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1 cleavage for the release of the biologically active metabolite.
2 d in biotransformation of clopidogrel to its active metabolite.
3 as the site of covalent modification by the active metabolite.
4 enhance the conversion of clopidogrel to its active metabolite.
5 ation of flutamide and hydroxyflutamide, its active metabolite.
6 e key enzyme required to convert PQ into its active metabolite.
7 ndex, and PK by plasma levels of prasugrel's active metabolite.
8 er to deplete bioactive retinoids or to form active metabolites.
9 oxide metabolites produced by FMOs are often active metabolites.
10 amount of drug available for conversion into active metabolites.
11 te a response to endogenously produced redox-active metabolites.
12 e more deterministically assembled than less active metabolites.
13 thotrexate, and pemetrexed to produce highly active metabolites.
14 production of toxins and other biologically active metabolites.
15 alysis to determine the presence of possible active metabolites.
16 ting that this could be attributed to highly active metabolites.
17 ene (CYP2D6), oxidizes tamoxifen to its most active metabolites.
18 ct possible parent compounds that might have active metabolites.
19 leoside analogues into powerful biologically active metabolites.
25 2) and 4.15 hours, respectively; whereas the active metabolite 17-aminogeldanamycin had a t(1/2) of 7
26 -hydroxyvitamin D(3) (25(OH)D(3)) and/or its active metabolite, 1alpha,25-dihydroxyvitamin D(3) (1,25
27 aptohept-4-enoic acid moiety to generate the active metabolite 2, which is an extraordinarily potent
29 assive apoptosis-1 (PRIMA-1) and its primary active metabolite, 2-methylene-3-quinuclidinone (MQ), ca
35 tate (NNN-5'-OAc), a stable precursor of the active metabolite 5'-hydroxy(+/-)-N'-nitrosonornicotine
37 inhibition in yields of the physiologically active metabolite 5alpha-dihydrotestosterone (DHT) in HG
38 nts, but intracellular accumulation of their active metabolites (6-thioguanine nucleotides, 6-TGN) ca
39 drolysis of the glucuronide conjugate of the active metabolite 7-ethyl-10-hydroxycamptothecin (SN-38)
40 omide was dosed to a targeted blood level of active metabolite, A77 1726, of 50 microg/ml to 100 micr
41 drug class would enhance liver levels of the active metabolite adefovir diphosphate (ADV-DP) and/or d
44 vitamin A to enzymes for metabolism into an active metabolite, all-trans retinoic acid (atRA), where
46 ur results showed that the production of the active metabolite (AM) from 2-oxoclopidogrel by human li
47 formation of a glutathionyl conjugate of the active metabolite (AM) of clopidogrel and the covalent m
48 cement of an anti-METH scFv for METH and its active metabolite amphetamine (AMP), through the introdu
49 ed biotransformation of clopidogrel into its active metabolite and decreased efficacy of clopidogrel
51 n by comparison of its induction between the active metabolite and its parent compound (B[a]PDE versu
52 nverted in rat or mouse plasma solely to two active metabolites and had significantly enhanced oral b
54 CYP)1A2, which converts clopidogrel into its active metabolite, and prior studies suggest greater inh
55 tion, decreases plasma levels of clopidogrel active metabolite, and retards and diminishes its effect
56 s with long-term adjuvant therapy, examining active metabolites, and considering chemoprevention all
57 rate this point, we use the example of redox-active metabolites, and in particular phenazines, which
58 ities recently entering the marketplace have active metabolites, and many more are (or have been) in
61 hine lowers the plasma levels of clopidogrel active metabolite as well as its effects on platelets.
63 to C(64)H(104)O(33) and the putatively found active metabolite at m/z 1283.58 [M + formic-H](-) corre
64 uted uracil analogue is converted to several active metabolites but the mechanism of cytotoxicity has
66 Clopidogrel requires transformation into an active metabolite by cytochrome P-450 (CYP) enzymes for
68 n attenuate metabolism of clopidogrel to its active metabolite by inhibiting various hepatic CYP450 e
69 l and prasugrel require biotransformation to active metabolites by cytochrome P450 (CYP) enzymes.
71 eudomonas aeruginosa produces colorful redox-active metabolites called phenazines, which underpin bio
73 lts show that modulating extracellular redox-active metabolites can influence the fitness of a biofil
74 Ceftaroline fosamil, the prodrug form of the active metabolite ceftaroline, is a new broad-spectrum p
78 sitivity of RZx (~ 53 mV/pH), secreted redox-active metabolites/compounds from whole cells are likely
79 ; P=0.47), despite yielding higher prasugrel active metabolite concentration (ng/mL; 62.3+/-82.6 vers
80 d with chewed prasugrel, which led to higher active metabolite concentration but not greater IPA comp
81 genesis in in vitro studies and implies that active metabolites contribute to its in vivo pharmacolog
83 next-generation hypomethylating agent whose active metabolite decitabine has a longer in-vivo exposu
85 The area under the curve for clopidogrel active metabolite decreased significantly with esomepraz
86 ucoma drugs tested only metipranolol and its active metabolite, desacetylmetipranolol, blunted the SN
88 9 alleles have significantly lower levels of active metabolite, diminished platelet inhibition, and h
89 inistration resulted in the formation of the active metabolite, diminution of tumor vasculature, and
90 technique that can detect hundreds of redox-active metabolites down to the level of femtograms on co
91 supplementation on the formation of flavour active metabolites during wine fermentation, we evaluate
92 n situ monitoring of the production of redox-active metabolites (e.g., pyocyanin) during the course o
93 umor activity of ICT2588 was superior to its active metabolite, exhibiting reduced toxicity, improved
97 s have demonstrated that triphosphate is the active metabolite for both these purine nucleoside analo
98 analog inhibitors, including the clinically active metabolite formed by sofosbuvir, to elucidate key
99 mercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel
100 t even the spontaneous release of NPY (or an active metabolite) from recurrent mossy fibers is suffic
101 18 to be more efficiently converted into its active metabolite, gemcitabine triphosphate (dFdCTP), an
102 ducts proved useful in the identification of active metabolites generated by either in vitro or in vi
103 has been associated with reduced clopidogrel active metabolite generation and higher ex vivo platelet
104 f a PPI with clopidogrel reduces clopidogrel active metabolite generation and subsequent platelet inh
106 h attenuates CYP2D6 metabolism and increases active metabolite half-lives and may therefore lead to s
107 and compared the effect of bupropion and its active metabolite hydroxybupropion on mouse homomeric 5-
108 Preferential hydrolysis of ICT2588 to its active metabolite (ICT2552) was observed in tumor homoge
109 ecent findings have identified lactate as an active metabolite in cell signalling, although its effec
110 ate are made available for the generation of active metabolites in platelets when the NEFA binding ca
111 earthworms possess a class of unique surface-active metabolites in their gut, which we term 'drilodef
113 ir in plasma, and tenofovir diphosphate, the active metabolite, in cervical tissue and dried blood sp
114 lethal and sub-lethal doses of TCBZ and its active metabolites, in order to collect EVs and evaluate
116 ion with dithiothreitol, confirming that the active metabolite is linked to a cysteinyl residue of CY
118 oped to release the doxorubicin-formaldehyde active metabolite, is tethered via derivatized ethylene
119 elta(9)THC) is metabolized to only one major active metabolite, it has been reported that several maj
120 report here that nitazoxanide (NTZ) and its active metabolite kill replicating and nonreplicating M.
121 (SC-51) is rapidly converted in vivo to the active metabolite L-N6-(1-iminoethyl)lysine (L-NIL).
122 ibed natural substance largazole (1) and its active metabolite largazole thiol (2) is described.
123 (TDM), which involves measurement of drug or active metabolite levels and anti-drug antibodies, is a
124 ogrel have significantly reduced clopidogrel active metabolite levels and high on-treatment platelet
125 ent data have surfaced demonstrating altered active metabolite levels of clopidogrel in patients harb
127 the way for further developing the NL-loaded active metabolites, M2 or M13, as novel targeted therape
130 ment (thionamides such as carbimazole or its active metabolite methimazole are the drugs of choice).
131 TGN) are currently being considered as major active metabolites, methylthioinosine nucleotides seem t
133 neurons, and behavioral changes due to TLR4 active metabolite, morphine-3-glucuronide (M3G) exposure
135 omilast and roflumilast; the latter (and its active metabolite N-oxide) is more selective and potent
137 dies have reported that both nitrate and its active metabolite, nitrite, have therapeutic activity in
139 like cycloguanil, however, 1a (WR99210), the active metabolite of 1, has retained in vitro potency ag
142 lves 1-methyl-4-phenylpyridinium (MPP+), the active metabolite of 1-methyl-4-phenyl-1,2,3,6-tetrahydr
143 levels of albendazole sulfoxide (ASOX), the active metabolite of albendazole, are highly variable am
144 stance to monodesethylamodiaquine (MDAQ; the active metabolite of AQ) than to CQ, whereas a pfcrt all
145 Benzo[a]pyrene diol epoxide (BPDE), the active metabolite of benzo[a]pyrene present in tobacco s
149 reduction of 32.4% in plasma exposure to the active metabolite of clopidogrel, as compared with nonca
150 allele had significantly lower levels of the active metabolite of clopidogrel, diminished platelet in
151 strated that cordycepin 5'-triphosphate, the active metabolite of cordycepin, can be formed not only
152 Almost 30% of the variability in SN-38 (the active metabolite of CPT-11) AUC is explained by ABCC1 1
153 With the combination therapy of SN-38 (the active metabolite of CPT-11) followed by flavopiridol, t
154 sensor, which emits light in response to the active metabolite of cytosine arabinoside (ara-C, cytara
155 l variability in blood concentrations of the active metabolite of dabigatran etexilate and influence
157 e is metabolised to monomethyl fumarate, the active metabolite of dimethyl fumarate, reduces circulat
158 , we show that 20-hydroxyecdysone (20E), the active metabolite of ecdysone that is induced by environ
159 hosphorylase (PNP) that locally converts the active metabolite of F-araAMP to a highly diffusible sub
160 tions and in complex with norfluoxetine, the active metabolite of fluoxetine (Prozac) and a state-dep
161 ecently demonstrated that FTY-phosphate, the active metabolite of FTY720, acts as a full agonist for
164 ure to cytotoxic concentration of SN-38, the active metabolite of irinotecan (0.1 microM) alone and i
165 Their response to oxaliplatin, to SN38, the active metabolite of irinotecan (drugs active in colon c
166 nized anti- Trop-2 antibody, conjugated with active metabolite of irinotecan (SN-38), on Trop-2 posit
167 a synergistic activity of 5c with SN-38 (the active metabolite of irinotecan) and 5-fluorouracil on c
168 platin, 5-fluorouracil (5-FU), or SN-38 (the active metabolite of irinotecan) induced Notch-1 intrace
169 d 7-ethyl-10-hydroxycamptothecin (SN-38; the active metabolite of irinotecan), two S-phaseselective a
170 porter that confers resistance to SN-38 (the active metabolite of irinotecan), was readily detected i
173 y 7-ethyl-10-hydroxycamptothecin (SN-38), an active metabolite of irinotecan, in p53-null compared wi
174 how for the first time that SN38, the potent active metabolite of irinotecan, induces c-Jun NH(2)-ter
182 Prior studies suggest that A77 1726, the active metabolite of leflunomide, inhibits the activity
183 lpropanolamine (PPA) (1) and ST-1059 (2, the active metabolite of midodrine), supporting the hypothes
184 ncentrations of mycophenolic acid (MPA), the active metabolite of MMF, and outcomes in 85 patients wi
187 d the effect of mycophenolic acid (MPA), the active metabolite of mycophenolate mofetil, on erythropo
188 etoprofen, etodolac, and nabumetone) and the active metabolite of nabumetone (6-methoxy-2-naphthylace
189 7,8,9,10-tetrahydro benzo[a]pyrene (BPDE, an active metabolite of PAHs) induced cytotoxicity, mutagen
192 4 inhibitor roflumilast N-oxide (RNO) is the active metabolite of roflumilast approved as a treatment
194 ulated that concentrations of endoxifen, the active metabolite of tamoxifen, are a better predictor o
196 optimization, to improve the binding of the active metabolite of the anti-inflammatory drug leflunom
197 cy are comparable or superior to MRE269 (the active metabolite of the clinical compound NS-304) with
198 possible to demonstrate that vedelianin, an active metabolite of the family of prenylated stilbenes
201 ound to gemcitabine diphosphate (GemdP), the active metabolite of the mechanism-based chemotherapeuti
202 1-Methyl-4-phenylpyridinium (MPP(+)), the active metabolite of the neurotoxin 1-methyl-4-phenyl-1,
203 oxide homeostasis and suggest that it is an active metabolite of the organic nitrates that can be us
204 in-2-yl)phenyl)-3-(pyridin-4-yl)urea (2), an active metabolite of the potent PI3 kinase inhibitor PKI
208 a role of endogenous retinoic acid (RA), the active metabolite of vitamin A in the initial differenti
209 herein that all-trans-retinoic acid (RA), an active metabolite of vitamin A that is known to induce m
211 unctionality.IMPORTANCE ATRA, a biologically active metabolite of vitamin A, exerts pleiotropic biolo
215 tem (CNS) the function of retinoic acid, the active metabolite of vitamin A, is best understood from
216 Retinoic acid (RA), the main biologically active metabolite of vitamin A, is known to promote gut
217 effect of all-trans retinoic acid (ATRA), an active metabolite of vitamin A, on the neuropathology an
219 All-trans-retinoic acid (atRA), the major active metabolite of vitamin A, plays a role in many bio
227 hus, we investigated the role of calcitriol (active metabolite of vitamin D) in the regulation of Th9
229 study, we hypothesized that the biologically active metabolite of vitamin D, 1,25(OH)2D3, inhibits hu
233 amin D3 (1alpha,25(OH)2D3), the biologically active metabolite of vitamin D3 To further investigate t
234 1,25-Dihydroxyvitamin D3 [1,25(OH)2D3], the active metabolite of vitamin D3, inhibits the proliferat
235 iously we demonstrated that the biologically active metabolites of 17beta-oestradiol, 2-hydroxyoestra
236 op1cc in biochemical assays, we propose that active metabolites of 4NQO trap Top1cc by forming DNA ad
238 A major mode of metabolism of the major active metabolites of TAM, 4-OH-TAM and endoxifen, is by
239 hylhexyl phthalate (MEHP) is one of the main active metabolites of the plasticizer di(2-ethylhexyl) p
240 provide comparable systemic exposure to the active metabolites of the prior, stable tetrabenazine re
241 ing compounds for the synthesis of the other active metabolites of these PAHs thought to be involved
243 ts produce an enormous array of biologically active metabolites, often with stereochemical variations
244 the peak plasma concentration of clopidogrel active metabolite (omeprazole > esomeprazole > lansopraz
246 Plasma concentrations of CI-1040 and its active metabolite, PD 0184264, increased in a less than
249 logic profile and its ability to deliver two active metabolites, potentially simplifying HCV treatmen
250 cessed by dendritic cells and T cells to the active metabolite, providing a mechanism for the local r
252 the high functional versatility of the redox-active metabolite pyocyanin and the susceptibility of ar
257 tration to mice and Wistar rats generated an active metabolite recovered from the rodent's brains.
259 ssential: they process the vitamins to their active metabolites (retinoic acid and 1,25(OH)(2)D3) for
260 is known about the role of vitamin A and its active metabolite, retinoic acid (RA) in host defenses a
262 SK 256066, roflumilast, and its biologically active metabolite roflumilast N-oxide generally potentia
263 ral levels of the prodrug irinotecan and its active metabolite SN-38 compared with free irinotecan.
264 ed PEG conjugates of the irinotecan (CPT-11) active metabolite SN-38 via a phenyl ether that release
268 ntrations of tenofovir, emtricitabine, their active metabolites (tenofovir diphosphate [TFVdp] and em
270 umatic fluorescent drug leflunomide into its active metabolite teriflunomide through isoxazole ring o
271 lized in rats, but MDC is the only centrally active metabolite that could contribute to overall effec
272 50 (CYP) metabolic activation to produce the active metabolite that inhibits the platelet P2Y(1)(2) a
273 l molecules would benefit the study of redox-active metabolites that are produced by microbial biofil
274 h agents undergo intracellular processing to active metabolites that disrupt RNA and DNA metabolism.
275 Clopidogrel is a prodrug anticoagulant with active metabolites that irreversibly inhibit the platele
276 omics results helped to prioritize potential active metabolites that modulated the hypothermic respon
277 s that PAHs are transformed enzymatically to active metabolites that react with DNA to form adducts t
278 lism leads to the generation of biologically active metabolites that regulate cell growth and prolife
279 oA modulating the generation of biologically active metabolites that regulate mitochondrial bioenerge
280 d that vitamin A, retinol, functions through active metabolites: the visual chromophore 11-cis-retina
281 an inactive prodrug; it is converted to its active metabolite through the cytochrome P450 (CYP3A4) p
282 eportedly reduce clopidogrel's metabolism to active metabolite, thus attenuating its inhibition of pl
285 is a novel prodrug formulated to deliver the active metabolite to target cells more efficiently than
286 vir impairs the conversion of 25(OH)D to the active metabolite, utilization of 25(OH)D may have been
287 a 7-fold lower rectal tissue ratio of PrEP's active metabolites vs competing deoxynucleotides compare
289 rther suggest that potentially biochemically active metabolites were more deterministically assembled
290 ationship suggested the presence of a common active metabolite which may preclude this series of comp
291 ch has been focused on the identification of active metabolites, which are crucial for selenium chemo
292 both the parent compound ranolazine and its active metabolites, which have shown potent blocking eff
294 pedunculata studied is a potential source of active metabolites with a positive effect on human healt
296 resuscitation to promote renal excretion of active metabolite, withholding the doses and timely mana
297 ical models by enhancing accumulation of its active metabolite within the tumor microenvironment.
298 their abilities to convert amifostine to its active metabolite WR-1065, amifostine may not only prote
300 WR-2721 is a prodrug and is converted to its active metabolite, WR-1065, by alkaline phosphatases in