ライフサイエンスコーパス: allosteric inhibition

1 ng the Kd for [(3)H]BTXB binding, indicating allosteric inhibition.

2 hether an ABL fusion protein is sensitive to allosteric inhibition.

3 ight into the pharmacophore requirements for allosteric inhibition.

4 mpervious to glucuronidation and demonstrate allosteric inhibition.

5 mall molecule probes that induce sub-maximal allosteric inhibition.

6 the modulatory binding site that mediate the allosteric inhibition.

7 e active site, defining a novel mechanism of allosteric inhibition.

8 equirement for an intact PH-KD interface for allosteric inhibition.

9 exible loop mediating the slow-onset step of allosteric inhibition.

10 ithin the L5 pocket is sufficient to restore allosteric inhibition.

11 t these motions are not sufficient to elicit allosteric inhibition.

12 e two compounds were not equivalent in their allosteric inhibition.

13 ions, a salient molecular mechanism enabling allosteric inhibition.

14 determinant of the magnitude of the observed allosteric inhibition.

15 the hetero-domain interaction underpins the allosteric inhibition.

16 ain-1 and calpain-2 make them susceptible to allosteric inhibition aimed at interfering with heterodi

17 ences to the DegS-PDZ domain, which relieves allosteric inhibition and activates proteolysis.

18 ructure-switching biosensors to enable their allosteric inhibition and activation.

19 e delicate structural discrimination between allosteric inhibition and potentiation of Cys-loop recep

20 We then elucidate mechanisms of allosteric inhibition and stimulation of MATs, which can

21 ification, subcellular compartmentalization, allosteric inhibition, and feedback regulation.

22 steresis in the reaction time course, to ATP allosteric inhibition, and to F6P homotropic cooperativi

23 Cleavage of ATP-bound Pak2 relaxes the allosteric inhibition, as shown by increased solvent acc

24 d 7 (PG14N, PG17N) show potent and selective allosteric inhibition at hMC5R with IC 50 values of 38 +

25 s, with mutual, weak negative cooperativity (allosteric inhibition) between their binding.

26 is a homohexameric enzyme that is subject to allosteric inhibition by 3'-phosphoadenosine 5'-phosphos

27 e efficacy and exhibits a complex pattern of allosteric inhibition by a wide variety of small molecul

28 They support the suggestion that allosteric inhibition by adenine nucleotides is a genera

29 des a PRPP synthetase that is insensitive to allosteric inhibition by adenylate nucleotides.

30 individual point mutations that: 1) mimicked allosteric inhibition by alanine, 2) mimicked inhibition

31 ntral role in the mechanism of catalysis and allosteric inhibition by AMP.

32 ial and eukaryotic enzyme, the mechanisms of allosteric inhibition by ATP binding at multiple sites,

33 ft in the matrix domain of Cox5A-involved in allosteric inhibition by ATP-may arise from its associat

34 compounds targeting mIDH demonstrated common allosteric inhibition by distinct chemotypes.

35 es that confer proton-sensitivity and enable allosteric inhibition by extracellular sodium ions.

36 teman domain that desensitizes the enzyme to allosteric inhibition by GDP/GTP.

37 he catalytic protein HisG(S) while mediating allosteric inhibition by histidine.

38 erculosis (MtIPMS) is subject to slow-onset, allosteric inhibition by l-leucine.

39 s not play the central role in producing the allosteric inhibition by PEP as originally envisioned in

40 R72E, T125A, and R171E maintained allosteric inhibition by PEP.

41 ncluded in changes previously identified for allosteric inhibition by Phe.

42 rmophilus have led to a structural model for allosteric inhibition by phosphoenolpyruvate (PEP) where

43 horylated form of MTHFR is more sensitive to allosteric inhibition by SAM.

44 We find that protons exert allosteric inhibition by suppressing the glutamate-drive

45 ariant makes the variant more susceptible to allosteric inhibition, compared to the tighter binding o

46 The allosteric inhibition exhibited by the unmodified sites

47 ism for inhibition by G418 and suggests that allosteric inhibition from this site is feasible.

48 A model for the mechanism of allosteric inhibition has been derived from conformation

49 A model for the mechanism of allosteric inhibition has been derived from conformation

50 ellular conformational switch which relieves allosteric inhibition imposed on the intracellular domai

51 that this structural transition explains the allosteric inhibition in BsPFK, and this explanation has

52 by phosphorylation in En. casseliflavus and allosteric inhibition in E. coli.

53 ue of Neuron explore the structural basis of allosteric inhibition in ionotropic glutamate receptors,

54 ccessful pharmacological validation of MALT1 allosteric inhibition in preclinical models of humoral i

55 resence of K(+) (but not Na(+)) enhances the allosteric inhibition induced by MgATP.

56 This allosteric inhibition is mediated by direct interaction

57 Notably, this relief from allosteric inhibition is not caused by self-activation t

58 mplification of the complement response, its allosteric inhibition likely represents a fundamental co

59 sis with heat-induced potentiation, and that allosteric inhibition may contribute, in part, to the co

60 The allosteric inhibition mechanism is further elucidated by

61 s eIF4E structure and reveals elements of an allosteric inhibition mechanism leading to the dislocati

62 Here, we describe the allosteric inhibition mechanism of HTRA1 by a clinical F

63 An allosteric inhibition mechanism of StaDDl by this compou

64 c site of one monomer and sheds light on the allosteric inhibition mechanism that makes the enzyme-su

65 Here, we identified a novel binding site and allosteric inhibition mechanism, disrupting the recently

66 Although the structure is indicative of an allosteric inhibition mechanism, mutational studies and

67 ive site and uses a relatively unappreciated allosteric inhibition mechanism.

68 epitope onto HTRA2 and HTRA3 transferred the allosteric inhibition mechanism.

69 sis revealed a dual active site-directed and allosteric inhibition mode of this compound class.

70 ture of the PRMT3-SGC707 complex confirm the allosteric inhibition mode.

71 ant for the utilization of amino sugars, and allosteric inhibition of Adk activity by HPr-P, but not

72 Allosteric inhibition of AhR was previously thought to b

73 ce as a pharmacologically tractable site for allosteric inhibition of Bcr-Abl.

74 rate constants for processes which alter the allosteric inhibition of beta-oxidation by acetyl-CoA.

75 , proline-based compound class that displays allosteric inhibition of both proteases.

76 an important signaling function through its allosteric inhibition of carnitine palmitoyltransferase

77 entical subunits, which exhibits cooperative allosteric inhibition of catalysis by AMP.

78 several hot spots for either orthosteric or allosteric inhibition of catalytic activity, consistent

79 obe dimer interface leads to an irreversible allosteric inhibition of channel activity upon UV illumi

80 the first time the structural mechanism for allosteric inhibition of DHDPS from the common grapevine

81 -nanosecond motions impact zinc (Zn)-induced allosteric inhibition of DNA binding by the Zn efflux re

82 of the thiophene inhibitors, consistent with allosteric inhibition of DNA gyrase.

83 Demonstrated here is the allosteric inhibition of E. coli FBPase by glucose 6-pho

84 collapse of the mitotic spindle through the allosteric inhibition of Eg5.

85 se Cys residues in Na(+) self-inhibition, an allosteric inhibition of ENaC activity by extracellular

86 for catalytic activity and the mechanism of allosteric inhibition of FBPase by AMP.

87 Both the allosteric inhibition of fibrinogen turnover caused by G

88 Evidently, two pathways of allosteric inhibition of fructose-1,6-bisphosphatase are

89 an colon carcinoma cells, demonstrating that allosteric inhibition of GCC by adenine nucleotides is m

90 We present a model for the allosteric inhibition of GCGR by a monoclonal antibody t

91 erammonemia disorder showed that the loss of allosteric inhibition of GDH by GTP causes excessive sec

92 hate pathway as a glycolytic shunt, reducing allosteric inhibition of glycolysis and supporting bioma

93 Additionally, we observed allosteric inhibition of glycosylase activity in the dim

94 discovery efforts have focused primarily on allosteric inhibition of hFPPS and the discovery of non-

95 Our data strengthen the case for allosteric inhibition of HIV RNase H activity, providing

96 in guard cell CO(2) signaling that relies on allosteric inhibition of HT1.

97 zation to a tetramer, thereby explaining the allosteric inhibition of htt(ex1) fibril formation by Fy

98 ed channel state, allowing for the selective allosteric inhibition of I(NaL) without the physical blo

99 te, and aconitate, which was consistent with allosteric inhibition of isocitrate dehydrogenase by P-e

100 se studies therefore offer insights into (i) allosteric inhibition of KGA by BPTES, revealing the dyn

101 With several marketed drugs, allosteric inhibition of kinases has translated to pharm

102 Asymmetry results in allosteric inhibition of L-protein engagement and ET in

103 sly block two steps in this pathway, through allosteric inhibition of mevalonate kinase (MK) and, for

104 Thus, allosteric inhibition of MKP5 represents a therapeutic s

105 ion of the ADMIDAS residues also reduced the allosteric inhibition of Mn2+-supported ligand binding b

106 to the genesis of monopolar spindles during allosteric inhibition of motility, but instead reveals a

107 combined into a model that accounts for the allosteric inhibition of MtATP-phosphoribosyltransferase

108 the profile of AAS modulation and that this allosteric inhibition of native GnRH neurons should be c

109 This conformational change induces allosteric inhibition of NF-kappaB DNA binding.

110 N2B ATD is essential for ifenprodil-mediated allosteric inhibition of NMDA receptors.

111 Our results suggest that the allosteric inhibition of NmeIPMS is achieved by restrict

112 lypeptides can bind to this exosite to cause allosteric inhibition of OGT through steric occlusion of

113 not only for successful efflux but also for allosteric inhibition of Pdr5 ATPase activity.

114 We show that direct allosteric inhibition of plasmin could led to new antifi

115 therefore creates the geometry that permits allosteric inhibition of PRC2 by methylated H3K36 in tra

116 cleotide pool, which results in the enhanced allosteric inhibition of PRPP synthetase and consequentl

117 phosphoenolpyruvate (PEP) contribute to the allosteric inhibition of rabbit muscle pyruvate kinase b

118 ing with TSC-Rheb complex, arginine relieves allosteric inhibition of Rheb by TSC.

119 Allosteric inhibition of RORgammat is conceptually new,

120 Here we show that allosteric inhibition of RXR results from a rotation of

121 interact with ALX/FPR2 receptors and lead to allosteric inhibition of SAA-initiated epithelial respon

122 s a ligandable Cys that can be exploited for allosteric inhibition of SHP1, which has been refractory

123 in the inv(16)/KitD816Y AML mouse model, but allosteric inhibition of Shp2 did not impair the clonoge

124 To broaden our approach to allosteric inhibition of SHP2, we conducted additional h

125 ly activated by RAR ligands only, because of allosteric inhibition of the binding of ligands to RXR b

126 gulation of the trypsin-like (T-L) site, (3) allosteric inhibition of the chymotrypsin-like (CT-L) an

127 l dynamic effects of nucleotide turnover and allosteric inhibition of the kinesin-5 motor.

128 e properties of compounds that would prevent allosteric inhibition of the receptor and how to test fo

129 in a manner consistent with noncompetitive, allosteric inhibition of the receptor-channel complex.

130 odel wherein CK2 phosphorylation triggers an allosteric inhibition of the SNAP190 Myb DNA binding dom

131 e-stimulated insulin secretion that includes allosteric inhibition of tricarboxylic acid cycle enzyme

132 ng dynamic transition metal signaling pools, allosteric inhibition or activation of protein targets b

133 ffect at RG is consistent with either strong allosteric inhibition or competitive inhibition at one o

134 nd binding and not to cause the heterotropic allosteric inhibition per se.

135 de of the protein binding site indicate that allosteric inhibition, rather than direct steric competi

136 tion of phenylethanolamines and ATD-mediated allosteric inhibition remain limited owing to a lack of

137 at an RXXD motif that normally serves as an allosteric inhibition site for active diguanylate cyclas

138 ition against calpain-2 was observed, and an allosteric inhibition site on the enzyme was identified

139 of the indirect activation, we narrowed down allosteric inhibition sites of negative allosteric modul

140 for the distant coupling locus to transplant allosteric inhibition suggest that the coupling locus mo

141 cepsilonRI and CD23 is blocked by reciprocal allosteric inhibition, suggesting that the 2 receptors e

142 Here we review the principles of allosteric inhibition, summarize the discovery of allost

143 l signaling, wherein ATP is the transmitter, allosteric inhibition the coupling mechanism, and regula

144 In the presence of folate binding and allosteric inhibition, the velocities show a remarkable

145 By illuminating the molecular mechanisms of allosteric inhibition, these studies delineate the intri

146 teric couple mutants still allow binding and allosteric inhibition, they partially relieve the mutual

147 gest the enzyme undergoes a slow relief from allosteric inhibition upon initiation of catalysis on un

148 sis for its regulation, we characterized the allosteric inhibition using gel filtration, steady-state

149 S-CoV-2 PLpro that may function as sites for allosteric inhibition were computationally identified.

150 that AcrIC8 inhibits PAM recognition through allosteric inhibition, whereas AcrIC9 achieves so throug

151 shows a kinetic lag in product formation and allosteric inhibition with unmethylated DNA that is not