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1 th c(RGDfK), a well-studied integrin-binding peptidomimetic.
2 ne and side chain torsion angles for a model peptidomimetic.
3 ning and refining therapeutically-attractive peptidomimetics.
4 al properties of this peptide by introducing peptidomimetics.
5 tives are valuable pharmacological agents as peptidomimetics.
6 e introduced as the backbone modification in peptidomimetics.
7 nthesis of biologically active molecules and peptidomimetics.
8 advantage of peptoids over other families of peptidomimetics.
9 ess to obtain the linear C-hydroxyalkylamido peptidomimetics.
10 synthesized and assayed libraries of mutant peptidomimetics.
11 n the design of conformationally constrained peptidomimetics.
12 chromenopyridine fused thiazolino-2-pyridone peptidomimetics.
13 ential applications in the field of peptides/peptidomimetics.
14 lent opportunity to construct small-molecule peptidomimetics.
15 development of new small antiviral drugs or peptidomimetics.
16 ioisostere to provide protease resistance in peptidomimetics.
17 rious ligands including TRP/NTL peptides and peptidomimetics.
22 Bicyclic peptidomimetic 7 and spirobicylic peptidomimetic 8 enhanced the binding of [3H] N-propylno
27 l pain conditions and to test potency of the peptidomimetic agonists in vivo, we evaluated these agon
29 y of conformationally restrained dipeptides, peptidomimetics, alkaloids, and other biologically activ
31 coated either with an alphavbeta3-selective peptidomimetic, an alpha5beta1-selective peptidomimetic,
36 is for developing gp120 dual inhibitors into peptidomimetic and increasingly smaller molecular weight
38 ovides structural rigidity within the cyclic peptidomimetic and promotes the creation of a stabilizin
39 458 binding was saturatable, displaceable by peptidomimetic and small molecule gamma-secretase inhibi
40 hput synthesis of linear C-hydroxyalkylamido peptidomimetics and beta-turn cyclic peptidomimetics via
41 es a concrete basis for the design of potent peptidomimetics and nonpeptidic compounds to inhibit MLL
43 -HIV-1 drug target and may help in designing peptidomimetics and small molecule drugs targeted to thi
44 derived from the C-terminal tail of FGF23 or peptidomimetics and small-molecule organomimetics of the
45 cellular uptake in cancer cells by designed peptidomimetics and suggest that cancer cells with certa
46 of rhodesain inhibitors, including peptidic, peptidomimetic, and nonpeptidic structures, emphasizing
47 ional active site and allosteric inhibitors, peptidomimetics, and novel proteolysis-targeted chimera
51 resent good candidates for further design of peptidomimetic antagonists capable of blocking the fusio
58 ligohydrazide (azatide) fragments into their peptidomimetic arms to reduce hydrophobicity and increas
60 nactive peptide, administration of the SOCS1 peptidomimetic at either early or advanced stages of dia
61 fluoromethyl aldimines, small psi[CH(CF3)NH]-peptidomimetic backbones can be achieved in which a new
62 zed, and pharmacologically characterized new peptidomimetics based on a PLEV tetrapeptide scaffold de
63 CB-TE1A1P-PEG4-LLP2A), a high-affinity VLA-4 peptidomimetic-based radiopharmaceutical, was evaluated
64 crown-6 (18C6) affinities of nine protonated peptidomimetic bases are determined using guided ion bea
65 tics for neutral and protonated 18C6 and the peptidomimetic bases, as well as the proton bound comple
66 tests the hypothesis that the conjugation of peptidomimetic beta-secretase inhibitors with a fragment
68 proapoptotic agent bone metastasis-targeting peptidomimetic (BMTP-11) in preclinical models of primar
69 nalyses revealed that the most potent cyclic peptidomimetic bound to the iNOS binding site of SPSB2 w
70 ERG inhibitory peptides (EIPs) and derived peptidomimetics bound ERG with high affinity and specifi
73 viously discovered anti-alphaVbeta3 integrin peptidomimetic (c(AmpRGD)) and the clinically approved a
75 in the low micromolar range, rivaling other peptidomimetic calpain inhibitors and presenting an impr
76 meostasis, and we suggest that ANXA1 and its peptidomimetics can be novel therapeutic targets in neur
80 o the surfaces and the alphavbeta3-selective peptidomimetic-coated nanotopographies promoted osteogen
81 leads to (i) a chemical library of putative peptidomimetics combining diverse azaheterocycles with t
83 cribe the assembly of an achiral oligo(urea) peptidomimetic compound into supramolecular helices.
84 rin extracellular fragment in complex with a peptidomimetic compound that was previously shown to par
85 r the rational design of specific and potent peptidomimetic compounds that may be useful for the trea
86 of the BCL-2 family of proteins, we designed peptidomimetic compounds using a benzoylurea scaffold to
90 latelets are less responsive to peptides and peptidomimetics containing an arginine-glycine-aspartic
92 TTT-28, a newly synthesized thiazole-valine peptidomimetic, could reverse ABCB1-mediated MDR in vitr
95 Tyr(All) and similar residues in peptide and peptidomimetic cyclizations performed on solid phase.
97 se compounds may be useful in the context of peptidomimetic design of biologically relevant compounds
98 tor conformations suitable for computational peptidomimetic design, and that inclusion of disordered
99 review aims to outline useful tools towards peptidomimetic design, spanning from local modifications
104 ce for the development of other peptidic and peptidomimetic drugs such as inhibitors of the blood clo
105 ts for SAR campaigns, integral components of peptidomimetic drugs, and potential drugs on their own.
106 evelopment has been complicated, as for many peptidomimetic drugs, mostly by poor drug-like propertie
107 A pyridine-enabled C-N bond activation of peptidomimetics employing cooperative palladium/copper c
108 etic and SLE model studies demonstrated that peptidomimetic FISLE-412,1 a reduced HIV protease inhibi
109 unique, selective, and potent small molecule peptidomimetic, FISLE-412, which neutralizes anti-dsDNA/
110 e mediated hydrolysis enabled preparation of peptidomimetic fluorophores with useful photophysical pr
113 minimalist scaffold for novel stereodefined peptidomimetic foldamers and topologically biased librar
114 toids are an increasingly important class of peptidomimetic foldamers comprised of N-alkylglycine uni
118 aim of using the tumor-homing cyclo[DKP-RGD] peptidomimetics for site-directed delivery of the cytoto
119 e present the synthesis of highly active RGD peptidomimetics for the alphavbeta3 integrin with remark
120 ve recently emerged as important examples of peptidomimetics for their interesting complexing propert
123 Optimization of our previously described peptidomimetic furin inhibitors was performed and yielde
124 be potentiated by NO signaling, therefore, a peptidomimetic furoxan was tested in hippocampal slices
128 ethod can be used to prepare imidazole based peptidomimetics, herein exemplified by the synthesis of
129 s and provides a guide for further design of peptidomimetic HIV-1 inactivators based on the PT pharma
130 gets for anticancer therapy, and a number of peptidomimetic IAP antagonists have entered clinical tri
132 ation of co-crystal structures of two potent peptidomimetics in complex with WDR5 establishes their s
133 c quantities, which can be exploited through peptidomimetics in diabetes or Alzheimer's disease.
135 g in a single process generating the desired peptidomimetics in good to excellent yields within a 25
136 ution studies of radiolabeled multi-triazolo-peptidomimetics in mice bearing receptor-positive tumor
141 y demonstrated the eutomer (3S,5R)-5 to be a peptidomimetic inhibitor binding to a nonsubstrate topog
145 east cancer cells, and targeting BCL6 with a peptidomimetic inhibitor leads to apoptosis of these cel
146 ear receptor corepressor 1 (NCoR) complex by peptidomimetic inhibitor not only significantly decrease
147 -principle, we developed a small, selective, peptidomimetic inhibitor of Ena/VASP EVH1 domain interac
148 escribe the design of a potent and selective peptidomimetic inhibitor of geranylgeranyltransferase I
149 d that zinc ion and a Michael acceptor-based peptidomimetic inhibitor synergistically inactivate FIPV
150 show that 19a is a novel potential antitumor peptidomimetic inhibitor that can be used as a starting
151 was found to be as potent as OM00-3, a known peptidomimetic inhibitor, 4-fold more selective toward b
152 e specific BCL6 inhibitor retro-inverso BCL6 peptidomimetic inhibitor-induced expression of BCL2 and
154 ing studies were conducted using a series of peptidomimetic inhibitors (compounds 1-6, Table 3) and t
155 molecular dynamics to model structures of 12 peptidomimetic inhibitors bound to the SH2 domain of STA
156 he dominant interface with small molecule or peptidomimetic inhibitors could specifically prevent act
159 pathways predictive of tumors responsive to peptidomimetic inhibitors of its 20S core protease activ
161 ign, synthesis, and evaluation of reversible peptidomimetic inhibitors of Plm II as potential antimal
162 The mode of inhibition for phosphoramidate peptidomimetic inhibitors of prostate-specific membrane
163 streamlined approach for discovering potent peptidomimetic inhibitors of protein-protein interaction
165 ied the factors affecting the selectivity of peptidomimetic inhibitors of the highly homologous prote
166 have designed a class of potent macrocyclic peptidomimetic inhibitors of the menin-MLL1 interaction.
167 n, synthesis, and characterization of cyclic peptidomimetic inhibitors of the SPSB2-iNOS interaction
168 y have been exploited in discovering related peptidomimetic inhibitors of the Tat-TAR interaction in
175 ugh binding to the neonatal Fc receptor, the peptidomimetic introduces cross-species binding to cell
181 (LLP2A) is a high-affinity, high-specificity peptidomimetic ligand (inhibitory concentration of 50% =
182 ching a synthetic high-affinity and specific peptidomimetic ligand (LLP2A) against integrin alpha4bet
183 PEG4-LLP2A ([(64)Cu]-LLP2A), a high affinity peptidomimetic ligand for very late Ag-4 (VLA-4; also ca
184 rmacological delivery of a soluble ephrin-A1 peptidomimetic ligand led to a reduction in EphA2 expres
185 injection of a (64)Cu-labeled high-affinity peptidomimetic ligand referred to as (64)Cu-LLP2A, which
186 This study investigates whether CN2097, a peptidomimetic ligand which targets the synaptic scaffol
187 luated 2 conjugates of a high-affinity VLA-4 peptidomimetic ligand, LLP2A, for PET/CT imaging in a su
193 inoline scaffold and show that the resulting peptidomimetics maintain the desired pharmacological pro
194 the basis for the development of functional peptidomimetic materials responsive to external stimuli.
195 ogen receptor-coregulator interactions using peptidomimetics may be a viable therapeutic approach for
196 type of proteolytically stable FPR2-specific peptidomimetics may serve as valuable tools for future a
199 ed drug design and optimization, macrocyclic peptidomimetic molecules bearing both a lipophilic P2 is
200 resentative of a new class of PSMA targeting peptidomimetic molecules that shows great promise as ima
201 r group chemically modified an antimicrobial peptidomimetic motif for targeted applications against c
202 lls are sensitive in vitro to ABT-263, a BH3-peptidomimetic, much more than the other tested cancer c
204 array comprising different types of cationic peptidomimetics obtained by a general monomer-based soli
205 We delivered dPGS-PTX in combination with a peptidomimetic of the anti-angiogenic protein thrombospo
211 atility and ease of structural modification, peptidomimetic oligomers have not yet been explored exte
213 lecule for the preparation of collections of peptidomimetics or biologically active compounds based o
215 inal heptapeptide, P7 (Ac-1FTLDADF7) and its peptidomimetic P6 (1Fmoc(Me)PhgLDChaDF7) bound to Saccha
217 2) (2-f-LIGRLO-NH(2)) underscores the use of peptidomimetic PAR(2) ligands as a mechanism to enhance
221 ttractive intermediates for the synthesis of peptidomimetics, polyheterocycles, and other multifuncti
224 Here, we describe how small peptide and peptidomimetic probes derived from the lipid binding dom
227 tems in Lepidoptera and aid in the design of peptidomimetics, pseudopeptides or small molecules capab
229 hat 6 out of all 8 possible stereoisomers of peptidomimetic pyrrolidines can be obtained in good yiel
232 Incorporation of unnatural amino acids and peptidomimetic residues into therapeutic peptides is hig
234 A series of opioid analogues with a common peptidomimetic scaffold displayed remarkable inversions
236 that, through N-acetylation of our original peptidomimetic series, we are able to improve DOR affini
238 ex with PBP 5 in complex with a boronic acid peptidomimetic shows that the position corresponding to
239 nd evaluated the therapeutic efficacy of the peptidomimetic small molecule ICG-001, which specificall
240 t the poor mimicry of the amide bond by many peptidomimetics stems from their inability to partake in
241 quence-defined family of oligomers, enable a peptidomimetic strategy, especially considering the easi
244 of drugs as they accept a large spectrum of peptidomimetics such as beta-lactam antibiotics, antivir
250 he Win motif-WDR5 interaction, we designed a peptidomimetic that binds WDR5 (Kd approximately 3 nm) a
251 gated it to an electrophilic derivative of a peptidomimetic that binds with high affinity and specifi
252 we have recently reported an imidazole-based peptidomimetic that has shown PCSK9 inhibitory activity
253 ion with new or approved beta-lactams, and a peptidomimetic that have entered full clinical developme
254 ared with cilengitide, an integrin-targeting peptidomimetic that performed poorly in recent clinical
255 Herein, we review recent developments in peptidomimetics that are formed via heteroatom replaceme
257 -AApeptides are a new class of antibacterial peptidomimetics that are not prone to antibiotic resista
258 describe Neoseptins, chemically synthesized peptidomimetics that bear no structural similarity to th
260 gn, synthesis, and evaluation of macrocyclic peptidomimetics that bind to WD repeat domain 5 (WDR5) a
261 menable to the development of small molecule peptidomimetics that could be used to modulate NER repai
262 ar weight drugs against NS3-4A are substrate peptidomimetics that have a similar binding and resistan
263 g monoclonal antibodies, fusion proteins and peptidomimetics that have been approved, that are underg
264 n order to obtain gold(III)-based anticancer peptidomimetics that might specifically target two pepti
265 he development of D-enantiomer antimicrobial peptidomimetics that target bacterial membranes of certa
266 be taken into account in designing potential peptidomimetics that target P. gingivalis adherence and
267 ibody and phage particles bearing a molinate peptidomimetic, the EI performed with an IC(50) of 0.15
269 ssess several features that are desirable in peptidomimetics; they are easily synthesized, fold into
271 otective antibodies may facilitate design of peptidomimetics to focus vaccine responses on protective
272 We report herein the capacity of sugar-based peptidomimetics to inhibit both Abeta1-42 early oligomer
273 present study, we designed a large number of peptidomimetics to target the MLL1/WDR5 interaction base
274 ylamido peptidomimetics and beta-turn cyclic peptidomimetics via "volatilizable" aminoalkyl functiona
278 structural variation of these antibacterial peptidomimetics was investigated as a tool for optimizin
284 of the inhibitors that are on the market are peptidomimetics, where a conserved water molecule mediat
285 of this Pauli repulsion by employing common peptidomimetics, wherein the n --> pi* interaction is at
286 completely new, previously unknown family of peptidomimetics, which are hydrolytically stable and dis
287 Our study led to the design of high-affinity peptidomimetics, which bind to WDR5 with K(i) < 1 nM and
288 resent a new generation of unnatural helical peptidomimetics, which have similar folding conformation
289 ysis of a novel class of heteroatom-modified peptidomimetics, which we shall call "oxyazapeptides".
290 affold was used for the preparation of model peptidomimetics, whose beta turn conformation was confir
291 characterization of this new thiazole-valine peptidomimetic will facilitate design and synthesis of a
292 , we report here for the first time a linear peptidomimetic with three triazole insertions in its bac
293 hermore, optimization of the length of these peptidomimetics with an alternating cationic-hydrophobic
294 rovided two pairs of Pro-Leu-Gly-NH(2) (PLG) peptidomimetics with contrasting dopamine receptor modul
296 n producing biologically functional, helical peptidomimetics with non-natural elements, increased pro
298 ioid receptor (DOR) antagonist bicyclic core peptidomimetics with promising analgesic activity and re
299 c compounds 1b and 3b provided the first PLG peptidomimetics with the ability to decrease the binding
300 on, and conformational analysis of the first peptidomimetics with two pendant, chiral nitronyl nitrox