ライフサイエンスコーパス: covalent

1 g as a simple and straightforward method for covalent 2D patterning of graphene remains challenging.

2 actam antibiotics through the formation of a covalent acyl-enzyme intermediate followed by deacylatio

3 ize beta-lactams via a hydrolytically labile covalent acyl-enzyme intermediate.

4 fferent substrates, as well as structures of covalent acyl-enzyme intermediates of PGA with canonical

5 ) star polymer, we can tune the stiffness of covalent adaptable hydrogels using different wavelengths

6 t materials, such as self-healing materials, covalent adaptable networks (CANs) and vitrimers.

7 s accordingly employed in the fabrication of covalent adaptable networks (CANs) that possess tunable

8 Covalent adaptable networks (CANs), unlike typical therm

9 ase (UGT) superfamily typically catalyze the covalent addition of the sugar moiety from a UDP-sugar c

10 d urethane methacrylate precursor, which has covalent affinity to dental collagen, in the formation o

11 How non-covalent agonists activate the channel and whether coval

12 ate the channel and whether covalent and non-covalent agonists elicit the same physiological response

13 binofuranose and several rationally designed covalent alpha-l-arabinofuranosidase inhibitors were ana

14 to opposite faces of the porphyrin plane via covalent and coordination bonds, respectively.

15 class of bonds different than covalent/polar-covalent and ionic bonds.

16 nt agonists activate the channel and whether covalent and non-covalent agonists elicit the same physi

17 op more potent inhibitors through merging of covalent and non-covalent fragment hits; one series of l

18 multiple complex transformations exploiting covalent and non-covalent interactions.

19 al bases for NAAA function and inhibition by covalent and noncovalent agents; and finally, the potent

20 We investigated different covalent and noncovalent surface treatments (PEGMA, HEMA

21 een found to be widely applicable to dynamic covalent and supramolecular polymers.

22 ent degradation by noncovalent, irreversible covalent, and reversible covalent PROTACs, with <10 nM D

23 temperature (371 K) where the pristine, non-covalent assembly exists exclusively in a molecularly di

24 y when compared to that recorded for the non-covalent assembly.

25 We then imparted light sensitivity through covalent attachment of a synthetic glutamate-based photo

26 In this work, the covalent attachment of an amine functionalized metal-org

27 accessible upon pocket opening for selective covalent attachment of electrophilic ligands in eubacter

28 l modification is S-acylation, involving the covalent attachment of fatty acids to cysteine residues

29 PTMs involve the covalent attachment of functional groups to specific ami

30 ), a mitochondrial enzyme that catalyzes the covalent attachment of heme to c-type cytochromes.

31 Covalent attachment of sensing and reference membranes t

32 ttranslational modification characterized by covalent attachment of small ubiquitin-like modifier (SU

33 eptor that allows for the post-translational covalent attachment of targeting ligands at the T-cell s

34 The covalent attachment of the hybrid POM forms new nanocomp

35 troscopic mapping of the distribution of the covalent attachment revealed that activated 4-methoxyphe

36 he top of the E helix using a site-specific, covalent attachment.

37 netii, we found that four different types of covalent attachments occur between OM proteins and PG, w

38 th ambiguous reports of both dative Au-I and covalent Au-C contacts.

39 converting various interacting proteins into covalent binders, achieving specific covalent protein ta

40 Optimal conditions to get Tyr-Tyr covalent binding between invertase and the support were

41 ng specificity and molecular interactions of covalent binding drugs in a cellular environment.

42 ibodies and DNA, which undergo important non-covalent binding interactions, with the formation of ant

43 iles that exhibit irreversible or reversibly covalent binding mechanisms towards cysteine thiols and

44 represents a valuable moiety that can induce covalent binding of an inhibitor to its target.

45 zed by two key molecular properties: (1) non-covalent binding to an antibody-based therapeutic, and (

46 st non-fluorescent chemical probe has a fast covalent binding with carbonyl moieties at neutral pH to

47 were introduced to specific biomolecules by covalent binding.

48 rime candidates for in vitro and in vivo non-covalent bioconjugation, for imaging and delivery applic

49 fused to a protein of interest, enabling the covalent biotin labeling of proteins and subsequent capt

50 The mutational disruption of covalent bond formation between the receptor and the tar

51 Here, we report that covalent bond formation by an aryl sulfonyl fluoride ele

52 trophiles that only become activated towards covalent bond formation on binding a specific protein.

53 ACs is driven by reversible binding prior to covalent bond formation, while the reversible covalent P

54 recombinant (r)C0C7 domains is achieved by a covalent bond formed between SpyCatcher (-sc; encoded at

55 the use of new thermodynamically controlled covalent bond forming methods.

56 ectrophiles that are recognized by TRPA1 via covalent bond modifications of specific cysteine residue

57 ative dissociation and subsequently catalyze covalent bond rearrangement, affording selective assembl

58 system that rapidly forms a highly specific covalent bond to its cognate catcher linked to the grid

59 lpha-selective galactosylations by forming a covalent bond to the anomeric carbon in dioxolenium-type

60 out of the ribosome exit tunnel, after their covalent bond to transfer-RNA has been broken, has not b

61 orbital-types are spatially coincident, the covalent bond-pairing is weakened by Pauli-repulsion wit

62 tor proteins' with a spectrum of heterolytic covalent-bond-forming activity (that is, reacting divers

63 Current cell-wall models assume no covalent bonding between cellulose and hemicelluloses su

64 Our work bridges the gap between covalent bonding taking place at an atomic level and col

65 We show that Ln can engage in covalent bonding with boron, and, in some members of the

66 hydrophobicity of the protein such that non-covalent bonding within network was modified.

67 interfacial interaction mechanisms of Ti-O-C covalent bonding, sliding of MXene nanosheets, and pai-p

68 self-healing mechanisms involving reversible covalent bonding, supramolecular chemistry, or polymers

69 improves the molecular anchoring by forming covalent bonds between molecular carbon and copper surfa

70 ed along polymer chains, is used to activate covalent bonds in mechanosensitive molecules (mechanopho

71 two dimensional sheets held together through covalent bonds which are then stacked together through n

72 ible formation and breaking of rather strong covalent bonds within molecules under certain external s

73 ork polymers typically crosslinked by strong covalent bonds.

74 Acalabrutinib is a selective, covalent Bruton tyrosine-kinase inhibitor with activity

75 Remibrutinib (LOU064) is a novel covalent BTK inhibitor that binds an inactive BTK confor

76 of PROTACs and develop RC-1 as a reversible covalent BTK PROTAC with a high target occupancy as its

77 The non-covalent capture of olive pheromones inside the beta-cyc

78 We demonstrated covalent cellulose-xyloglucan bonding in plant cell wall

79 henolics may complex with starch through non-covalent CH-pai bonds along alpha-(1 -> 4) glycosidic ch

80 rily require a metal-ligand bond with highly covalent character, and that interactions between organi

81 Strong covalent chemical bonds that can also be reversed, cleav

82 Covalent chemical modifications of cellular RNAs directl

83 -based protein profiling, which makes use of covalent chemical probes for labeling the active site an

84 ling the amount of water, the influence of a covalent chemical process on noncovalent aggregates can

85 or more forms of stimuli-responsive, dynamic covalent chemistries as a means to transition their beha

86 changed are the subject of so-called dynamic covalent chemistry (DCC).

87 Dynamic covalent chemistry (DCvC) describes systems in which rea

88 covalent monolayers mainly utilizes dynamic covalent chemistry (DCvC), which relies on the reversibl

89 A dynamic covalent chemistry approach was used for the stereoselec

90 In this study, we introduce a new dynamic covalent chemistry based on siloxane equilibrium exchang

91 cover that cyano-acrylamide-based reversible covalent chemistry can significantly enhance the intrace

92 that mimic these attributes using reversible covalent chemistry for base-pairing pose unique syntheti

93 While, initial recruiters have utilized non-covalent chemistry for protein binding, very recently co

94 llectively, we describe SuTEx as a versatile covalent chemistry with broad applications for chemical

95 Click Chips) by synergistically integrating covalent chemistry-mediated EV capture/release, multimar

96 networks (CANs) that possess tunable dynamic covalent chemistry.

97 Here we show that topoisomerase 1-DNA covalent cleavage complex (TOP1cc) is both necessary and

98 ins, we synthesized UBE2K-Ub and UBE2K-Ub(2) covalent complexes and analyzed E2 interactions with the

99 Several new structures of non-covalent complexes of PGA with different substrates, as

100 ing metabolite found is isocaproyltaurine, a covalent conjugate of a distinctive C. difficile ferment

101 to time and cost saving post-translational, covalent conjugation of recombinant proteins in plants.

102 alphaM) superfamily use thiol esters to form covalent conjugation products upon their proteolytic act

103 re a unique materials platform that combines covalent connectivity, structural regularity, and molecu

104 Appreciable covalent contributions to the metal-ligand bonds were de

105 h we attribute to partial graphitization and covalent coupling between PDA subunits during annealing.

106 concanavalin A agarose beads or directly via covalent coupling of free amines on the enzyme surface w

107 en shown to recognize epitopes formed by the covalent cross-linking of proinsulin and secretory granu

108 ng byssus fabrication, achieved by oxidative covalent cross-linking or formation of metal coordinatio

109 the tissue surface, followed by physical and covalent cross-linking with the tissue surface.

110 th mucin forming a network structure via non-covalent cross-links between mucin chains.

111 es the toughness and 3 times the strength of covalent crosslinked PSeD elastomers, while maintaining

112 difficult, or chemical modification, such as covalent crosslinking of DNA strands.

113 We utilize a covalent crosslinking probe to trap transient interactio

114 otein whose polypeptide chains are linked by covalent crosslinks.

115 le and membrane-bound proteins exists as non-covalent dimers, trimers, and higher-order oligomers.

116 We further showed that covalent disulfide adducts of this residue promote autop

117 r the eIF4E cap binding site, we developed a covalent docking approach focused on lysine.

118 (b) Some non-covalent drug-protein complexes rely on rather affine bi

119 Small molecule covalent drugs provide desirable therapeutic properties

120 allenges and solutions in the development of covalent drugs, including the use of an alpha-fluoroacry

121 With a resurgence in interest in covalent drugs, there is a need to identify new moieties

122 2 to 12, which to our knowledge is the first covalent eIF4E inhibitor with cellular activity.

123 chemistry for protein binding, very recently covalent engagement to novel E3's has proven fruitful in

124 alent PROTACs drive degradation primarily by covalent engagement.

125 ls targeting of a cytotoxic agent, through a covalent enzyme inhibitor that is detrimental to tumor t

126 As nucleotidyl transferases, formation of a covalent enzyme-adenylate intermediate is a common first

127 Here we generated covalent enzyme-substrate complexes of DNMT3A and DNMT3B

128 control, the design and synthesis of dense, covalent extended solids has been a longstanding challen

129 These include covalent FBDD, FBDD for the stabilization of proteins or

130 which are then stacked together through non-covalent forces.

131 hibitors through merging of covalent and non-covalent fragment hits; one series of low-reactivity, tr

132 its; one series of low-reactivity, tractable covalent fragments were progressed to discover improved

133 higher dimensionality COFs, paves the way to covalent frameworks composed of hierachical chemical str

134 both current main approaches-tether-directed covalent functionalization and supramolecular masks-the

135 In this context, the covalent fusion of GNRs and porphyrins (Pors) is a highl

136 ne bindings and have a similar appearance as covalent hapten-protein adducts.

137 o the polysaccharide hyaluronan (HA) to form covalent HC.HA complexes, thereby stabilizing an extrace

138 chrome c, which we assign to the presence of covalent heme-protein bonds.

139 We also present additional results on covalent homodimerization through disulfide formation of

140 ns into a short polymer block leading to non-covalent, hydrophobic interactions with the lipid bilaye

141 Finally, we demonstrate that important covalent, i.e., spin pairing, reactivity modes can be mi

142 n order to provide functional groups for the covalent immobilization of the biological recognition el

143 for a variety of applications, including the covalent inhibition of protein targets and dynamic combi

144 cribe our efforts to develop a selective SRC covalent inhibitor by targeting cysteine 277 on the P-lo

145 new opportunity for small-molecule targeted covalent inhibitor design.

146 t of MFH290, a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13.

147 ent candidate MRTX849 as a potent, selective covalent inhibitor of KRAS(G12C) is described.

148 ve UCHL1 probe (IMP-1710) to date based on a covalent inhibitor scaffold and apply this probe to iden

149 nt hits revealed binding hotspots, while the covalent inhibitor structure-activity relationship enabl

150 As an irreversible covalent inhibitor, compound 15a exhibited sustained inh

151 Now, with the success of allele-specific covalent inhibitors against the most frequently mutated

152 by fungi grown on complex biomass, potential covalent inhibitors and probes which mimic alpha-l-arabi

153 Targeted covalent inhibitors are currently showing great promise

154 ible protein target recognition and binding, covalent inhibitors irreversibly modify a proximal nucle

155 tein crystallography demonstrated 8 and 9 as covalent inhibitors of hOAT, which exhibit two distinct

156 emical assays show that, on binding Bz-LL or covalent inhibitors, MtClpP1P2 undergoes a conformationa

157 design and optimization of cysteine-targeted covalent inhibitors.

158 et class coverage and application of FBDD to covalent inhibitors.

159 y and optimization of selectiveand effective covalent inhibitors.

160 The subsequent covalent integration of antibodies generates interfaces

161 OI) through a modular SNAP-Tag/benzylguanine covalent interaction.

162 enormous potential, in which attractive non-covalent interactions between a chiral catalyst and the

163 atalysis, where reactions rely on reversible covalent interactions between an organic substrate and a

164 lts more from stabilizing intramolecular non-covalent interactions in the secondary coordination sphe

165 ave previously been synthesized by using non-covalent interactions to assemble and entangle molecular

166 ceptors which bind carbohydrates through non-covalent interactions, mimicking the strategies used in

167 a structural basis for their high-affinity, covalent interactions.

168 transformations exploiting covalent and non-covalent interactions.

169 ugh the encoding of adaptable, plug-and-play covalent interfaces.

170 sparaginases proceeds through formation of a covalent intermediate, as observed previously for EcAII.

171 yrimidine ring of ectoine through an unusual covalent intermediate, N-alpha-2 acetyl-l-2,4-diaminobut

172 he formation of fibrinogen hydrogels through covalent intermolecular crosslinking.

173 , reversible covalent (RC), and irreversible covalent (IRC) binders, affects the degradation of Bruto

174 Using covalent labeling and mass spectrometry, we measure the

175 rotein HOS analysis, through which different covalent labeling approaches "mark" the solvent accessib

176 All of these covalent labeling approaches combine to constitute a pro

177 review, we provide a structured overview of covalent labeling approaches for nucleic acids and highl

178 iples, mechanisms, and applications of these covalent labeling approaches.

179 rresolution fluorescence microscopy based on covalent labeling highlights specific proteins and has s

180 nd-directed acyl imidazole chemistry enables covalent labeling of AMPA-type glutamate receptors in th

181 ns in Env glycoprotein on the viral surface, covalent labeling of the Cys residues using a Cys-reacti

182 us labeling concepts that have been devised, covalent labeling provides the most stable linkage, an u

183 aptive behavior within the generated dynamic covalent libraries (DCLs) was revealed, providing in-dep

184 ling for in-depth proteome-wide analysis and covalent ligand discovery.

185 ponse despite concomitant degradation of the covalent ligand/Hsp90 complex.

186 egy for developing selective lysine-targeted covalent ligands.

187 and allows selections in the presence of non-covalent ligands.

188 The covalent linkage allowed overcoming solubility problems

189 Thus, the covalent linkage concept offers several advantages, espe

190 ACPs) an acyl chain of a specific length for covalent linkage to the protoxin.

191 s indicate that tyrosine can undergo stable, covalent linkages in fibrillar fibronectin under inflamm

192 Drug candidates that form covalent linkages with their target proteins have been u

193 Owing to strong covalent linkages, drilling fluids that were formulated

194 Covalent long-range ordered (crystalline) sheets called

195 some cases even unprecedented properties for covalent materials, such as self-healing materials, cova

196 oGEF method to systematically evaluate every covalent mechanophore reported to date and compare the p

197 M-808 represents a promising, covalent menin inhibitor for further optimization and ev

198 These disulfides can be converted to covalent metal-thiolate bonds by exposure to free thiols

199 ble approach to the development of novel non-covalent methods of binding, retention, and release of a

200 However, covalent Michael adduct formation with Cys-18, a residue

201 epoxide and aziridines and demonstrate their covalent modification and time-dependent inhibition of G

202 ted photocatalytic process that introduces a covalent modification at a C(sp(3))-H bond in the methyl

203 rimary human T cells that are susceptible to covalent modification by electrophilic small molecules.

204 rolled environments, or functionalization or covalent modification of reagents.

205 c acetal groups are installed through direct covalent modification of the dextran.

206 redox-sensitive cysteine residues that, upon covalent modification, can allosterically regulate kinas

207 ctionality to the monomer structures through covalent modification, or through the use of new thermod

208 cules and form adducts known as nonenzymatic covalent modifications (NECMs).

209 genomic enhancers and promoters, but also by covalent modifications added to both chromatin and RNAs.

210 By contrast, the various covalent modifications added to RNAs, termed epitranscri

211 nisms of bacteria, while phages have evolved covalent modifications as a counterdefense mechanism to

212 ependent redox changes can mediate transient covalent modifications of cysteine thiols to modulate th

213 o protect their genomes from R-M cleavage by covalent modifications, such as the hydroxymethylation a

214 tive group with the discovery of a selective covalent modifier of adenosine deaminase (ADA).

215 dered covalent organic frameworks (COFs) and covalent monolayers have shown great potential in a broa

216 The synthesis of COF thin films and covalent monolayers mainly utilizes dynamic covalent che

217 This model was validated by using synthetic covalent MSA-2 dimers, which were potent agonists.

218 The covalent nature of the B-C bonding results in a hard, in

219 sses containing complex anions, and in which covalent network formation is minimized, may exhibit pad

220 present a strategy of interfacially bridging covalent network within tobacco mosaic virus (TMV) virus

221 Dynamic covalent networks (DCvNs) are increasingly used in advan

222 cellular mechanisms that regulate mRNA fate, covalent nucleotide modification has emerged as a major

223 s challenging due to their inherently strong covalent or ionic bonding, which usually leads to materi

224 n approach of using reversible interactions (covalent or noncovalent) becomes challenging, especially

225 nding in CSBs does not arise from either the covalent or the ionic structures of the bond, but rather

226 eper insight into the imine bond dynamics of covalent organic cages, we studied the formation and exc

227 sis of a novel two-dimensional corrole-based covalent organic framework (COF) by reacting the unusual

228 n a novel highly crystalline two-dimensional covalent organic framework (COF), COF-616, bearing pre-i

229 Herein, we report a truxenone-based covalent organic framework (COF-TRO) as cathode material

230 the synthesis of a vinylene-linked (-CH=CH-) covalent organic framework, COF-701, directly from aceto

231 2D covalent organic frameworks (2D COFs) are a unique mater

232 tructures are very common in two-dimensional covalent organic frameworks (2D COFs).

233 and rich functionality, structurally ordered covalent organic frameworks (COFs) and covalent monolaye

234 Covalent organic frameworks (COFs) are an emerging class

235 Covalent organic frameworks (COFs) are an emerging class

236 Covalent organic frameworks (COFs) are commonly synthesi

237 Covalent organic frameworks (COFs) are highly modular po

238 Three-dimensional (3D) covalent organic frameworks (COFs) are rare because ther

239 ro and mesopores into two-dimensional porous covalent organic frameworks (COFs) could enhance the exp

240 2D covalent organic frameworks (COFs) could have well-defin

241 we have been exploring the applicability of covalent organic frameworks (COFs) for water harvesting

242 f highly crystalline, porous, and stable new covalent organic frameworks (COFs) have been developed b

243 Ester-linked, crystalline, porous covalent organic frameworks (COFs) have been synthesized

244 Covalent organic frameworks (COFs) have entered the stag

245 irradiation of the 2D poly(arylenevinylene) covalent organic frameworks (COFs) results in topologica

246 blocks allowed the construction of two rare covalent organic frameworks (COFs) with high crystallini

247 While many covalent organic frameworks (COFs)-extended, covalently

248 Nanoscale imine-linked covalent organic frameworks (nCOFs) were first loaded wi

249 materials, such as graphene and single layer covalent organic frameworks (sCOFs) are being widely stu

250 ctrode, which is superior to the reported 2D covalent organic frameworks and most carbon nitride mate

251 Covalent organic frameworks are an emerging class of por

252 Covalent organic frameworks offer a molecular platform f

253 nted for the synthesis of crystalline porous covalent organic frameworks via topology-templated polym

254 e weaves(2-16) include isotropic crystalline covalent organic frameworks(12-14) that feature rigid he

255 lymers (also classified as 2D pai-conjugated covalent organic frameworks) and 2D pai-conjugated metal

256 ype materials, metal-organic frameworks, and covalent organic frameworks.

257 administrated in immune-humanized mice, the covalent PD-1(FSY) exhibited strikingly more potent anti

258 mer nicks one of the DNA strands and forms a covalent phosphotyrosyl bond with the 5' end.

259 nstitute a new class of bonds different than covalent/polar-covalent and ionic bonds.

260 Then, the linear covalent polymer (P) was synthesized by polymerization o

261 Macrocycle-containing covalent polymer networks have begun to attract attentio

262 tants from water using macrocycle-containing covalent polymer networks.

263 The devices exploit a bioresorbable dynamic covalent polymer that facilitates tight bonding to itsel

264 the polysaccharides by the formation of non-covalent polysaccharides-OE complexes.

265 e several known reversible PRMT6 inhibitors, covalent PRMT6 inhibitors have not been reported.

266 pyrimidine (CP) group, respectively, to give covalent products.

267 ovalent bond formation, while the reversible covalent PROTACs drive degradation primarily by covalent

268 compounds may pave the way for the design of covalent PROTACs for a wide variety of challenging targe

269 part of the degradation by our irreversible covalent PROTACs is driven by reversible binding prior t

270 Reversible covalent PROTACs potentially offer the best of both worl

271 alent, irreversible covalent, and reversible covalent PROTACs, with <10 nM DC(50)'s and >85% degradat

272 al scaffolds, change of mechanism of action (covalents, PROTACs), increases in blood-brain barrier pe

273 The potential of covalent protein drugs, however, remains unexplored due

274 ive therapeutics (PERx) approach to generate covalent protein drugs.

275 ns into covalent binders, achieving specific covalent protein targeting for biological studies and th

276 The covalent protein-ligand linkage enabled structural chara

277 ry, reversible noncovalent (RNC), reversible covalent (RC), and irreversible covalent (IRC) binders,

278 tion is demonstrated as an efficient dynamic covalent reaction in phosphate buffers at neutral pH.

279 e and dihydroquinazoline moieties capable of covalent reaction with cysteine.

280 lization of a fluoride leaving group (LG) in covalent reactions of sulfonyl fluorides and arylfluoros

281 e MPC complex by binding to C54 of MPC2 in a covalent reversible manner that can be quantified in cel

282 t the tethers and subsequent cleavage of the covalent ring/thread ester linkages.

283 With the help of an electrostatics-aided covalent self-assembly approach, we demonstrate efficien

284 this, we outline an electrostatics-enhanced covalent self-assembly strategy to generate polymer-prot

285 ly neutralize its oncogenic activity using a covalent stapled-peptide inhibitor.

286 SIM) in the TOC159 GTPase domain and a SUMO3 covalent SUMOylation site in the membrane domain.

287 ng challenges in the prospering field of non-covalent surface functionalization.

288 s give guidance to the planning of a dynamic covalent synthesis by predicting time to maximum yield o

289 an attractive bottom-up approach for the non-covalent synthesis of nascent axial organic heterostruct

290 onal tool in tuning self-assembling, dynamic covalent systems.

291 Finally, we demonstrate selective covalent targeting of cellular Hsp90, which results in a

292 o overcome these challenges, we envisioned a covalent targeting strategy.

293 mer stabilization depends on the site of the covalent tether and the nature of the protein-fragment i

294 li, Braun's lipoprotein (Lpp) forms the only covalent tether between the OM and PG and is crucial for

295 We exemplify the power of covalent tethering using the naturally occurring truncat

296 rity of clinical candidates and FDA approved covalent therapies.

297 o the alpha-amino terminus without forming a covalent thioester intermediate.

298 sumptions about the spontaneous formation of covalent thiol-metal bonds.

299 erials, imparting electrical conductivity to covalent three-dimensional organic polymers is challengi

300 issociation energies and dissociation modes (covalent vs ionic), as well as alteration of molecular g