ライフサイエンスコーパス: allosteric binding site

1 y, whereas preliminary data had indicated an allosteric binding site.

2 gesting that alcohols interact at a discrete allosteric binding site.

3 780 may cause receptor activation through an allosteric binding site.

4 plex with (S)-fluoxetine (SFX), revealing an allosteric binding site.

5 hich lack a crucial amino acid in the Cmpd-6 allosteric binding site.

6 AMPA-mediated excitotoxicity by targeting an allosteric binding site.

7 iate conformations and identified a putative allosteric binding site.

8 ing SHP099 (2), which binds to a tunnel-like allosteric binding site.

9 mbrane through binding of Ras.GTP in the SOS allosteric binding site.

10 established a Ki value of 4.4 nM at a known allosteric binding site.

11 art because of the hydrophobic nature of the allosteric binding site.

12 interaction and supporting the model of the allosteric binding site.

13 vity with ACh upon interaction with a common allosteric binding site.

14 ituted phenyl rings C that interact with the allosteric binding site.

15 -(phenylethynyl)pyridine] for the antagonist allosteric binding site.

16 while also implicating a possible secondary allosteric-binding site.

17 of HKI by G6P can occur from both active and allosteric binding sites.

18 ogical and structural approaches to identify allosteric binding sites.

19 it remains a challenge to identify suitable allosteric binding sites.

20 d discuss their potential as a new source of allosteric binding sites.

21 ation with X-ray crystallography to identify allosteric binding sites.

22 ally the human M2 and M4 muscarinic receptor allosteric binding sites.

23 ide) as a novel probe of the human M2 and M4 allosteric binding sites.

24 ivating (AMP, ADP) and inhibitory (ATP, ADP) allosteric binding sites.

25 nic receptors occurs through orthosteric and allosteric binding sites.

26 s, the results indicate a possible conserved allosteric binding site across the opioid receptor famil

27 h suggests a general lack of selectivity for allosteric binding sites across aminergic G protein-coup

28 given recent structures that reveal similar allosteric binding sites across receptors.

29 This conformational change reveals an allosteric binding site adjacent to the D2 domain active

30 late PAD4 activity through interactions with allosteric binding sites adjacent to the catalytic pocke

31 residues that interact with IIA(Glc) at the allosteric binding site and 3 residues in the conserved

32 nzyme bound to lysine (2.4 A) identifies the allosteric binding site and clearly shows a conformation

33 tive PRMT3 inhibitor, which occupies a novel allosteric binding site and is noncompetitive with both

34 This site is adjacent to the MgATP allosteric binding site and is only observed in the pres

35 inst GPR61 and structural elucidation of its allosteric binding site and mode of action.

36 uterium exchange analyses, we identified the allosteric binding site and revealed how this compound b

37 , namely the better fit of the ligand to the allosteric binding site and the addition of fluorine ato

38 gand binding simulations to identify cryptic allosteric binding sites and is widely applicable to oth

39 To date, the discovery of allosteric binding sites and lead compounds has been mos

40 We envisioned that MBSs can be regarded as allosteric binding sites and targeted by homobivalent bi

41 oms, simulations can enable the discovery of allosteric binding sites and the determination of the me

42 Thus we identify key elements of allosteric binding sites, and extend drug design possibi

43 it does define the propagation pathways, the allosteric binding sites, and key on-path residues.

44 s the interrogation of protein active sites, allosteric binding sites, and protein-protein interactio

45 activation, discusses the elucidation of the allosteric binding sites, and summarizes the clinical de

46 Allosteric binding sites are topographically distinct fr

47 Allosteric binding sites are topographically distinct fr

48 firmed that this inhibitor occupied the same allosteric binding site as our initial lead compound.

49 T-1284), as a tool for characterizing the M1 allosteric binding site, as well as profiling novel M1 P

50 We identify an allosteric binding site at the interface of the VFT doma

51 nts in transmembrane domains 1 and 2 and the allosteric binding site between transmembrane domains 2

52 th compact and extended conformations in the allosteric binding sites but conserve extended conformat

53 ia X-ray crystallography a nanobody-targeted allosteric binding site by which Nb6 stabilizes a ligand

54 This allosteric binding site can potentially be utilized to g

55 sis of the N terminus, which is regulated by allosteric binding sites, cofactors, membrane localizati

56 to alanine decreased affinity of NMS for the allosteric binding site confirming results of molecular

57 We have tested the hypothesis that distinct allosteric binding sites control GluR6 receptors via a c

58 a previously identified UDP-glucuronic acid allosteric binding site decreased the binding affinity o

59 We propose that this allosteric binding site defines a pocket that is differe

60 Allosteric binding sites, elsewhere on the receptors, ar

61 These results suggest that an allosteric binding site exists on the HIV-1 PR and that

62 g and site-directed mutagenesis suggested an allosteric binding site for 5-BDBD located between two s

63 We describe a completely novel allosteric binding site for class B receptors, providing

64 We show here that PPM1H also contains an allosteric binding site for its nonphosphorylated reacti

65 role of beta(2)AR extracellular region as an allosteric binding site for larger drugs such as salmete

66 ains and show that the DH-PH unit blocks the allosteric binding site for Ras and suppresses the activ

67 egulatory domain (Delta1-147), suggesting an allosteric binding site for recifin A on the regulatory

68 n-sensitive rod rhodopsins have at least one allosteric binding site for retinoid, but beta-ionone bi

69 s in C-C chemokine receptor 5 (CCR5) near an allosteric binding site for the drug maraviroc.

70 r sAC because they bind to the sAC-specific, allosteric binding site for the physiological activator

71 ed in several CNS disorders and possesses an allosteric binding site for which ligands modulating the

72 (GLIC), are receptors that contain multiple allosteric binding sites for a variety of therapeutics,

73 valuated rheostat positions located near the allosteric binding sites for inhibitor alanine (Ala) and

74 C80 binds to an allosteric binding site formed by a network of nine resi

75 The existence of such an allosteric binding site had been predicted by biochemica

76 interacting with both the orthosteric and an allosteric binding site has gained importance to achieve

77 Because allosteric binding sites have been found on many other G

78 d the identification of both orthosteric and allosteric binding sites have provided further guidance

79 orescent ligands targeting the intracellular allosteric binding site (IABS) of CXC chemokine receptor

80 rate that E. coli RNA polymerase contains an allosteric binding site in addition to the catalytic sit

81 ng of the ion channel and represents a novel allosteric binding site in Cys-loop receptors.

82 Together, these data unveil an allosteric binding site in the extracellular ligand-bind

83 The allosteric binding site in the proteases was probed usin

84 activated by ACh when PAMs were bound to the allosteric binding site in the transmembrane domain.

85 expands our understanding of the topology of allosteric binding sites in AChBP and, by extrapolation,

86 t interact with both the orthosteric and the allosteric binding sites in order to deepen the inhibiti

87 tructural biology have identified additional allosteric binding sites in other parts of these recepto

88 resents a structural framework for different allosteric binding sites in the alpha7 nAChR and paves t

89 5 inhibitors were used to translate the CCR5 allosteric binding site into a general pharmacophore, wh

90 Understanding of interactions of NMS at the allosteric binding site is essential for correct analysi

91 th both the orthosteric binding site and the allosteric binding site located between the second and t

92 nt-based screening approach, we uncovered an allosteric binding site located near the beta8-beta9 loo

93 trapeptide (OC252-324) further defines a new allosteric binding site located near the center of fruct

94 i.e., noncompetitive binding sites, negative allosteric binding sites) located on nAChRs.

95 Impaired interaction with the allosteric binding site manifests as low-affinity bindin

96 , reciprocal linkage of functionally opposed allosteric binding sites must have developed independent

97 ate (HPP) tautomerase activity of MIF and an allosteric binding site of AV411 and AV1013 is detected

98 The allosteric binding site of dyclonine can serve as a temp

99 The allosteric binding site of NMS overlaps with the binding

100 inhibitors can be created by exploiting the allosteric binding site of PRMT3.

101 reflects the electrostatic properties in the allosteric binding site of the LDH enzymes.

102 as PET tracers for the in vivo imaging of an allosteric binding site of the M4 receptor.

103 PET) radiotracers for in vivo imaging of the allosteric binding site of the metabotropic glutamate (m

104 with important residues in the catalytic and allosteric binding sites of bacterial PFK and that are c

105 Here we show that the allosteric binding sites of the enzyme are plastic and c

106 inding affinities of Pi to the catalytic and allosteric binding sites of the enzymes modeled in proto

107 at the interface between the orthosteric and allosteric binding sites of the receptor.

108 These data suggest that a specific allosteric binding site on b5, which includes residues E

109 Second, removal of Mg(2+) from an allosteric binding site on SecA does not perturb the end

110 These findings identify a allosteric binding site on the beta(2)AR, whose activati

111 esign and synthesis of ligands targeting the allosteric binding site on the CB(1) cannabinoid recepto

112 ology modeling of the proposed lipid-exposed allosteric binding site on the cytosolic side, we functi

113 ine can bind solely with low affinity to the allosteric binding site on the extracellular domain of N

114 We report the discovery of a novel allosteric binding site on the nuclear receptor RORgamma

115 en identified, it has been proposed to be an allosteric binding site on the PDE-IV enzyme.

116 served results, which includes an additional allosteric binding site on the viral NTPases/helicases t

117 Since the discovery of allosteric binding sites on G protein-coupled receptors,

118 Allosteric binding sites on the adenosine receptor famil

119 when inhibitors are bound at three different allosteric binding sites on the enzyme.

120 These include the presence of allosteric binding sites on the receptor that can be exp

121 of chronic pain and bind to a high-affinity allosteric-binding site on the human glycine transporter

122 ted details on the existence of lipid-facing allosteric binding sites outside the transmembrane helic

123 The putative allosteric binding site partially overlaps the dimerizat

124 , together with predictions of substrate and allosteric binding sites, protein-ligand docking, SARS-C

125 -1 FL CA and characterization of a potential allosteric binding site provides three-dimensional views

126 , Fe2+, Co2+, Ni2+, Zn2+ and Cd2+, but their allosteric binding sites reject other divalent metals su

127 ural understanding of the M(5) mAChR and its allosteric binding sites remains limited.

128 We identified two allosteric binding sites representing attractive targets

129 ly interact with both the orthosteric and an allosteric binding site represents a novel approach in m

130 ess route of bicarbonate ion to and from the allosteric binding site, respectively.

131 -loop, and anion-binding exosite 1, the main allosteric binding site, retain mus-ms motions.

132 s of the positive allosteric modulators, the allosteric binding site(s) and structure-activity relati

133 g will be useful for the characterization of allosteric binding site(s) on CB(2)Rs which will be esse

134 and the inhibitors were found to bind in an allosteric binding site separate from the active site.

135 ations and molecular modelling identified an allosteric binding site that forms at the subunit interf

136 ochemical assays indicated a noncompetitive, allosteric binding site that is distinct from that of kn

137 , reveals differences in the orthosteric and allosteric binding sites that contribute to a role in dr

138 le binding sites may provide a new source of allosteric binding sites that could be exploited in the

139 The first structure of a SULT allosteric-binding site (that of SULT1A1) has recently c

140 When the ATP molecules occupy the allosteric binding sites, the allosteric trigger from AT

141 es have surprisingly uncovered two potential allosteric binding sites, the most characterized of whic

142 Here, we present the structure of an SULT allosteric binding site-the catechin-binding site of SUL

143 ted by application to 22 proteins with known allosteric binding sites; the orthosteric and allosteric

144 e such protease, gamma secretase, through an allosteric binding site to preferentially increase the c

145 ntify key communication pathways linking the allosteric binding site to the active site of the enzyme

146 o bind to the previously identified ;common' allosteric binding site, Trankle et al. provide evidence

147 ic mechanism, we identified several possible allosteric binding sites using computational searches.

148 llosteric binding sites; the orthosteric and allosteric binding sites were identified in all but one

149 nsistent with the structural evidence for an allosteric binding site which is present in the glucose-

150 RORyt features an allosteric binding site within its ligand-binding domain

151 eptors including the precise location of the allosteric binding site within the transmembrane domain