Weaver Lab Publications
2018
Abney
KK ,
Ramos-Hunter
SJ ,
Romaine
IM ,
Goodwin
JS ,
Sulikowski
GA ,
Weaver
CD ,
Selective Activation of N,N’-Diacyl Rhodamine Pro-fluorophores Paired with Releasing Enzyme, Porcine Liver Esterase (PLE)
Chemistry (Weinheim an der Bergstrasse, Germany).
2018 May
25;
24
(36).
8985-8988
- PMID: 29679472 [PubMed].
- PMCID: PMC6035858.
Kharade
SV ,
Kurata
H ,
Bender
AM ,
Blobaum
AL ,
Figueroa
EE ,
Duran
A ,
Kramer
M ,
Days
E ,
Vinson
P ,
Flores
D ,
Satlin
LM ,
Meiler
J ,
Weaver
CD ,
Lindsley
CW ,
Hopkins
CR ,
Denton
JS ,
Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992
Molecular pharmacology.
2018 Jun
12;
94
(2).
926-937
- PMID: 29895592 [PubMed].
Dutter
BF ,
Ender
A ,
Sulikowski
GA ,
Weaver
CD ,
Rhodol-based thallium sensors for cellular imaging of potassium channel activity
Organic & biomolecular chemistry.
2018 Jul
27;
- PMID: 30051127 [PubMed].
2017
Nance
KD ,
Days
EL ,
Weaver
CD ,
Coldren
A ,
Farmer
TD ,
Cho
HP ,
Niswender
CM ,
Blobaum
AL ,
Niswender
KD ,
Lindsley
CW ,
Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core
Journal of medicinal chemistry.
2017 Feb
03;
60
(4).
1611-1616
- PMID: 28103022 [PubMed].
Azumaya
CM ,
Days
EL ,
Vinson
PN ,
Stauffer
S ,
Sulikowski
G ,
Weaver
CD ,
Nakagawa
T ,
Screening for AMPA receptor auxiliary subunit specific modulators
PloS one.
2017 Mar
30;
12
(3).
e0174742
- PMID: 28358902 [PubMed].
- PMCID: PMC5373622.
Marron Fernandez de Velasco
E ,
Zhang
L ,
N Vo
B ,
Tipps
M ,
Farris
S ,
Xia
Z ,
Anderson
A ,
Carlblom
N ,
Weaver
CD ,
Dudek
SM ,
Wickman
K ,
GIRK2 splice variants and neuronal G protein-gated K channels: implications for channel function and behavior
Scientific reports.
2017 May
09;
7
(1).
1639
- PMID: 28487514 [PubMed].
- PMCID: PMC5431628.
Wieting
JM ,
Vadukoot
AK ,
Sharma
S ,
Abney
KK ,
Bridges
TM ,
Daniels
JS ,
Morrison
RD ,
Wickman
K ,
Weaver
CD ,
Hopkins
CR ,
Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators
ACS chemical neuroscience.
2017 Jul
19;
8
(9).
1873-1879
- PMID: 28697302 [PubMed].
Schubert
M ,
Stichel
J ,
Du
Y ,
Tough
IR ,
Sliwoski
G ,
Meiler
J ,
Cox
HM ,
Weaver
CD ,
Beck-Sickinger
AG ,
Identification and Characterization of the First Selective Y Receptor Positive Allosteric Modulator
Journal of medicinal chemistry.
2017 Aug
28;
60
(17).
7605-7612
- PMID: 28795803 [PubMed].
2016
Dadi
PK ,
Vierra
NC ,
Days
E ,
Dickerson
MT ,
Vinson
PN ,
Weaver
CD ,
Jacobson
DA ,
Selective Small Molecule Activators of TREK-2 Channels Stimulate Dorsal Root Ganglion c-Fiber Nociceptor Two-Pore-Domain Potassium Channel Currents and Limit Calcium Influx
ACS chemical neuroscience.
2016 Nov
23;
8
(3).
558-568
- PMID: 27805811 [PubMed].
- PMCID: PMC5901755.
Delpire
E ,
Weaver
CD ,
Challenges of Finding Novel Drugs Targeting the K-Cl Cotransporter
ACS chemical neuroscience.
2016 Nov
08;
7
(12).
1624-1627
- PMID: 27998063 [PubMed].
- PMCID: PMC5473358.
Kim
HY ,
Korade
Z ,
Tallman
KA ,
Liu
W ,
Weaver
CD ,
Mirnics
K ,
Porter
NA ,
Inhibitors of 7-Dehydrocholesterol Reductase: Screening of a Collection of Pharmacologically Active …
Chemical research in toxicology.
2016 May
16;
29
(5).
892-900
- PMID: 27097157 [PubMed].
- PMCID: PMC4868769.
- NIHMSID: NIHMS782657
Sliwoski
G ,
Schubert
M ,
Stichel
J ,
Weaver
D ,
Beck-Sickinger
AG ,
Meiler
J ,
Discovery of Small-Molecule Modulators of the Human Y4 Receptor.
PloS one.
2016
;
11
(6).
e0157146
- PMID: 27294784 [PubMed].
- PMCID: PMC4905667.
Barber
M. ,
Schönberger
,
Burgstaller
,
Levitz
,
Weaver
,
Isacoff
Y. ,
Baier
,
Trauner
Dirk ,
Optical control of neuronal activity using a light-operated GIRK channel opener (LOGO)
Chemical Science.
2016
;
(7).
2347-2352
2015
Barber
DM ,
Schönberger
M ,
Burgstaller
J ,
Levitz
J ,
Weaver
CD ,
Isacoff
EY ,
Baier
H ,
Trauner
D ,
Optical control of neuronal activity using a light-operated GIRK channel opener (LOGO)
Chemical science.
2015 Nov
23;
7
(3).
2347-2352
- PMID: 28090283 [PubMed].
- PMCID: PMC5234268.
Kotecki
L ,
Hearing
M ,
McCall
NM ,
Marron Fernandez de Velasco
E ,
Pravetoni
M ,
Arora
D ,
Victoria
NC ,
Munoz
MB ,
Xia
Z ,
Slesinger
PA ,
Weaver
CD ,
Wickman
K ,
GIRK Channels Modulate Opioid-Induced Motor Activity in a Cell Type- and Subunit-Dependent Manner.
The Journal of neuroscience : the official journal of the Society for Neuroscience.
2015 May
6;
35
(18).
7131-42
- PMID: 25948263 [PubMed].
- PMCID: PMC4420781.
Du
Y ,
Days
E ,
Romaine
I ,
Abney
KK ,
Kaufmann
K ,
Sulikowski
G ,
Stauffer
S ,
Lindsley
CW ,
Weaver
CD ,
Development and Validation of a Thallium Flux-Based Functional Assay for the Sodium Channel NaV1.7 a…
ACS chemical neuroscience.
2015 Jun
17;
6
(6).
871-8
- PMID: 25879403 [PubMed].
2014
Morris
LC ,
Nance
KD ,
Gentry
PR ,
Days
EL ,
Weaver
CD ,
Niswender
CM ,
Thompson
AD ,
Jones
CK ,
Locuson
CW ,
Morrison
RD ,
Daniels
JS ,
Niswender
KD ,
Lindsley
CW ,
Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[…
Journal of medicinal chemistry.
2014 Dec
11;
57
(23).
10192-7
- PMID: 25423411 [PubMed].
- PMCID: PMC4266362.
Glickman
JF ,
Lundbäck
T ,
Napper
AD ,
Niles
WD ,
Simeonov
A ,
Weaver
CD ,
Yin
HH ,
Zaman
GJ ,
Osada
H ,
Controversies in ASSAY and drug development technologies: a focus on assessing irreproducibility.
Assay and drug development technologies.
2014 Oct
;
12
(8).
443-51
- PMID: 25383720 [PubMed].
Raphemot
R ,
Rouhier
MF ,
Swale
DR ,
Days
E ,
Weaver
CD ,
Lovell
KM ,
Konkel
LC ,
Engers
DW ,
Bollinger
SF ,
Hopkins
C ,
Piermarini
PM ,
Denton
JS ,
Discovery and characterization of a potent and selective inhibitor of Aedes aegypti inward rectifier…
PloS one.
2014
;
9
(11).
e110772
- PMID: 25375326 [PubMed].
- PMCID: PMC4222822.
Kumar
KK ,
Lowe
EW ,
Aboud
AA ,
Neely
MD ,
Redha
R ,
Bauer
JA ,
Odak
M ,
Weaver
CD ,
Meiler
J ,
Aschner
M ,
Bowman
AB ,
Cellular manganese content is developmentally regulated in human dopaminergic neurons.
Scientific reports.
2014
;
4
6801
- PMID: 25348053 [PubMed].
- PMCID: PMC4210885.
Wen
W ,
Wu
W ,
Weaver
CD ,
Lindsley
CW ,
Discovery of potent and selective GIRK1/2 modulators via ‘molecular switches’ within a series of 1-(…
Bioorganic & medicinal chemistry letters.
2014 Nov
1;
24
(21).
5102-6
- PMID: 25264075 [PubMed].
Jalan-Sakrikar
N ,
Field
JR ,
Klar
R ,
Mattmann
ME ,
Gregory
KJ ,
Zamorano
R ,
Engers
DW ,
Bollinger
SR ,
Weaver
CD ,
Days
EL ,
Lewis
LM ,
Utley
TJ ,
Hurtado
M ,
Rigault
D ,
Acher
F ,
Walker
AG ,
Melancon
BJ ,
Wood
MR ,
Lindsley
CW ,
Conn
PJ ,
Xiang
Z ,
Hopkins
CR ,
Niswender
CM ,
Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new…
ACS chemical neuroscience.
2014 Dec
17;
5
(12).
1221-37
- PMID: 25225882 [PubMed].
- PMCID: PMC4306484.
Wydeven
N ,
Marron Fernandez de Velasco
E ,
Du
Y ,
Benneyworth
MA ,
Hearing
MC ,
Fischer
RA ,
Thomas
MJ ,
Weaver
CD ,
Wickman
K ,
Mechanisms underlying the activation of G-protein-gated inwardly rectifying K+ (GIRK) channels by th…
Proceedings of the National Academy of Sciences of the United States of America.
2014 Jul
22;
111
(29).
10755-60
- PMID: 25002517 [PubMed].
- PMCID: PMC4115558.
Turlington
M ,
Malosh
C ,
Jacobs
J ,
Manka
JT ,
Noetzel
MJ ,
Vinson
PN ,
Jadhav
S ,
Herman
EJ ,
Lavreysen
H ,
Mackie
C ,
Bartolomé-Nebreda
JM ,
Conde-Ceide
S ,
Martín-Martín
ML ,
Tong
HM ,
López
S ,
MacDonald
GJ ,
Steckler
T ,
Daniels
JS ,
Weaver
CD ,
Niswender
CM ,
Jones
CK ,
Conn
PJ ,
Lindsley
CW ,
Stauffer
SR ,
Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the m…
Journal of medicinal chemistry.
2014 Jul
10;
57
(13).
5620-37
- PMID: 24914612 [PubMed].
- PMCID: PMC4096224.
Morris
LC ,
Days
EL ,
Turney
M ,
Mi
D ,
Lindsley
CW ,
Weaver
CD ,
Niswender
KD ,
A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 a…
Journal of biomolecular screening.
2014 Feb
13;
19
(6).
847-858
- PMID: 24525870 [PubMed].
- PMCID: PMC4306651.
- NIHMSID: NIHMS580600
2013
Wu
YJ ,
Conway
CM ,
Sun
LQ ,
Machet
F ,
Chen
J ,
Chen
P ,
He
H ,
Bourin
C ,
Calandra
V ,
Polino
JL ,
Davis
CD ,
Heman
K ,
Gribkoff
VK ,
Boissard
CG ,
Knox
RJ ,
Thompson
MW ,
Fitzpatrick
W ,
Weaver
D ,
Harden
DG ,
Natale
J ,
Dworetzky
SI ,
Starrett
JE ,
Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent …
Bioorganic & medicinal chemistry letters.
2013 Nov
15;
23
(22).
6188-91
- PMID: 24070783 [PubMed].
Raphemot
R ,
Kadakia
RJ ,
Olsen
ML ,
Banerjee
S ,
Days
E ,
Smith
SS ,
Weaver
CD ,
Denton
JS ,
Development and validation of fluorescence-based and automated patch clamp-based functional assays f…
Assay and drug development technologies.
2013 Nov
;
11
(9-10).
532-43
- PMID: 24266659 [PubMed].
- PMCID: PMC3870600.
Gregory
KJ ,
Herman
EJ ,
Ramsey
AJ ,
Hammond
AS ,
Byun
NE ,
Stauffer
SR ,
Manka
JT ,
Jadhav
S ,
Bridges
TM ,
Weaver
CD ,
Niswender
CM ,
Steckler
T ,
Drinkenburg
WH ,
Ahnaou
A ,
Lavreysen
H ,
Macdonald
GJ ,
Bartolomé
JM ,
Mackie
C ,
Hrupka
BJ ,
Caron
MG ,
Daigle
TL ,
Lindsley
CW ,
Conn
PJ ,
Jones
CK ,
N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy …
The Journal of pharmacology and experimental therapeutics.
2013 Nov
;
347
(2).
438-57
- PMID: 23965381 [PubMed].
- PMCID: PMC3807069.
Bartolomé-Nebreda
JM ,
Conde-Ceide
S ,
Delgado
F ,
Iturrino
L ,
Pastor
J ,
Pena
MÁ ,
Trabanco
AA ,
Tresadern
G ,
Wassvik
CM ,
Stauffer
SR ,
Jadhav
S ,
Gogi
K ,
Vinson
PN ,
Noetzel
MJ ,
Days
E ,
Weaver
CD ,
Lindsley
CW ,
Niswender
CM ,
Jones
CK ,
Conn
PJ ,
Rombouts
F ,
Lavreysen
H ,
Macdonald
GJ ,
Mackie
C ,
Steckler
T ,
Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metab…
Journal of medicinal chemistry.
2013 Sep
26;
56
(18).
7243-59
- PMID: 23947773 [PubMed].
- PMCID: PMC3924858.
- NIHMSID: NIHMS547633
Ramos-Hunter
SJ ,
Engers
DW ,
Kaufmann
K ,
Du
Y ,
Lindsley
CW ,
Weaver
CD ,
Sulikowski
GA ,
Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators.
Bioorganic & medicinal chemistry letters.
2013 Sep
15;
23
(18).
5195-8
- PMID: 23916258 [PubMed].
- PMCID: PMC4066871.
- NIHMSID: NIHMS589020
Wen
W ,
Wu
W ,
Romaine
IM ,
Kaufmann
K ,
Du
Y ,
Sulikowski
GA ,
Weaver
CD ,
Lindsley
CW ,
Discovery of ‘molecular switches’ within a GIRK activator scaffold that afford selective GIRK inhibi…
Bioorganic & medicinal chemistry letters.
2013 Aug
15;
23
(16).
4562-6
- PMID: 23838260 [PubMed].
- PMCID: PMC3816575.
- NIHMSID: NIHMS497033
Kaufmann
K ,
Romaine
I ,
Days
E ,
Pascual
C ,
Malik
A ,
Yang
L ,
Zou
B ,
Du
Y ,
Sliwoski
G ,
Morrison
RD ,
Denton
J ,
Niswender
CM ,
Daniels
JS ,
Sulikowski
GA ,
Xie
XS ,
Lindsley
CW ,
Weaver
CD ,
ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays …
ACS chemical neuroscience.
2013 Sep
18;
4
(9).
1278-86
- PMID: 23730969 [PubMed].
- PMCID: PMC3778424.
Raphemot
R ,
Weaver
CD ,
Denton
JS ,
High-throughput screening for small-molecule modulators of inward rectifier potassium channels.
Journal of visualized experiments : JoVE.
2013
;
(71).
- PMID: 23381507 [PubMed].
- PMCID: PMC3582647.
- NIHMSID: NIHMS505282
Butkiewicz
M ,
Lowe
EW ,
Mueller
R ,
Mendenhall
JL ,
Teixeira
PL ,
Weaver
CD ,
Meiler
J ,
Benchmarking ligand-based virtual High-Throughput Screening with the PubChem database.
Molecules (Basel, Switzerland).
2013
;
18
(1).
735-56
- PMID: 23299552 [PubMed].
- PMCID: PMC3759399.
- NIHMSID: NIHMS499237
2012
Rinker
C. ,
Jones
L. ,
Pitts
,
Rutzler
,
Camp
,
Sun
,
Xu
,
Dorset
C. ,
Weaver
,
Zwiebel
J. ,
Novel high-throughput screens of Anopheles gambiae odorant receptors reveal candidate behaviour-modi…
Physiological Entomology.
2012 Mar
;
37
(1).
33-41
Ruggiero
AM ,
Wright
J ,
Ferguson
SM ,
Lewis
M ,
Emerson
KS ,
Iwamoto
H ,
Ivy
MT ,
Holmstrand
EC ,
Ennis
EA ,
Weaver
CD ,
Blakely
RD ,
Nonoisotopic assay for the presynaptic choline transporter reveals capacity for allosteric modulatio…
ACS chemical neuroscience.
2012 Oct
17;
3
(10).
767-81
- PMID: 23077721 [PubMed].
- PMCID: PMC3474274.
Potet
F ,
Lorinc
AN ,
Chaigne
S ,
Hopkins
CR ,
Venkataraman
R ,
Stepanovic
SZ ,
Lewis
LM ,
Days
E ,
Sidorov
VY ,
Engers
DW ,
Zou
B ,
Afshartous
D ,
George
AL ,
Campbell
CM ,
Balser
JR ,
Li
M ,
Baudenbacher
FJ ,
Lindsley
CW ,
Weaver
CD ,
Kupershmidt
S ,
Identification and characterization of a compound that protects cardiac tissue from human Ether-à-g…
The Journal of biological chemistry.
2012 Nov
16;
287
(47).
39613-25
- PMID: 23033485 [PubMed].
- PMCID: PMC3501040.
Manka
JT ,
Vinson
PN ,
Gregory
KJ ,
Zhou
Y ,
Williams
R ,
Gogi
K ,
Days
E ,
Jadhav
S ,
Herman
EJ ,
Lavreysen
H ,
Mackie
C ,
Bartolomé
JM ,
Macdonald
GJ ,
Steckler
T ,
Daniels
JS ,
Weaver
CD ,
Niswender
CM ,
Jones
CK ,
Conn
PJ ,
Lindsley
CW ,
Stauffer
SR ,
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of M…
Bioorganic & medicinal chemistry letters.
2012 Oct
15;
22
(20).
6481-5
- PMID: 22981332 [PubMed].
- PMCID: PMC3755010.
- NIHMSID: NIHMS498112
Delpire
E ,
Baranczak
A ,
Waterson
AG ,
Kim
K ,
Kett
N ,
Morrison
RD ,
Daniels
JS ,
Weaver
CD ,
Lindsley
CW ,
Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly select…
Bioorganic & medicinal chemistry letters.
2012 Jul
15;
22
(14).
4532-5
- PMID: 22727639 [PubMed].
- PMCID: PMC3389279.
- NIHMSID: NIHMS383474
Blättermann
S ,
Peters
L ,
Ottersbach
PA ,
Bock
A ,
Konya
V ,
Weaver
CD ,
Gonzalez
A ,
Schröder
R ,
Tyagi
R ,
Luschnig
P ,
Gäb
J ,
Hennen
S ,
Ulven
T ,
Pardo
L ,
Mohr
K ,
Gütschow
M ,
Heinemann
A ,
Kostenis
E ,
A biased ligand for OXE-R uncouples Gα and Gβγ signaling within a heterotrimer.
Nature chemical biology.
2012 Jul
;
8
(7).
631-8
- PMID: 22634634 [PubMed].
Mueller
R ,
Dawson
ES ,
Niswender
CM ,
Butkiewicz
M ,
Hopkins
CR ,
Weaver
CD ,
Lindsley
CW ,
Conn
PJ ,
Meiler
J ,
Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate recep…
Journal of molecular modeling.
2012 Sep
;
18
(9).
4437-46
- PMID: 22592386 [PubMed].
- PMCID: PMC3766737.
- NIHMSID: NIHMS499346
Padula
WV ,
Mishra
MK ,
Weaver
CD ,
Yilmaz
T ,
Splaine
ME ,
Building information for systematic improvement of the prevention of hospital-acquired pressure ulce…
BMJ quality & safety.
2012 Jun
;
21
(6).
473-80
- PMID: 22447820 [PubMed].
Noetzel
MJ ,
Rook
JM ,
Vinson
PN ,
Cho
HP ,
Days
E ,
Zhou
Y ,
Rodriguez
AL ,
Lavreysen
H ,
Stauffer
SR ,
Niswender
CM ,
Xiang
Z ,
Daniels
JS ,
Jones
CK ,
Lindsley
CW ,
Weaver
CD ,
Conn
PJ ,
Functional impact of allosteric agonist activity of selective positive allosteric modulators of meta…
Molecular pharmacology.
2012 Feb
;
81
(2).
120-33
- PMID: 22021324 [PubMed].
- PMCID: PMC3263948.
Noetzel
MJ ,
Rook
JM ,
Vinson
PN ,
Cho
HP ,
Days
E ,
Zhou
Y ,
Rodriguez
AL ,
Lavreysen
H ,
Stauffer
SR ,
Niswender
CM ,
Xiang
Z ,
Daniels
JS ,
Jones
CK ,
Lindsley
CW ,
Weaver
CD ,
Conn
PJ ,
Functional impact of allosteric agonist activity of selective positive allosteric modulators of meta…
Molecular pharmacology.
2012 Feb
;
81
(2).
120-33
- PMID: 22021324 [PubMed].
- PMCID: PMC3263948.
Rodriguez
AL ,
Zhou
Y ,
Williams
R ,
Weaver
CD ,
Vinson
PN ,
Dawson
ES ,
Steckler
T ,
Lavreysen
H ,
Mackie
C ,
Bartolomé
JM ,
Macdonald
GJ ,
Daniels
JS ,
Niswender
CM ,
Jones
CK ,
Conn
PJ ,
Lindsley
CW ,
Stauffer
SR ,
Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonami…
Bioorganic & medicinal chemistry letters.
2012 Dec
15;
22
(24).
7388-92
- PMID: 23142615 [PubMed].
- PMCID: PMC3539767.
- NIHMSID: NIHMS421242
2011
Thorne
CA ,
Lafleur
B ,
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