens 49-67 29500402-9 2018 However, we further found that phenytoin attenuated RIPK1 kinase activity in vitro, likely due to the hydantoin scaffold also present in necrostatin-1, and blocked upstream necrosome formation steps in the cells undergoing necroptosis. Hydantoins 102-111 receptor interacting serine/threonine kinase 1 Homo sapiens 52-57 29227678-4 2018 A hydantoin-bearing submicromolar primary hit acting as an Aurora kinase A inhibitor was discovered with a combination of rational design, parallel synthesis using the procedures developed, in silico and in vitro screenings. Hydantoins 2-11 aurora kinase A Homo sapiens 59-74 29126741-1 2017 A series of novel hydantoin-bridged analogues of combretastatin A-4 (CA-4) were designed, synthesized and evaluated for antiproliferative activities in vitro and in vivo. Hydantoins 18-27 carbonic anhydrase 4 Homo sapiens 69-73 27151486-8 2016 Molecular docking study performed for two hydantoins with the highest bioavailability scores shows high binding affinity to tyrosine kinase receptor IGF-1R. Hydantoins 42-52 insulin like growth factor 1 receptor Homo sapiens 149-155 28711352-0 2017 Development of a prodrug of hydantoin based TACE inhibitor. Hydantoins 28-37 ADAM metallopeptidase domain 17 Homo sapiens 44-48 28711352-1 2017 Our research on hydantoin based TNF-alpha converting enzyme (TACE) inhibitors led to fused bi-heteroaryl hydantoin series that demonstrate sub-nanomolar potency (Ki) as well as excellent activity in human whole blood (hWBA). Hydantoins 16-25 ADAM metallopeptidase domain 17 Homo sapiens 32-59 28711352-1 2017 Our research on hydantoin based TNF-alpha converting enzyme (TACE) inhibitors led to fused bi-heteroaryl hydantoin series that demonstrate sub-nanomolar potency (Ki) as well as excellent activity in human whole blood (hWBA). Hydantoins 16-25 ADAM metallopeptidase domain 17 Homo sapiens 61-65 28558971-0 2017 Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors. Hydantoins 32-41 ADAM metallopeptidase domain 17 Homo sapiens 55-59 28558971-1 2017 We have identified a series of hydantoin-derived TNF-a converting enzyme (TACE) inhibitors containing a pendant fused bi-heteroaryl group, which demonstrate sub-nanomolar potency (Ki), excellent activity in human whole blood assay, and improved DMPK profiles over prior series. Hydantoins 31-40 ADAM metallopeptidase domain 17 Homo sapiens 49-72 28613895-0 2017 A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose. Hydantoins 19-28 ADAM metallopeptidase with thrombospondin type 1 motif 4 Homo sapiens 42-55 28613895-0 2017 A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose. Hydantoins 19-28 ADAM metallopeptidase with thrombospondin type 1 motif 5 Homo sapiens 60-73 27933964-5 2016 The principal SAR insight was that the hydantoin core of 1 is required for high antischistosomal activity. Hydantoins 39-48 sarcosine dehydrogenase Homo sapiens 14-17 27283790-4 2016 We revealed that a combination of our newly developed linker and hydantoin (54) plays a pivotal role in improving the potency and selectivity of LXRbeta. Hydantoins 65-74 nuclear receptor subfamily 1, group H, member 2 Mus musculus 145-152 28558971-1 2017 We have identified a series of hydantoin-derived TNF-a converting enzyme (TACE) inhibitors containing a pendant fused bi-heteroaryl group, which demonstrate sub-nanomolar potency (Ki), excellent activity in human whole blood assay, and improved DMPK profiles over prior series. Hydantoins 31-40 ADAM metallopeptidase domain 17 Homo sapiens 74-78 28558971-1 2017 We have identified a series of hydantoin-derived TNF-a converting enzyme (TACE) inhibitors containing a pendant fused bi-heteroaryl group, which demonstrate sub-nanomolar potency (Ki), excellent activity in human whole blood assay, and improved DMPK profiles over prior series. Hydantoins 31-40 DM1 protein kinase Homo sapiens 245-249 27009905-0 2016 Plasmin inhibitors with hydrophobic amino acid-based linker between hydantoin moiety and benzimidazole scaffold enhance inhibitory activity. Hydantoins 68-77 plasminogen Homo sapiens 0-7 27009905-1 2016 In this letter we report the design and synthesis of a series of plasmin inhibitors, which share the amino acid-based linker with limited free rotation between the hydantoin moiety and the benzimidazole scaffold. Hydantoins 164-173 plasminogen Homo sapiens 65-72 25813041-4 2015 Also, the NEIL1 and NEIL3 DNA glycosylases can remove hydantoin lesions but none of the glycosylases, including OGG1, are able to remove 8-oxoG from telomeric quadruplexes. Hydantoins 54-63 nei like DNA glycosylase 1 Homo sapiens 10-15 25813041-4 2015 Also, the NEIL1 and NEIL3 DNA glycosylases can remove hydantoin lesions but none of the glycosylases, including OGG1, are able to remove 8-oxoG from telomeric quadruplexes. Hydantoins 54-63 nei like DNA glycosylase 3 Homo sapiens 20-25 25813041-6 2015 However, NEIL1, NEIL2 and NEIL3 remove hydantoins from telomeric quadruplexes formed by five TTAGGG repeats much more rapidly than the commonly studied four-repeat quadruplex structures. Hydantoins 39-49 nei like DNA glycosylase 1 Homo sapiens 9-14 25813041-6 2015 However, NEIL1, NEIL2 and NEIL3 remove hydantoins from telomeric quadruplexes formed by five TTAGGG repeats much more rapidly than the commonly studied four-repeat quadruplex structures. Hydantoins 39-49 nei like DNA glycosylase 2 Homo sapiens 16-21 25813041-6 2015 However, NEIL1, NEIL2 and NEIL3 remove hydantoins from telomeric quadruplexes formed by five TTAGGG repeats much more rapidly than the commonly studied four-repeat quadruplex structures. Hydantoins 39-49 nei like DNA glycosylase 3 Homo sapiens 26-31 25580690-3 2015 The hydantoin, 3-phenyl-5-(4-ethylphenyl)-imidazolidine-2,4-dione (IM-3), synthesized from the amino acid, glycine, was selected for psychopharmacological studies in mice on the basis of its chemical and structural similarity with phenytoin. Hydantoins 4-13 immunoregulatory 3 Mus musculus 67-71 25415648-0 2014 Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis. Hydantoins 39-48 ADAM metallopeptidase with thrombospondin type 1 motif, 4 Rattus norvegicus 63-76 25415648-4 2014 A series of hydantoin inhibitors of ADAMTS-4 and ADAMTS-5 were identified from a screening campaign and optimized through structure-based drug design to give hydantoin 13. Hydantoins 12-21 ADAM metallopeptidase with thrombospondin type 1 motif, 4 Rattus norvegicus 36-44 25415648-4 2014 A series of hydantoin inhibitors of ADAMTS-4 and ADAMTS-5 were identified from a screening campaign and optimized through structure-based drug design to give hydantoin 13. Hydantoins 12-21 ADAM metallopeptidase with thrombospondin type 1 motif, 5 Rattus norvegicus 49-57 25415648-4 2014 A series of hydantoin inhibitors of ADAMTS-4 and ADAMTS-5 were identified from a screening campaign and optimized through structure-based drug design to give hydantoin 13. Hydantoins 158-167 ADAM metallopeptidase with thrombospondin type 1 motif, 4 Rattus norvegicus 36-44 25415648-4 2014 A series of hydantoin inhibitors of ADAMTS-4 and ADAMTS-5 were identified from a screening campaign and optimized through structure-based drug design to give hydantoin 13. Hydantoins 158-167 ADAM metallopeptidase with thrombospondin type 1 motif, 5 Rattus norvegicus 49-57 25372819-2 2014 Allantoinase catalyzes the reversible hydrolysis of allantoin into allantoate by hydrolytic cleavage of the N1-C2 amide bond of the five-membered hydantoin ring. Hydantoins 146-155 allantoinase AllB Bacillus licheniformis DSM 13 = ATCC 14580 0-12 25173590-1 2014 Two series of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 2,4-imidazolinedione/pyrazolone scaffold were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against HT-29, H460, A549, MKN-45, and U87MG cancer cell lines in vitro. Hydantoins 71-91 MET proto-oncogene, receptor tyrosine kinase Homo sapiens 163-168 23755964-5 2013 GD NEIL3 excised the hydantoin lesions spiroiminodihydantoin (Sp) and guanidinohydantoin (Gh) in single-stranded (ss) and double-stranded (ds) DNA efficiently. Hydantoins 21-30 nei like DNA glycosylase 3 Homo sapiens 3-8 24660679-9 2014 Additionally, the hydantoin ring of 66 is able to interact by hydrogen bonds with two conserved water molecules in the MAO-A active site, while the methyl-thiohydantoin ring of 68 is within hydrogen bond distance from the hydrogen atom attached to the (N-5) of FAD cofactor. Hydantoins 18-27 monoamine oxidase A Homo sapiens 119-124 23810497-0 2013 Hydantoin based inhibitors of MMP13--discovery of AZD6605. Hydantoins 0-9 matrix metallopeptidase 13 Rattus norvegicus 30-35 22381672-1 2012 An association between alpha(1)-adrenoceptor affinities, hERG K(+)-antagonistic properties and antiarrhythmic activities for a series of phenylpiperazine derivatives of hydantoin (2a-21a) was investigated. Hydantoins 169-178 ETS transcription factor ERG Homo sapiens 57-61 23305905-0 2013 Loss of Neil3, the major DNA glycosylase activity for removal of hydantoins in single stranded DNA, reduces cellular proliferation and sensitizes cells to genotoxic stress. Hydantoins 65-75 nei like 3 (E. coli) Mus musculus 8-13 23305905-4 2013 The mammalian endonuclease VIII-like 3 (Neil3) is one of the four DNA glycosylases found to recognize and remove hydantoins in the first step of base excision repair (BER) pathway. Hydantoins 113-123 nei like DNA glycosylase 3 Homo sapiens 14-38 23305905-4 2013 The mammalian endonuclease VIII-like 3 (Neil3) is one of the four DNA glycosylases found to recognize and remove hydantoins in the first step of base excision repair (BER) pathway. Hydantoins 113-123 nei like DNA glycosylase 3 Homo sapiens 40-45 23305905-5 2013 We have generated mice lacking Neil3 and by using total cell extracts we demonstrate that Neil3 is the main DNA glycosylase that incises hydantoins in single stranded DNA in tissues. Hydantoins 137-147 nei like 3 (E. coli) Mus musculus 31-36 23305905-5 2013 We have generated mice lacking Neil3 and by using total cell extracts we demonstrate that Neil3 is the main DNA glycosylase that incises hydantoins in single stranded DNA in tissues. Hydantoins 137-147 nei like 3 (E. coli) Mus musculus 90-95 22897611-1 2012 A novel selective androgen receptor modulator scaffold has been discovered through structural modifications of hydantoin antiandrogens. Hydantoins 111-120 androgen receptor Rattus norvegicus 18-35 23543430-4 2013 Small-molecule BACE1 inhibitors of the hydroxyethylamine, hydantoin, and sulfamide classes were functionalized by biotin PEG linkers of varying lengths forming probes that were bound to streptavidin donor beads. Hydantoins 58-67 beta-secretase 1 Homo sapiens 15-20 23543430-7 2013 A probe from the hydantoin class was chosen for further optimization, where the final assay conditions of 50 nM BACE and 250 nM probe were used and Z(") values >0.75 were commonly observed. Hydantoins 17-26 beta-secretase 1 Homo sapiens 112-116 23117589-5 2012 The difference in potencies of hydantoin and piperazinedione analogues, together with the necessity of C-5/C-6 R-absolute configuration has been revealed through molecular docking. Hydantoins 31-40 complement C5 Homo sapiens 103-106 23117589-5 2012 The difference in potencies of hydantoin and piperazinedione analogues, together with the necessity of C-5/C-6 R-absolute configuration has been revealed through molecular docking. Hydantoins 31-40 complement C6 Homo sapiens 107-110 22959434-3 2012 In mice, Neil3 is the main DNA glycosylase for repair of hydantoin lesions in single-stranded DNA of neural stem/progenitor cells, promoting neurogenesis. Hydantoins 57-66 nei like 3 (E. coli) Mus musculus 9-14 21696967-0 2011 The discovery of long-acting saligenin beta2 adrenergic receptor agonists incorporating hydantoin or uracil rings. Hydantoins 88-97 adrenoceptor beta 2 Rattus norvegicus 39-64 21965738-2 2011 Previously, we demonstrated that eight hydantoin derivatives inhibited the P-glycoprotein (ABCB1) efflux pump of mouse T-lymphoma cells, as well as acting synergistically with the anticancer drug doxorubicin. Hydantoins 39-48 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 91-96 21737263-2 2011 A novel series of potent bicyclic hydantoin Smo antagonists was reported in the preceding article, these have been resolved, and optimized to identify potent homochiral derivatives with clean off-target profiles and good pharmacokinetic properties in preclinical species. Hydantoins 34-43 smoothened, frizzled class receptor Homo sapiens 44-47 22351672-0 2012 Activity of fourteen new hydantoin compounds on the human ABCB1 efflux pump. Hydantoins 25-34 ATP binding cassette subfamily B member 1 Homo sapiens 58-63 22351672-3 2012 Previously it was observed that hydantoin compounds can modulate the activity of the ABCB1 pump. Hydantoins 32-41 ATP binding cassette subfamily B member 1 Homo sapiens 85-90 22351672-4 2012 MATERIALS AND METHODS: Fourteen hydantoin derivatives were synthesized and studied for their capacity to increase accumulation of ethidium bromide (EB) by mouse lymphoma cancer cells that were transfected with the human ABCB1 gene and overexpress the human ABCB1 pump. Hydantoins 32-41 ATP binding cassette subfamily B member 1 Homo sapiens 220-225 21671576-3 2011 The combination of a recognized privileged scaffold (hydantoin) and a functional group with high incidence in bioactive molecules (guanidine) guided the design of a library of amphipatic compounds, which allowed the discovery of novel TRPV1 ion channel blockers. Hydantoins 53-62 transient receptor potential cation channel subfamily V member 1 Homo sapiens 235-240 21696967-1 2011 A series of novel, potent and selective human beta(2) adrenoceptor agonists incorporating a hydantoin or a uracil ring on the right-hand side phenyl ring of (R)-salmeterol is presented. Hydantoins 92-101 adrenoceptor beta 2 Homo sapiens 46-66 20386016-1 2010 RO5068760, a substituted hydantoin, represents a new class of potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1/2 inhibitors. Hydantoins 25-34 mitogen-activated protein kinase kinase 1 Homo sapiens 133-139 21799731-10 2011 Importantly, a number of redundant DNA glycosylase activities can excise hydantoin residues, including human NTH1, NEIL1 and NEIL2 and the former protein being a major DNA glycosylase activity in HeLa cells extracts. Hydantoins 73-82 nth like DNA glycosylase 1 Homo sapiens 109-113 21799731-10 2011 Importantly, a number of redundant DNA glycosylase activities can excise hydantoin residues, including human NTH1, NEIL1 and NEIL2 and the former protein being a major DNA glycosylase activity in HeLa cells extracts. Hydantoins 73-82 nei like DNA glycosylase 1 Homo sapiens 115-120 21799731-10 2011 Importantly, a number of redundant DNA glycosylase activities can excise hydantoin residues, including human NTH1, NEIL1 and NEIL2 and the former protein being a major DNA glycosylase activity in HeLa cells extracts. Hydantoins 73-82 nei like DNA glycosylase 2 Homo sapiens 125-130 21187464-0 2010 Biological activity of hydantoin derivatives on P-glycoprotein (ABCB1) of mouse lymphoma cells. Hydantoins 23-32 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 64-69 21187464-8 2010 CONCLUSION: These results indicated the role of chemical modifications within the hydantoin ring for its potential inhibition of the ABCB1 transporter. Hydantoins 82-91 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 133-138 21441024-1 2011 A new series of IGF-1R inhibitors related to hydantoins were identified from a lead originating from HTS. Hydantoins 45-55 insulin like growth factor 1 receptor Homo sapiens 16-22 21106451-1 2010 Our research on hydantoin based TNF-alpha converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (K(i)) as well as excellent activity in human whole blood. Hydantoins 16-25 ADAM metallopeptidase domain 17 Homo sapiens 32-59 21106451-1 2010 Our research on hydantoin based TNF-alpha converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (K(i)) as well as excellent activity in human whole blood. Hydantoins 16-25 ADAM metallopeptidase domain 17 Homo sapiens 61-65