Fesik Lab Publications
2018
Shaw
S ,
Bian
Z ,
Zhao
B ,
Tarr
JC ,
Veerasamy
N ,
Jeon
KO ,
Belmar
J ,
Arnold
AL ,
Fogarty
SA ,
Perry
E ,
Sensintaffar
JL ,
Camper
DV ,
Rossanese
OW ,
Lee
T ,
Olejniczak
ET ,
Fesik
SW ,
Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors…
Journal of medicinal chemistry.
2018 Mar
22;
61
(6).
2410-2421
- PMID: 29323899 [PubMed].
Howes
JE ,
Akan
DT ,
Burns
MC ,
Rossanese
OW ,
Waterson
AG ,
Fesik
SW ,
Small molecule-mediated activation of RAS elicits biphasic modulation of phospho ERK levels that are…
Molecular cancer therapeutics.
2018 Feb
13;
- PMID: 29440291 [PubMed].
Burns
MC ,
Howes
JE ,
Sun
Q ,
Little
AJ ,
Camper
DV ,
Abbott
JR ,
Phan
J ,
Lee
T ,
Waterson
AG ,
Rossanese
OW ,
Fesik
SW ,
High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and pertur…
Analytical biochemistry.
2018 Feb
11;
548
44-52
- PMID: 29444450 [PubMed].
2017
Zhao
B ,
Sensintaffar
J ,
Bian
Z ,
Belmar
J ,
Lee
T ,
Olejniczak
ET ,
Fesik
SW ,
Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin…
Bioorganic & medicinal chemistry.
2017 Dec
15;
25
(12).
3087-3092
- PMID: 28428041 [PubMed].
Lee
KM ,
Giltnane
JM ,
Balko
JM ,
Schwarz
LJ ,
Guerrero-Zotano
AL ,
Hutchinson
KE ,
Nixon
MJ ,
Estrada
MV ,
Sánchez
V ,
Sanders
ME ,
Lee
T ,
Gómez
H ,
Lluch
A ,
Pérez-Fidalgo
JA ,
Wolf
MM ,
Andrejeva
G ,
Rathmell
JC ,
Fesik
SW ,
Arteaga
CL ,
MYC and MCL1 Cooperatively Promote Chemotherapy-Resistant Breast Cancer Stem Cells via Regulation of…
Cell metabolism.
2017 Oct
3;
26
(4).
633-647.e7
- PMID: 28978427 [PubMed].
- PMCID: PMC5650077.
- NIHMSID: NIHMS910106
Lee
T ,
Bian
Z ,
Zhao
B ,
Hogdal
LJ ,
Sensintaffar
JL ,
Goodwin
CM ,
Belmar
J ,
Shaw
S ,
Tarr
JC ,
Veerasamy
N ,
Matulis
SM ,
Koss
B ,
Fischer
MA ,
Arnold
AL ,
Camper
DV ,
Browning
CF ,
Rossanese
OW ,
Budhraja
A ,
Opferman
J ,
Boise
LH ,
Savona
MR ,
Letai
A ,
Olejniczak
ET ,
Fesik
SW ,
Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors.
FEBS letters.
2017 Jan
;
591
(1).
240-251
- PMID: 27878989 [PubMed].
- PMCID: PMC5381274.
- NIHMSID: NIHMS831578
2016
Erlanson
DA ,
Fesik
SW ,
Hubbard
RE ,
Jahnke
W ,
Jhoti
H ,
Twenty years on: the impact of fragments on drug discovery.
Nature reviews. Drug discovery.
2016 Dec
;
15
(9).
605-19
- PMID: 27417849 [PubMed].
Patrone
JD ,
Pelz
NF ,
Bates
BS ,
Souza-Fagundes
EM ,
Vangamudi
B ,
Camper
DV ,
Kuznetsov
AG ,
Browning
CF ,
Feldkamp
MD ,
Frank
AO ,
Gilston
BA ,
Olejniczak
ET ,
Rossanese
OW ,
Waterson
AG ,
Chazin
WJ ,
Fesik
SW ,
Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A.
ChemMedChem.
2016 Jan
8;
- PMID: 26748787 [PubMed].
Pelz
NF ,
Bian
Z ,
Zhao
B ,
Shaw
S ,
Tarr
JC ,
Belmar
J ,
Gregg
C ,
Camper
DV ,
Goodwin
CM ,
Arnold
AL ,
Sensintaffar
JL ,
Friberg
A ,
Rossanese
OW ,
Lee
T ,
Olejniczak
ET ,
Fesik
SW ,
Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Base…
Journal of medicinal chemistry.
2016 Mar
10;
59
(5).
2054-66
- PMID: 26878343 [PubMed].
2015
Belmar
J ,
Fesik
SW ,
Small molecule Mcl-1 inhibitors for the treatment of cancer.
Pharmacology & therapeutics.
2015 Jan
;
145
76-84
- PMID: 25172548 [PubMed].
- PMCID: PMC4340597.
- NIHMSID: NIHMS629203
Goodwin
CM ,
Rossanese
OW ,
Olejniczak
ET ,
Fesik
SW ,
Myeloid cell leukemia-1 is an important apoptotic survival factor in triple-negative breast cancer.
Cell death and differentiation.
2015 Dec
;
22
(12).
2098-106
- PMID: 26045046 [PubMed].
Burke
JP ,
Bian
Z ,
Shaw
S ,
Zhao
B ,
Goodwin
CM ,
Belmar
J ,
Browning
CF ,
Vigil
D ,
Friberg
A ,
Camper
DV ,
Rossanese
OW ,
Lee
T ,
Olejniczak
ET ,
Fesik
SW ,
Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structur…
Journal of medicinal chemistry.
2015 May
14;
58
(9).
3794-805
- PMID: 25844895 [PubMed].
Thomas
LR ,
Wang
Q ,
Grieb
BC ,
Phan
J ,
Foshage
AM ,
Sun
Q ,
Olejniczak
ET ,
Clark
T ,
Dey
S ,
Lorey
S ,
Alicie
B ,
Howard
GC ,
Cawthon
B ,
Ess
KC ,
Eischen
CM ,
Zhao
Z ,
Fesik
SW ,
Tansey
WP ,
Interaction with WDR5 promotes target gene recognition and tumorigenesis by MYC.
Molecular cell.
2015 May
7;
58
(3).
440-52
- PMID: 25818646 [PubMed].
- PMCID: PMC4427524.
- NIHMSID: NIHMS667450
Waterson
AG ,
Kennedy
JP ,
Patrone
JD ,
Pelz
NF ,
Feldkamp
MD ,
Frank
AO ,
Vangamudi
B ,
Souza-Fagundes
EM ,
Rossanese
OW ,
Chazin
WJ ,
Fesik
SW ,
Diphenylpyrazoles as replication protein a inhibitors.
ACS medicinal chemistry letters.
2015 Feb
12;
6
(2).
140-5
- PMID: 25699140 [PubMed].
- PMCID: PMC4329576.
2014
Sun
Q ,
Phan
J ,
Friberg
AR ,
Camper
DV ,
Olejniczak
ET ,
Fesik
SW ,
A method for the second-site screening of K-Ras in the presence of a covalently attached first-site …
Journal of biomolecular NMR.
2014 Sep
;
60
(1).
11-4
- PMID: 25087006 [PubMed].
- PMCID: PMC4358732.
- NIHMSID: NIHMS667573
Cox
AD ,
Fesik
SW ,
Kimmelman
AC ,
Luo
J ,
Der
CJ ,
Drugging the undruggable RAS: Mission possible?
Nature reviews. Drug discovery.
2014 Nov
;
13
(11).
828-51
- PMID: 25323927 [PubMed].
- PMCID: PMC4355017.
- NIHMSID: NIHMS648334
Harner
MJ ,
Chauder
BA ,
Phan
J ,
Fesik
SW ,
Fragment-based screening of the bromodomain of ATAD2.
Journal of medicinal chemistry.
2014 Nov
26;
57
(22).
9687-92
- PMID: 25314628 [PubMed].
- PMCID: PMC4255743.
Frank
AO ,
Vangamudi
B ,
Feldkamp
MD ,
Souza-Fagundes
EM ,
Luzwick
JW ,
Cortez
D ,
Olejniczak
ET ,
Waterson
AG ,
Rossanese
OW ,
Chazin
WJ ,
Fesik
SW ,
Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A.
Journal of medicinal chemistry.
2014 Mar
27;
57
(6).
2455-61
- PMID: 24491171 [PubMed].
- PMCID: PMC3969094.
Burns
MC ,
Sun
Q ,
Daniels
RN ,
Camper
D ,
Kennedy
JP ,
Phan
J ,
Olejniczak
ET ,
Lee
T ,
Waterson
AG ,
Rossanese
OW ,
Fesik
SW ,
Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange.
Proceedings of the National Academy of Sciences of the United States of America.
2014 Mar
4;
111
(9).
3401-6
- PMID: 24550516 [PubMed].
- PMCID: PMC3948241.
2013
Harner
MJ ,
Frank
AO ,
Fesik
SW ,
Fragment-based drug discovery using NMR spectroscopy.
Journal of biomolecular NMR.
2013 Jun
;
56
(2).
65-75
- PMID: 23686385 [PubMed].
- PMCID: PMC3699969.
- NIHMSID: NIHMS482117
Patrone
JD ,
Kennedy
JP ,
Frank
AO ,
Feldkamp
MD ,
Vangamudi
B ,
Pelz
NF ,
Rossanese
OW ,
Waterson
AG ,
Chazin
WJ ,
Fesik
SW ,
Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A.
ACS medicinal chemistry letters.
2013 Jul
11;
4
(7).
601-605
- PMID: 23914285 [PubMed].
- PMCID: PMC3728914.
- NIHMSID: NIHMS480655
Li
L ,
Wang
R ,
Wilcox
D ,
Sarthy
A ,
Lin
X ,
Huang
X ,
Tian
L ,
Dande
P ,
Hubbard
RD ,
Hansen
TM ,
Wada
C ,
Zhao
X ,
Kohlbrenner
WM ,
Fesik
SW ,
Shen
Y ,
Developing lipid nanoparticle-based siRNA therapeutics for hepatocellular carcinoma using an integra…
Molecular cancer therapeutics.
2013 Nov
;
12
(11).
2308-18
- PMID: 23943805 [PubMed].
Feldkamp
MD ,
Frank
AO ,
Kennedy
JP ,
Patrone
JD ,
Vangamudi
B ,
Waterson
AG ,
Fesik
SW ,
Chazin
WJ ,
Surface reengineering of RPA70N enables cocrystallization with an inhibitor of the replication prote…
Biochemistry.
2013 Sep
17;
52
(37).
6515-24
- PMID: 23962067 [PubMed].
- PMCID: PMC3804075.
- NIHMSID: NIHMS518404
Frank
AO ,
Feldkamp
MD ,
Kennedy
JP ,
Waterson
AG ,
Pelz
NF ,
Patrone
JD ,
Vangamudi
B ,
Camper
DV ,
Rossanese
OW ,
Chazin
WJ ,
Fesik
SW ,
Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragme…
Journal of medicinal chemistry.
2013 Nov
27;
56
(22).
9242-50
- PMID: 24147804 [PubMed].
- PMCID: PMC3932990.
- NIHMSID: NIHMS536706
Friberg
A ,
Vigil
D ,
Zhao
B ,
Daniels
RN ,
Burke
JP ,
Garcia-Barrantes
PM ,
Camper
D ,
Chauder
BA ,
Lee
T ,
Olejniczak
ET ,
Fesik
SW ,
Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and stru…
Journal of medicinal chemistry.
2013 Jan
10;
56
(1).
15-30
- PMID: 23244564 [PubMed].
- PMCID: PMC3646517.
- NIHMSID: NIHMS429806
2012
Sun
Q ,
Burke
JP ,
Phan
J ,
Burns
MC ,
Olejniczak
ET ,
Waterson
AG ,
Lee
T ,
Rossanese
OW ,
Fesik
SW ,
Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation.
Angewandte Chemie (International ed. in English).
2012 Jun
18;
51
(25).
6140-3
- PMID: 22566140 [PubMed].
- PMCID: PMC3620661.
- NIHMSID: NIHMS379240
Souza-Fagundes
EM ,
Frank
AO ,
Feldkamp
MD ,
Dorset
DC ,
Chazin
WJ ,
Rossanese
OW ,
Olejniczak
ET ,
Fesik
SW ,
A high-throughput fluorescence polarization anisotropy assay for the 70N domain of replication prote…
Analytical biochemistry.
2012 Feb
15;
421
(2).
742-9
- PMID: 22197419 [PubMed].
- PMCID: PMC3274598.
- NIHMSID: NIHMS342215
1997
Olejniczak
ET ,
Hajduk
PJ ,
Marcotte
PA ,
Nettesheim
D ,
Meadows
RP ,
Edalji
R ,
Holzman
TF ,
Fesik
SW ,
Stromelysin inhibitors designed from weakly bound fragments: Effects of linking and cooperativity
Journal of the American Chemical Society.
1997 Jun
25;
25
(119).
5828-5832
Hadjuk
PJ ,
Sheppard
G ,
Nettesheim
D ,
Olejniczak
ET ,
Shuker
SB ,
Meadows
RP ,
Steinman
DH ,
Carrera
GM ,
Marcotte
PA ,
Severin
J ,
Walter
K ,
Smith
H ,
Gubbins
E ,
Simmer
R ,
Holzman
TF ,
Morgan
DW ,
Davidsen
SK ,
Summers
JB ,
Fesik
SW ,
Discovery of potent nonpeptide inhibitors of stromelysin using SAR by NMR
Journal of the American Chemical Society.
1997 Jun
25;
25
(119).
5818-5827
Sattler
M ,
Liang
H ,
Nettesheim
D ,
Meadows
RP ,
Harlan
JE ,
Eberstadt
M ,
Yoon
HS ,
Shuker
SB ,
Chang
BS ,
Minn
AJ ,
Thompson
CB ,
Fesik
SW ,
Structure of Bcl-xL/Bak peptide complex: Recognition between regulators of apoptosis
Science.
1997 Feb
14;
275
(5302).
983-986
- PMID: 9020082 [PubMed].
Minn
AJ ,
Velez
P ,
Schendel
SL ,
Liang
H ,
Muchmore
SW ,
Fesik
SW ,
Fill
M ,
Thompson
CB ,
Bcl-x(L) forms an ion channel in synthetic lipid membranes
Nature.
1997 Jan
23;
385
(6614).
353-357
- PMID: 9002522 [PubMed].
1996
Huang
B ,
Eberstadt
M ,
Olejniczak
ET ,
Meadows
RP ,
Fesik
SW ,
NMR structure and mutagenesis of the Fas (APO-1/CD95) death domain
Nature.
1996 Dec
19;
384
(6610).
638-641
- PMID: 8967952 [PubMed].
Shuker
SB ,
Hadjuk
PJ ,
Meadows
RP ,
Fesik
SW ,
Discovering high-affinity ligands for proteins: SAR by NMR
Science.
1996 Nov
29;
274
(5292).
1531-1534
- PMID: 8929414 [PubMed].
Muchmore
SW ,
Sattler
M ,
Liang
H ,
Meadows
RP ,
Harlan
JE ,
Yoon
HS ,
Nettesheim
D ,
Chang
BS ,
Thompson
CB ,
Wong
SL ,
Ng
SL ,
Fesik
SW ,
X-ray and NMR structure of human Bcl-xL, an inhibitor of programmed cell death
Nature.
1996 May
23;
381
(6580).
335-341
- PMID: 8692274 [PubMed].
1995
Zhou
MM ,
Ravichandran
KS ,
Olejniczak
EF ,
Petros
AM ,
Meadows
RP ,
Sattler
M ,
Harlan
JE ,
Wade
WS ,
Burakoff
SJ ,
Fesik
SW ,
Structure and ligand recognition of the phosphotyrosine binding domain of Shc
Nature.
1995 Dec
7;
378
(6557).
584-592
- PMID: 8524391 [PubMed].
1994
Harlan
JE ,
Hajduk
PJ ,
Yoon
HS ,
Fesik
SW ,
Pleckstrin homology domains bind to phosphatidylinositol 4,5-bisphosphate
Nature.
1994 Sep
8;
271
(6493).
168-170
- PMID: 8072546 [PubMed].
Yoon
HS ,
Hajduk
PJ ,
Petros
AM ,
Olejniczak
ET ,
Meadows
RP ,
Fesik
SW ,
Solution structure of a pleckstrin homology domain
Nature.
1994 Jun
23;
(369).
672–675
1993
Thériault
Y ,
Logan
TM ,
Meadows
R ,
Yu
L ,
Olejniczak
ET ,
Holzman
TF ,
Simmer
RL ,
Fesik
SW ,
Solution structure of the cyclosporin A/cyclophilin complex by NMR
Nature.
1993 Jan
7;
361
(6407).
88-91
- PMID: 8421500 [PubMed].
1990
Fesik
SW ,
Gampe
RT ,
Holzman
TF ,
Egan
DA ,
Edalji
R ,
Luly
JR ,
Simmer
R ,
Helfrich
R ,
Kishore
V ,
Rich
DH ,
Isotope-edited NMR of cyclosporin A bound to cyclophilin: Evidence for a trans 9,10 amide bond.
Science.
1990 Dec
7;
250
(4986).
1406-1409
Fesik
SW ,
Eaton
HL ,
Olejniczak
ET ,
Zuiderweg
ERP ,
McIntosh
LP ,
Dahlquist
FW ,
2D and 3D NMR Spectroscopy employing 13C-13C magnetization transfer by isotropic mixing. Spin system identification in large proteins
Journal of the American Chemical Society.
1990 Jan
1;
112
(2).
886-888
1988
Fesik
SW ,
Zuiderweg
ERP ,
Heteronuclear three-dimensional NMR spectroscopy. A strategy for the simplification of homonuclear two-dimensional NMR spectra
Journal of Magnetic Resonance .
1988 Jul
;
78
(3).
588-593
Fesik
SW ,
Isotope-edited NMR spectroscopy
Nature.
1988 Apr
28;
(332).
865-866