ライフサイエンスコーパス: semisynthetic

1 design and synthesis of structurally defined semisynthetic adaptors we refer to as "switch" molecules

2 ave developed a method of discriminating two semisynthetic aequorin variants from one another using t

3 Acylfulvenes (AFs) are a class of semisynthetic agents with high toxicity toward certain t

4 ielding six-step convergent synthesis of the semisynthetic alkaloid (-)-perhydrohistrionicotoxin is d

5 Semisynthetic aminoglycoside derivatives may provide a m

6 -50 binding and competition experiments with semisynthetic aminoglycosides and neomycin B and tobramy

7 ction of GM1 ganglioside, whereas LIGA 20, a semisynthetic analog of GM1, substantially reduced both

8 Epothilone B (BMS-247550) is a semisynthetic analog of the natural product epothilone B

9 BMS-247550 is a semisynthetic analog of the natural product epothilone B

10 stem analysis for the S(2) site of KcsA, its semisynthetic analog, and valinomycin yields the free en

11 ounds have served as the starting points for semisynthetic analogs with improved properties.

12 ination drugs containing artemisinin (or its semisynthetic analogs), known as artemisinin combination

13 led that metabolites 2-4 and, in particular, semisynthetic analogue 5, are strong growth inhibitors o

14 tive CRPC cell line, with paclitaxel and its semisynthetic analogue docetaxel decreases expression of

15 n a previous report, a seven-membered D-ring semisynthetic analogue of cyclopamine, IPI-269609 (2), w

16 TNP-470, a semisynthetic analogue of fumagillin, was studied in vit

17 using the folate ligand to target a potent, semisynthetic analogue of the microtubule inhibitor tubu

18 6-Hydroxymethylacylfulvene (MGI-114) is a semisynthetic analogue of the toxin illudin S, a product

19 nd resistance have led to efforts to prepare semisynthetic analogues (i.e., KW-2149 (3), BMS-181174 (

20 macrolide antibiotic erythromycin A and its semisynthetic analogues have been among the most useful

21 Semisynthetic analogues such as FK973 (3) and FK317 (4)

22 ealth, chemists have succeeded in generating semisynthetic analogues that sometimes overshadow the or

23 de series, 6, 7, 10, 11, 20, and 22, and the semisynthetic analogues, 30, 31, 33, and 36, inhibit con

24 Intensive semisynthetic and biosynthetic efforts have been directe

25 ts replenished the arsenal of antibiotics by semisynthetic and to a lesser degree fully synthetic rou

26 atural product family, including biomimetic, semisynthetic, and de novo synthetic strategies.

27 N-Benzyladriamycin-14-valerate (AD 198) is a semisynthetic anthracycline with experimental antitumor

28 We demonstrate that the resultant semisynthetic anti-idiotype peptibodies kill tumor cells

29 ronan shows promise as an example of a novel semisynthetic anti-inflammatory molecule.

30 ) that are an important source of natural or semisynthetic anticancer drugs.

31 Several semisynthetic antimitotic alkaloids are emerging as poss

32 methylacylfulvene (HMAF; MGI 114) is a novel semisynthetic antitumor agent derived from the sesquiter

33 erpene indole alkaloid (MIA) used to produce semisynthetic antitumor drugs.

34 he production of paclitaxel, specifically, a semisynthetic approach and the application of biocatalys

35 This semisynthetic approach is likely to be applicable to the

36 The semisynthetic approach relies on the solid-phase peptide

37 route to produce betaMdeltaVL, an efficient semisynthetic approach that employs high-yielding chemic

38 Utilizing our recently published semisynthetic approach to the (3'S)-K-252a diastereomer,

39 different acyl tails were synthesized via a semisynthetic approach.

40 es for PglC, PglJ, and PglB are prepared via semisynthetic approaches.

41 rse structures not accessible by traditional semisynthetic approaches.

42 ss toward the goal of developing a supply of semisynthetic artemisinin based on production of the art

43 The semisynthetic artemisinin derivatives such as artesunate

44 present a complete process for production of semisynthetic artemisinin.

45 ents, and limited proteolysis assays on this semisynthetic ATP-linked protein, we have obtained uniqu

46 ly stable oxime linkage to furnish the first semisynthetic bacterial-based immunogen construct target

47 resent study, we describe a novel library of semisynthetic bile acid derivatives obtained by modifica

48 ndogenous bile acids and currently available semisynthetic bile acids are poorly selective toward GP-

49 y chromophore substitution experiments using semisynthetic bilin monoamides, which indicate that the

50 This was further confirmed using a semisynthetic biotinylated p300 HAT domain that could be

51 em, we tested a library of bioengineered and semisynthetic borrelidin analogs for their antimalarial

52 from dihydroartemisinin, a small array of 16 semisynthetic C-10 pyrrole Mannich artemisinin derivativ

53 Herein, we disclose a semisynthetic, catalytic approach for structure diversif

54 wiss, Phadia and Siemens) with and without a semisynthetic CCD blocker with minimized potential for n

55 However, recent work using a semisynthetic channel that is unable to adopt a constric

56 ibilities for combinatorial biosynthesis and semisynthetic chemistry because of the introduction of f

57 hen combinatorial biosynthesis is coupled to semisynthetic chemistry.

58 We show that these semisynthetic, circularly permuted acetylated proteins r

59 This tubulin-binding semisynthetic compound is a selective and potent anti-br

60 Here we explored the capability of a semisynthetic compound to intercept mTOR signaling.

61 mycins has been shown to produce a series of semisynthetic compounds, the dihydropacidamycins, with a

62 nus of the nisin A/B ring system to generate semisynthetic constructs that display potent inhibition

63 A strategy for the preparation of semisynthetic copper(II)-based catalytic metalloproteins

64 determine the DNA-binding specificity of the semisynthetic covalent DNA-binding polyamide tallimustin

65 discovery of IPI-926 (compound 28), a novel semisynthetic cyclopamine analogue with substantially im

66 We generated 100 different semisynthetic data sets for each F-ratio and evaluated t

67 he approach was validated through the use of semisynthetic data, which was a combination of real envi

68 if spaced closely), as we demonstrate using semisynthetic datasets, performing ChIP-seq for the TF T

69 in mice of natural product gossypol and its semisynthetic derivative apo-gossypol, compounds that bi

70 s to examine whether GM1 ganglioside and its semisynthetic derivative LIGA20 activate various neurotr

71 PG490-88, a semisynthetic derivative of a novel compound PG490 (trip

72 PG490-88 is a water soluble, semisynthetic derivative of a novel compound PG490 (trip

73 PG490-88, a semisynthetic derivative of PG490 (triptolide, present i

74 lide, a constituent of PG27) and PG490-88 (a semisynthetic derivative of PG490) suppressed rejection

75 adin-Darby canine kidney epithelial cells: a semisynthetic derivative of quinocarmycin (also known as

76 47, 6alpha-ethyl-chenodeoxycholic acid) is a semisynthetic derivative of the primary human bile acid

77 cal evaluation of crocin 1, safranal and its semisynthetic derivatives as selective inhibitors of fiv

78 Using suvanine as a novel hit, a library of semisynthetic derivatives has been designed and prepared

79 ir effectiveness as antifungal agents, three semisynthetic derivatives have been developed and approv

80 to further probe the mechanism of action, 19 semisynthetic derivatives of gedunin were prepared and t

81 ied conductance behavior in a membrane using semisynthetic derivatives of the ion-channel-forming pep

82 of a new class of anticancer agents that are semisynthetic derivatives of the mushroom toxin illudin

83 ities of a number of related metabolites and semisynthetic derivatives revealed key features required

84 hibit bacterial protein synthesis, and their semisynthetic derivatives, such as dalfopristin-quinupri

85 gues of the insect molting hormone and their semisynthetic derivatives, were tested for their activit

86 nts, and larger glycosaminoglycans and their semisynthetic derivatives.

87 nthetic means or modifications by late-stage semisynthetic derivatization in ways that enhance their

88 The structure was elucidated through the semisynthetic derivatization of starting material via ch

89 an analogue class presently inaccessible by semisynthetic derivatization of the natural product, by

90 By using semisynthetic 'designer' chromatin containing H2B-Ub bea

91 taining 5% sucrose polybehenate was fed in a semisynthetic diet to rats and mice.

92 l, and control diet C was a standard AIN-76A semisynthetic diet which is lower in fat content and hig

93 Rats were fed semisynthetic diets containing either juniper berry oil,

94 ice and studied on both low-fat and high-fat semisynthetic diets.

95 umor cell population following exposure to a semisynthetic dimerizing ligand, AP20187.

96 al malaria, development of clinically useful semisynthetic drugs for severe and complicated malaria (

97 lex has 350-500-fold lower activity than the semisynthetic enzyme produced by peptide ligation.

98 As the viral structure ensures semisynthetic enzymes remain linked to the genetic seque

99 biochemical platform for engineering de novo semisynthetic enzymes, functionally modular and widely s

100 ent the need for cultivation of mayapple and semisynthetic epimerization and demethylation of podophy

101 We demonstrated the generality of semisynthetic epitope construction with 13 diverse kinas

102 one, 17beta-trenbolone, for the nonsteroidal semisynthetic estrogen agonist, alpha-zearalanol, and th

103 Ethinyl estradiol is a semisynthetic estrogen compound found in birth control p

104 Flavopiridol is a novel semisynthetic flavone derivative of the alkaloid rohituk

105 Although flavopiridol, a semisynthetic flavone, was initially thought to be a spe

106 Flavopiridol is a semisynthetic flavonoid that inhibits cyclin-dependent k

107 ate, chondroitin sulfate A, heparin, and the semisynthetic fully sulfated chondroitin sulfate, FSCS,

108 GABA-Snifit is a semisynthetic fusion protein containing the GABA(B) rece

109 conformation of the carboxyl terminus of the semisynthetic G protein, we applied high resolution solu

110 ted a marked loss of signal intensity in the semisynthetic Galpha subunit but not in free peptide sub

111 tion in a more native system, we generated a semisynthetic Galpha subunit, site-specifically labeled

112 A semisynthetic gene encoding the entire protein sequence

113 Our method, using semisynthetic GFP as a readout, is facile, sensitive, la

114 Oritavancin is an investigational semisynthetic glycopeptide with potent in vitro activity

115 ncomycin; some of the most promising include semisynthetic glycopeptides, quinupristin-dalfopristin,

116 ased on phosphorylation-mediated assembly of semisynthetic green fluorescent protein (GFP).

117 Semisynthetic green fluorescent proteins (GFPs) can be p

118 pombe and chromatin substrates that contain semisynthetic H2Bub1.

119 pH 7.4 than is artelinic acid (1), a leading semisynthetic, herb-derived antimalarial trioxane drug c

120 We have prepared semisynthetic histone H3 acetylated at Lys-115 and/or Ly

121 cleosomes reconstituted from recombinant and semisynthetic histones on barcoded DNA prior to immunopr

122 d in the rest of the PLA(2), we have created semisynthetic human group IB PLA(2) in which the N-termi

123 of the protein folding behavior reveals that semisynthetic Im7 analogues are well suited for protein

124 mino-17-demethoxygeldanamycin (17-AAG)1 is a semisynthetic inhibitor of the 90 kDa heat shock protein

125 naptic factors, we developed and validated a semisynthetic inhibitory network that approximates simul

126 acid (GLCA) (its glycine conjugate), and the semisynthetic isomers, 7alpha-OH- and 12alpha-OH-cholano

127 Using the semisynthetic KcsA and KvAP channels, we show that block

128 wo-dimensional infrared (2D IR) spectra of a semisynthetic KcsA channel with site-specific heavy ((13

129 uctural studies based on chemically modified semisynthetic KcsA channels along the selectivity filter

130 Importantly, MD simulations reveal that the semisynthetic KcsA(D-ala77) channel can adopt an asymmet

131 tivity of this conjugate as well as of other semisynthetic lipid A derivatives was also reported.

132 Oritavancin is a semisynthetic lipoglycopeptide analogue of vancomycin th

133 Telavancin is a semisynthetic lipoglycopeptide derivative of vancomycin.

134 overed in 2000 and became the first marketed semisynthetic lipoglycopeptide in 2009.

135 The TEM precursor and several semisynthetic lipopeptide TEM derivatives showed rapid b

136 properties of sdAbs, we constructed a large, semisynthetic llama sdAb library.

137 We now report a series of semisynthetic LMB derivatives showing substantially impr

138 Solithromycin (1), a third-generation semisynthetic macrolide discovered by combinatorial copp

139 particular, ketolides, a promising class of semisynthetic macrolides with activity against erythromy

140 Semisynthetic, mechanism-based protein inhibitors of ubi

141 e typically collected from cultures grown in semisynthetic medium in vitro.

142 Here, we present a semisynthetic method for preparing mammalian thioredoxin

143 Here we report a site-specific, semisynthetic method for the production of bispecific an

144 Herein we report a semisynthetic method of producing membrane-anchored prot

145 N(alpha)-acetylated alpha-syn first using a semisynthetic methodology based on expressed protein lig

146 e of molecules that would be inaccessible by semisynthetic methods (presently the only means of tetra

147 The development of semisynthetic methods for the site-specific introduction

148 Semisynthetic modification of 1 provided several analogs

149 Semisynthetic modification of its glycolic acid subunit

150 Aside from accessible semisynthetic modifications of existing functional group

151 of sulfation was confirmed using a panel of semisynthetic modified heparins with variable levels of

152 Functional characterization of the folded semisynthetic NaK channels indicates that it is function

153 he recombinant peptide thioester to form the semisynthetic NaK polypeptide.

154 Development of exosome-based semisynthetic nanovesicles for diagnostic and therapeuti

155 Acylfulvenes comprise a family of semisynthetic natural product derivatives with potent an

156 Here, we show that a semisynthetic nontoxic tubulin-binding agent, 9-bromonos

157 end, we covalently associated LSD1-CoREST to semisynthetic nucleosomal particles.

158 developed an unnatural base pair (UBP) and a semisynthetic organism (SSO) that imports the constituen

159 ird base pair would lay the foundation for a semisynthetic organism with an expanded genetic code and

160 plications and also lay the foundation for a semisynthetic organism with an expanded genetic code.

161 ions and would also lay the foundation for a semisynthetic organism.

162 a coli, thus making the world's first stable semisynthetic organism.

163 eveloped a physiological microenvironment of semisynthetic origin, called gelatin methacryloyl (GelMA

164 alization studies and functional analyses of semisynthetic PEGylated Rab1, Rab5, Rab7, and Rab35 prot

165 al cysteine side-chain protection in the two semisynthetic peptide substrates, we were able to rule o

166 or potentially useful for the preparation of semisynthetic peptides and proteins incorporating charge

167 ed a method of targeting idiotype by using a semisynthetic personalized therapeutic that is more prac

168 Here we describe "semisynthetic" pH-sensitive protein conjugates with orga

169 We used a semisynthetic phage display human antibody library to ra

170 ized immunoglobulin products, or transfusing semisynthetic platelet substitutes (thromboerythrocytes,

171 A new series of semisynthetic pleuromutilin derivatives were synthesized

172 ped for measuring nanogram concentrations of semisynthetic pneumocandin antifungal agents in human pl

173 Semisynthetic pneumocandin L-733,560 was conjugated to s

174 ida albicans mutants resistant to the potent semisynthetic pneumocandin L-733,560.

175 ul for quantitating plasma levels of related semisynthetic pneumocandins including clinical candidate

176 Semisynthetic polymers and polysaccharides as sources of

177 Such semisynthetic preparation of sex pheromones is a novel a

178 hat will facilitate ongoing efforts on their semisynthetic preparation.

179 oter failed to activate transcription from a semisynthetic promoter, and this failure was not due to

180 ld not be activated by receptor; whereas the semisynthetic protein demonstrated functionality that wa

181 The resulting semisynthetic protein has enhanced affinity for the expr

182 potential for FRET between mixtures of these semisynthetic proteins.

183 of the streptamine ring of other natural or semisynthetic pseudodisaccharide aminoglycoside scaffold

184 Our design originates a vast class of semisynthetic rare-cleaving DNA nickases, which are esse

185 tivity of individual kinases, we developed a semisynthetic reaction scheme, which results in the affi

186 Thus, this semisynthetic reassembly process offers a general route

187 .A pair is replaced with inosine (I) in both semisynthetic ribozymes and oligonucleotide mimics of th

188 Rifampin, a semisynthetic rifamycin, is the cornerstone of current t

189 Among many semisynthetic rifamycins, benzoxazinorifamycins have gre

190 satile biocatalyst that converts an array of semisynthetic roquefortine C derivatives bearing indolin

191 f the de novo route complements the existing semisynthetic route from chlorophylls and should enable

192 rotein folding pathways, we have developed a semisynthetic route toward the immunity protein Im7.

193 cated reaction sequence into widely utilized semisynthetic routes to next generation Taxol (paclitaxe

194 we use expressed protein ligation to produce semisynthetic SAHH acetylated at Lys(401) and Lys(408) a

195 ve used an experimental approach utilizing a semisynthetic scheme that employs native chemical ligati

196 The semisynthetic scheme was also employed to construct a va

197 A novel semisynthetic scheme was developed to couple amine-react

198 Minocycline is a semisynthetic second-generation tetracycline that exerts

199 hod allows production of a fully functional, semisynthetic selenoenzyme that is amenable to structure

200 The performance of these semisynthetic sensor proteins makes them attractive for

201 A novel semisynthetic sequence to QS-7-Api has also been establi

202 g structure-based design, we generated a new semisynthetic series of spectinomycin analogs with selec

203 Biological evaluation of these semisynthetic sesquiterpene lactone derivatives in HeLa

204 xpressed protein ligation, we have generated semisynthetic SHP-1 proteins containing phosphotyrosine

205 regulation by phosphorylation, we generated semisynthetic site-specifically tetra-phosphorylated PTE

206 ong our 22 collected naturally occurring and semisynthetic stilbenic compounds, significantly attenua

207 A novel, entirely carbohydrate, semisynthetic STn-polysaccharide (PS) A1 conjugate was p

208 Here, we describe chemical and semisynthetic strategies for site-specific incorporation

209 Our semisynthetic strategy for generating site-specifically

210 lenges, we developed a general and efficient semisynthetic strategy that enables the site-specific in

211 We describe here a semisynthetic strategy to identify inhibitors based on t

212 A semisynthetic strategy to obtain monophosphoryl lipid A

213 Here, we describe a general semisynthetic strategy to obtain these oligoribonucleoti

214 e development and application of a versatile semisynthetic strategy, based on a combination of sortas

215 cium to the group A component of natural and semisynthetic streptogramin mixtures is a prerequisite f

216 Although several successful semisynthetic studies have been performed to elucidate s

217 of 2-debenzoyl-7,13-diacetylbaccatin III, a semisynthetic substrate, to 7,13-diacetylbaccatin III, a

218 These semisynthetic substrates were evaluated as Csk substrate

219 alphaHL pores with one semisynthetic subunit were then used as nanoreactors for

220 A second semisynthetic system is also reported that makes use of

221 The semisynthetic tail-phosphorylated Csk showed evidence of

222 for new antibiotics has been met largely by semisynthetic tailoring of natural product scaffolds dis

223 Docetaxel is a semisynthetic taxane, a class of anticancer agents that

224 plored because of limitations in traditional semisynthetic techniques.

225 Minocycline is a semisynthetic tetracycline derivative with activity agai

226 bial low doses of the commercially available semisynthetic tetracycline doxycycline, have been used i

227 Minocycline is a semisynthetic tetracycline with antiinflammatory propert

228 Minocycline, a semisynthetic tetracycline, has been shown to be neuropr

229 We now report that minocycline, a semisynthetic tetracycline, recently shown to have neuro

230 Semisynthetic tetracyclines used in the adjunctive treat

231 We produced the semisynthetic thioredoxin reductase with a total yield o

232 This novel semisynthetic translation system is a powerful tool for

233 (efficacy/toxicity) as that of water-soluble semisynthetic trioxane artelinic acid (5).

234 The semisynthetic triterpenoid 2-cyano-3,12-dioxooleana-1,9(

235 esized and chemically characterized a novel, semisynthetic triterpenoid derivative, 3-cinnamoyl-11-ke

236 Semisynthetic triterpenoids such as bardoxolone methyl (

237 g them with synthetic tRNAs, we formulated a semisynthetic tRNA complement for all 20 amino acids.

238 ine 1 and to the carrier protein KLH to form semisynthetic vaccine 2.

239 The semisynthetic version of thioredoxin reductase that we p

240 Vinorelbine (Navelbine), an amphiphilic semisynthetic Vinca alkaloid, has displayed superior act

241 The semisynthetic vitamin E derivative alpha-tocopheryloxyac

242 Chlorophyllin, a mixture of semisynthetic, water-soluble derivatives of chlorophyll

243 ivity relationships, we obtained natural and semisynthetic withanolides 1, 2a, 2c, and 3-36 and compa

244 t properties of self-assembled structures of semisynthetic zinc chlorins (ZnChls) in the solid state