ライフサイエンスコーパス: peptidomimetics

1 mRNAs into specific peptide analog polymers (peptidomimetics).

2 ess to obtain the linear C-hydroxyalkylamido peptidomimetics.

3 synthesized and assayed libraries of mutant peptidomimetics.

4 ng conformationally constrained beta-hairpin peptidomimetics.

5 r-Psi[(Z and E)CH=C]-Pro-Arg-NH(2), 1 and 2, peptidomimetics.

6 nd to increase the water solubilities of the peptidomimetics.

7 opamine receptor modulating activity of such peptidomimetics.

8 s as components in pharmaceutical agents and peptidomimetics.

9 for incorporation into biologically relevant peptidomimetics.

10 erate the clinical utility of small molecule peptidomimetics.

11 or related amino acid motifs, and RGD-based peptidomimetics.

12 f strain-specific antibacterial peptides and peptidomimetics.

13 rent drug discovery efforts based on proline peptidomimetics.

14 and represent a novel approach to designing peptidomimetics.

15 n the design of conformationally constrained peptidomimetics.

16 luding linear peptides, cyclic peptides, and peptidomimetics.

17 opamine receptor modulating activity of such peptidomimetics.

18 chromenopyridine fused thiazolino-2-pyridone peptidomimetics.

19 andostatin-based conformationally restricted peptidomimetics.

20 ith delivery and formulation of peptides and peptidomimetics.

21 lts facilitate the design of new sandostatin peptidomimetics.

22 ive catalysis and the preparation of diverse peptidomimetics.

23 ential applications in the field of peptides/peptidomimetics.

24 ress various liabilities in hit antimalarial peptidomimetics.

25 erve for the synthesis of various structured peptidomimetics.

26 es comprising small molecules, peptides, and peptidomimetics.

27 f concept was first obtained by peptides and peptidomimetics.

28 lent opportunity to construct small-molecule peptidomimetics.

29 ts ability to induce secondary structures in peptidomimetics.

30 in-protein interaction and other therapeutic peptidomimetics.

31 vides a rapid and efficient route to enamine peptidomimetics.

32 sting the possibility of LptD inhibition via peptidomimetics.

33 ilding blocks with considerable potential as peptidomimetics.

34 dues in building programmable and functional peptidomimetics.

35 evelopment of targeted therapeutics based on peptidomimetics.

36 development of new small antiviral drugs or peptidomimetics.

37 ioisostere to provide protease resistance in peptidomimetics.

38 rious ligands including TRP/NTL peptides and peptidomimetics.

39 ning and refining therapeutically-attractive peptidomimetics.

40 al properties of this peptide by introducing peptidomimetics.

41 tives are valuable pharmacological agents as peptidomimetics.

42 e introduced as the backbone modification in peptidomimetics.

43 nthesis of biologically active molecules and peptidomimetics.

44 advantage of peptoids over other families of peptidomimetics.

45 beta-Turn peptidomimetics 1 were designed to mimic hot spots of ne

46 in-protein interactions led us to design the peptidomimetics 1-3.

47 ects observed previously for PLG and the PLG peptidomimetics 2 and 4.

48 Peptidomimetics 3 and 4 also increased the percentage of

49 Peptidomimetics 3 and 4 were evaluated in vivo as modula

50 Peptidomimetics 3-5 each affected rotational behavior in

51 , butyl, and benzyl moieties to give the PLG peptidomimetics 3-5, respectively.

52 e isobutyl, butyl, and benzyl groups to give peptidomimetics 3-5, respectively.

53 ent study, L-prolyl-L-leucyl-glycinamide (1) peptidomimetics 3a-3d and 4a-4d were synthesized utilizi

54 deprotection provided the epoxide-containing peptidomimetics, 4 and 5.

55 etter than in the corresponding syntheses of peptidomimetics A.

56 Toward the design of new proline-rich peptidomimetics, a short peptide segment, present in sev

57 des can be used to design highly potent lead peptidomimetics against multi-resistant bacteria.

58 For this purpose, the development of peptidomimetics against the SARS-CoV-2 main protease (M(

59 y of conformationally restrained dipeptides, peptidomimetics, alkaloids, and other biologically activ

60 gamma-secretase, SPP is inhibited by helical peptidomimetics and apparently contains a substrate-bind

61 hput synthesis of linear C-hydroxyalkylamido peptidomimetics and beta-turn cyclic peptidomimetics via

62 es a concrete basis for the design of potent peptidomimetics and nonpeptidic compounds to inhibit MLL

63 r, the process can readily provide access to peptidomimetics and peptides with reversed sequences or

64 ing blocks of bioactive molecules, including peptidomimetics and pharmaceutical compounds.

65 The peptidomimetics and pyrimidoindolones bind to both activ

66 -HIV-1 drug target and may help in designing peptidomimetics and small molecule drugs targeted to thi

67 derived from the C-terminal tail of FGF23 or peptidomimetics and small-molecule organomimetics of the

68 cellular uptake in cancer cells by designed peptidomimetics and suggest that cancer cells with certa

69 en, select and optimize synthetic "designer" peptidomimetics and synthetic biologics.

70 chain stabilized peptides, (iii) non-natural peptidomimetics, and (iv) synthetic proteomimetics, and

71 , antimicrobial dendrimers and polypeptides, peptidomimetics, and AMP-drug conjugates and consider re

72 nd their corresponding prolines in peptides, peptidomimetics, and natural products has motivated rese

73 ional active site and allosteric inhibitors, peptidomimetics, and novel proteolysis-targeted chimera

74 cks for numerous bioactive natural products, peptidomimetics, and pharmaceuticals, yet efficient asym

75 Antibodies, peptides/peptidomimetics, and small molecules constitute three cl

76 e peptidomimetic and LgN, the copy number of peptidomimetics, and the spacer between SmN and VHH, gen

77 Dual-capped peptidomimetics are a new, generalizable paradigm for he

78 y) showed that the presented hydantoin-based peptidomimetics are able to project their substituents i

79 Non-natural antimicrobial peptidomimetics are an ideal example of this, as they ha

80 Amidoboronic acid-containing peptidomimetics are an important class of scaffolds in c

81 Peptides and peptidomimetics are attractive drug candidates because o

82 biomedical challenges to which antimicrobial peptidomimetics are being applied.

83 Peptidomimetics are classes of molecules that mimic stru

84 s derived from amino acids, peptides, and/or peptidomimetics are described.

85 Peptidomimetics are developed by modifications of native

86 Thiazolino fused 2-pyridone peptidomimetics are of significant biological importance

87 Peptidomimetics are one set of probes used in the transi

88 ially addressable microchips of peptides and peptidomimetics are powerful tools for high-throughput b

89 Peptidomimetics are small protein-like molecules designe

90 ent building blocks, proteins, peptides, and peptidomimetics, are being coopted to build hierarchy be

91 e infusion of PF4 or PF4-related peptides or peptidomimetics as a way of beneficially stimulating "en

92 ion toward the design of cyclic peptides and peptidomimetics as calpain inhibitors.

93 ch offers a general framework for optimizing peptidomimetics as inhibitors of protein-protein interac

94 However, the development of G protein peptidomimetics, as discussed in Mannes et al. represent

95 zed, and pharmacologically characterized new peptidomimetics based on a PLEV tetrapeptide scaffold de

96 eening a gamma-AA peptide library for cyclic peptidomimetics binding to the HECT domain of E6AP, an E

97 ERG inhibitory peptides (EIPs) and derived peptidomimetics bound ERG with high affinity and specifi

98 ionally restricted beta-sheet breaker hybrid peptidomimetics (BSBHps).

99 olefin containing N-peptidyl-O-hydroxylamine peptidomimetics, by virtue of their inhibitory potency a

100 meostasis, and we suggest that ANXA1 and its peptidomimetics can be novel therapeutic targets in neur

101 Since phage-borne peptidomimetics can be selected from phage display libra

102 Peptides or peptidomimetics can mimic binding of the tethered ligand

103 with molecular libraries, demonstrating that peptidomimetics can provide valuable clues about recepto

104 Peptidomimetics can respond to peptide limitations by di

105 A collection of peptidomimetics characterized by having an aspartic acid

106 leads to (i) a chemical library of putative peptidomimetics combining diverse azaheterocycles with t

107 5.5.6. and 5.6.5. spiro bicyclic lactam PLG peptidomimetics, compounds 3 and 4, respectively, was un

108 We have studied the efficacy of BH3 peptidomimetics consisting of the minimal death, or BH3,

109 Peptidomimetics containing ( S)- or ( R)-imidazolidin-2-

110 latelets are less responsive to peptides and peptidomimetics containing an arginine-glycine-aspartic

111 Protein-tyrosine peptidomimetics containing nonhydrolyzable phosphotyrosi

112 ion events by receptor cleavage or synthetic peptidomimetics corresponding to the newly generated N-t

113 Exocyclic small peptidomimetics corresponding to three critical binding

114 ed that sulfonyl-gamma-AApeptides as helical peptidomimetics could direct Abeta into the off-pathway

115 3 peptides (including all-D enantiomers) and peptidomimetics, covering more than seven orders of magn

116 The peptidomimetics described herein comprise a dibenzofuran

117 6 and was 20-fold more potent than synthetic peptidomimetics designed from the GPR56 tethered agonist

118 The peptidomimetics did not show cytotoxicity to HEK293T and

119 lustrate the procedure, a series of bivalent peptidomimetics directed toward the Trk receptors were p

120 A pyridine-enabled C-N bond activation of peptidomimetics employing cooperative palladium/copper c

121 Intermolecular stacking of the collapsed peptidomimetics, enabled by intermolecular hydrogen bond

122 A selected small library of six peptidomimetics, encompassing analogues of biological re

123 otential to be developed into cell-permeable peptidomimetics for delivery in vivo.

124 h was followed by amino acids, peptides, and peptidomimetics for medicinal chemistry.

125 This approach may yield reagents such as peptidomimetics for novel diagnostic and therapeutic int

126 ecognition that could be useful in designing peptidomimetics for RNA targeting.

127 aim of using the tumor-homing cyclo[DKP-RGD] peptidomimetics for site-directed delivery of the cytoto

128 e present the synthesis of highly active RGD peptidomimetics for the alphavbeta3 integrin with remark

129 ve recently emerged as important examples of peptidomimetics for their interesting complexing propert

130 forward in the development of PCNA targeting peptidomimetics for use as anti-cancer agents or as canc

131 Peptidomimetics, FTI-276 and GGTI-287, inhibit the trans

132 Synthetic strategies for the development of peptidomimetics have also been implemented with time.

133 Peptidomimetics have been applied to inhibit PPIs, howev

134 Compared to small molecules, peptidomimetics have emerged as powerful tools to disrup

135 Peptidomimetics have gained great attention for their fu

136 unnatural amino acids and their peptides as peptidomimetics have shown remarkable structural and fun

137 ethod can be used to prepare imidazole based peptidomimetics, herein exemplified by the synthesis of

138 and design of different classes of designer peptidomimetics: (i) macrocyclic peptides, (ii) side cha

139 clodehydration to afford thiazole containing peptidomimetics in a short synthetic sequence.

140 ation of co-crystal structures of two potent peptidomimetics in complex with WDR5 establishes their s

141 c quantities, which can be exploited through peptidomimetics in diabetes or Alzheimer's disease.

142 h are presented to document the relevance of peptidomimetics in drug discovery.

143 g in a single process generating the desired peptidomimetics in good to excellent yields within a 25

144 of K-Ras as well as H- and N-Ras to the CAAX peptidomimetics in human tumor cell lines is not known.

145 ution studies of radiolabeled multi-triazolo-peptidomimetics in mice bearing receptor-positive tumor

146 ility and increased receptor affinity of the peptidomimetics in vitro.

147 beta-Strand peptidomimetics incorporating amino acid analogues based

148 This demonstrates that peptidomimetics, incorporating in this case the promiscu

149 elective novel class of non-thiol-containing peptidomimetics inhibits human tumor growth in whole ani

150 ate that the bioactive conformation of these peptidomimetics is close to the minimal energy conformat

151 polyhydroxylated piperidine and pyrrolidine peptidomimetics is described.

152 amino acid as the central core and acting as peptidomimetics, is presented.

153 with three different classes of inhibitors: peptidomimetics, isatins, and pyrimidoindolones.

154 Candidate inhibitors were isolated from a peptidomimetics library.

155 Two stapled peptidomimetics, M1-S1 and M1-S2, were identified as eff

156 inoline scaffold and show that the resulting peptidomimetics maintain the desired pharmacological pro

157 ogen receptor-coregulator interactions using peptidomimetics may be a viable therapeutic approach for

158 type of proteolytically stable FPR2-specific peptidomimetics may serve as valuable tools for future a

159 ors, as delineated into three broad domains: peptidomimetics, natural products, and synthetic small m

160 array comprising different types of cationic peptidomimetics obtained by a general monomer-based soli

161 design, a series of macrocyclic ("stapled") peptidomimetics of (10)Panx1, the most established pepti

162 The reported novel mono-triazolo-peptidomimetics of [Nle(15)]MG11 showed either improved

163 ructure mimetic that can be used to generate peptidomimetics of biological interest.

164 Peptoids are peptidomimetics of interest in the fields of drug develo

165 ay a role in the potency of the gamma-lactam peptidomimetics of PLG, it does not appear to be the pri

166 6-Substituted bicyclic thiazolidine lactam peptidomimetics of Pro-Leu-Gly-NH(2) (1) were synthesize

167 r continuing program exploring glucose-based peptidomimetics of somatostatin (SRIF-14), we sought to

168 rial activities of OMP-targeting macrocyclic peptidomimetics of the antimicrobial peptide protegrin-1

169 Two epoxide-containing peptidomimetics of the isopeptide, glutamyl-gamma-glutam

170 f the activity of antimicrobial peptides and peptidomimetics on the inoculum should be considered.

171 lecule for the preparation of collections of peptidomimetics or biologically active compounds based o

172 can be performed in solution on unprotected peptidomimetics or on resin-bound peptides with side-cha

173 of AhR-protein and AhR-DNA interfaces using peptidomimetics or small molecules.

174 structural diverse inhibitors of Vif such as peptidomimetics or small organic molecules.

175 ttractive intermediates for the synthesis of peptidomimetics, polyheterocycles, and other multifuncti

176 Most of the peptidomimetics possessed high to moderate activity towa

177 Azapeptides are peptidomimetics possessing semicarbazide residues that c

178 s an important strategy for the synthesis of peptidomimetics (pseudo-peptides).

179 tems in Lepidoptera and aid in the design of peptidomimetics, pseudopeptides or small molecules capab

180 Peptidomimetics represent an important field in chemistr

181 Peptides and peptidomimetics represent the middle space between small

182 pha/beta, alpha/gamma and alpha/delta hybrid peptidomimetics, respectively.

183 These non-thiol-containing peptidomimetics show exceptional selectivity for PGGTase

184 s the practical applications of peptides and peptidomimetics, showcasing their successful integration

185 t the poor mimicry of the amide bond by many peptidomimetics stems from their inability to partake in

186 of drugs as they accept a large spectrum of peptidomimetics such as beta-lactam antibiotics, antivir

187 (Hydroxyethyl)urea peptidomimetics systematically altered at positions P2-P

188 ptides is a means to begin accessing complex peptidomimetics systematically.

189 of amyloid diseases, the use of peptides and peptidomimetics tailor-designed to overcome amyloidogene

190 ional inhibitory property of the synthesized peptidomimetics, taking advantage of the C-terminal Q am

191 re-based strategy for the rational design of peptidomimetics targeting RING domains, and we demonstra

192 search for effective cationic antimicrobial peptidomimetics targeting specific bacteria.

193 udopeptides have emerged as attractive small peptidomimetics that are capable of forming the characte

194 Herein, we review recent developments in peptidomimetics that are formed via heteroatom replaceme

195 ionships, we developed phenylimidazole-based peptidomimetics that are highly potent for Mtb20S.

196 -AApeptides are a new class of antibacterial peptidomimetics that are not prone to antibiotic resista

197 Here we present peptidomimetics that are very effective in stimulating t

198 describe Neoseptins, chemically synthesized peptidomimetics that bear no structural similarity to th

199 to focus our attention on short peptides or peptidomimetics that behave as LMWGs.

200 a-D-glucose have been employed to synthesize peptidomimetics that bind the SRIF receptors on AtT-20 m

201 gn, synthesis, and evaluation of macrocyclic peptidomimetics that bind to WD repeat domain 5 (WDR5) a

202 menable to the development of small molecule peptidomimetics that could be used to modulate NER repai

203 ogy emerging as pivotal tools for developing peptidomimetics that exhibit improved stability, specifi

204 ar weight drugs against NS3-4A are substrate peptidomimetics that have a similar binding and resistan

205 g monoclonal antibodies, fusion proteins and peptidomimetics that have been approved, that are underg

206 n order to obtain gold(III)-based anticancer peptidomimetics that might specifically target two pepti

207 elical structure at the interacting surface, peptidomimetics that reproduce the essential conformatio

208 A series of beta-diketone derivatives of RGD peptidomimetics that selectively bind to alphavbeta3 and

209 ped a set of TAT-based proteasome-activating peptidomimetics that stably penetrated the blood-brain b

210 he development of D-enantiomer antimicrobial peptidomimetics that target bacterial membranes of certa

211 bination of beta-diketone derivatives of RGD peptidomimetics that target cell surface integrins alpha

212 be taken into account in designing potential peptidomimetics that target P. gingivalis adherence and

213 date prodrugs (8-10) of phosphate-containing peptidomimetics that target the SH2 domain were synthesi

214 Similar to peptides and other peptidomimetics, these well-defined synthetic macromolec

215 ssess several features that are desirable in peptidomimetics; they are easily synthesized, fold into

216 our previously developed strategy of dimeric peptidomimetics to address the hypothesis that loop 4 sm

217 inhibitors ranging from small molecules and peptidomimetics to biologics.

218 Application of GPR114 TA peptidomimetics to EoL-1 cells stimulated cAMP productio

219 otective antibodies may facilitate design of peptidomimetics to focus vaccine responses on protective

220 The ability of these peptidomimetics to increase the binding of agonist N-pro

221 We report herein the capacity of sugar-based peptidomimetics to inhibit both Abeta1-42 early oligomer

222 rturbations would have on the ability of the peptidomimetics to modulate dopamine receptors.

223 present study, we designed a large number of peptidomimetics to target the MLL1/WDR5 interaction base

224 use of sequence-defined peptoids, a class of peptidomimetics, to achieve the accelerated calcite step

225 Upon testing in vitro, the peptidomimetics unexpectedly enhanced, rather than inhib

226 Developing peptidomimetics using hydrocarbon (HC)-stapling or other

227 iptase, we optimized ketobenzothiazole-based peptidomimetics using the P4-P3-P2-Arg-Kbt scaffold.

228 ylamido peptidomimetics and beta-turn cyclic peptidomimetics via "volatilizable" aminoalkyl functiona

229 ransferase, a series of imidazole-containing peptidomimetics was designed and synthesized, and their

230 for the synthesis of bicyclic 2-pyridones as peptidomimetics was developed.

231 structural variation of these antibacterial peptidomimetics was investigated as a tool for optimizin

232 ical interaction site for rational design of peptidomimetics was localized to the loop1/domain3 of th

233 Furthermore, both peptidomimetics were able to attenuate the Gpp(NH)p-indu

234 Taurine-containing water-soluble peptidomimetics were designed and synthesized.

235 These peptidomimetics were designed to examine the following:

236 These peptidomimetics were evaluated in vivo as modulators of

237 Beta-turn cyclic peptidomimetics were generated by intramolecular S(N)Ar

238 Peptidomimetics were observed to have significant oral t

239 Both the linear and the cyclic peptidomimetics were obtained with good to excellent yie

240 A series of vinyl sulfone-containing peptidomimetics were rationally designed, synthesized, a

241 These peptidomimetics were tested for their ability to enhance

242 The peptidomimetics were used at very low concentrations (10

243 Peptidomimetics where the 5-position of the imidazole ri

244 of the inhibitors that are on the market are peptidomimetics, where a conserved water molecule mediat

245 of this Pauli repulsion by employing common peptidomimetics, wherein the n --> pi* interaction is at

246 hese structures can facilitate the design of peptidomimetics which have been applied for example, as

247 completely new, previously unknown family of peptidomimetics, which are hydrolytically stable and dis

248 Our study led to the design of high-affinity peptidomimetics, which bind to WDR5 with K(i) < 1 nM and

249 resent a new generation of unnatural helical peptidomimetics, which have similar folding conformation

250 ysis of a novel class of heteroatom-modified peptidomimetics, which we shall call "oxyazapeptides".

251 affold was used for the preparation of model peptidomimetics, whose beta turn conformation was confir

252 hermore, optimization of the length of these peptidomimetics with an alternating cationic-hydrophobic

253 rovided two pairs of Pro-Leu-Gly-NH(2) (PLG) peptidomimetics with contrasting dopamine receptor modul

254 ro-Met-Leu resulted in the design of smaller peptidomimetics with enhanced affinity including Ac-pTyr

255 f Mfa1 and SspB and suggest that peptides or peptidomimetics with greater specific inhibitory activit

256 The "triazole scan" yielded peptidomimetics with improved resistance to enzymatic de

257 ch led to the development of ERF-VII derived peptidomimetics with modified N termini.

258 potential value in transforming peptides and peptidomimetics with N-CH(2)F, the very existence of thi

259 n producing biologically functional, helical peptidomimetics with non-natural elements, increased pro

260 Peptoids constitute a class of peptidomimetics with potential as protease resistant, bi

261 ioid receptor (DOR) antagonist bicyclic core peptidomimetics with promising analgesic activity and re

262 Low molecular weight peptidomimetics with simple amphiphilic sequences can he

263 sage of the technology to discover synthetic peptidomimetics with specific functions and reactivity.

264 c compounds 1b and 3b provided the first PLG peptidomimetics with the ability to decrease the binding

265 on, and conformational analysis of the first peptidomimetics with two pendant, chiral nitronyl nitrox