Kendall Nettles

Kendall Nettles, Ph.D.

Associate Professor

Department: SR-IS&CB-NETTLES LAB
Business Phone: (561) 228-3209
Business Email: k.nettles@ufl.edu

About Kendall Nettles

Related Links:
Additional Positions:
Associate Professor, Cancer Biology
2005 – 2017 · Scripps Research

Research Profile

Open Researcher and Contributor ID (ORCID)

0000-0003-2917-7574

Publications

2022
The SARS-CoV-2 spike protein binds and modulates estrogen receptors.
bioRxiv : the preprint server for biology. [DOI] 10.1101/2022.05.21.492920. [PMID] 35665018.
2021
Activation of Crtc2/Creb1 in skeletal muscle enhances weight loss during intermittent fasting
The FASEB Journal. [DOI] 10.1096/fj.202100171r.
2021
Chemical systems biology reveals mechanisms of glucocorticoid receptor signaling
Nature Chemical Biology. [DOI] 10.1038/s41589-020-00719-w. [PMID] 33510451.
2021
Dual-mechanism estrogen receptor inhibitors
Proceedings of the National Academy of Sciences. [DOI] 10.1073/pnas.2101657118. [PMID] 34452998.
2020
Suppression of breast cancer metastasis and extension of survival by a new antiestrogen in a preclinical model driven by mutant estrogen receptors.
Breast cancer research and treatment. [DOI] 10.1007/s10549-020-05629-y. [PMID] 32277377.
2019
Didehydro-Cortistatin A Inhibits HIV-1 by Specifically Binding to the Unstructured Basic Region of Tat.
mBio. [DOI] 10.1128/mBio.02662-18. [PMID] 30723126.
2019
Pocket similarity identifies selective estrogen receptor modulators as microtubule modulators at the taxane site.
Nature communications. [DOI] 10.1038/s41467-019-08965-w. [PMID] 30833575.
2019
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
Bioorganic & medicinal chemistry letters. [DOI] 10.1016/j.bmcl.2019.01.036. [PMID] 30732944.
2018
Cryptic glucocorticoid receptor-binding sites pervade genomic NF-κB response elements.
Nature communications. [DOI] 10.1038/s41467-018-03780-1. [PMID] 29626214.
2018
The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells.
eLife. [DOI] 10.7554/eLife.37161. [PMID] 30489256.
2017
Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.
Journal of medicinal chemistry. [DOI] 10.1021/acs.jmedchem.7b00585. [PMID] 28657320.
2017
Exploring the Structural Compliancy versus Specificity of the Estrogen Receptor Using Isomeric Three-Dimensional Ligands.
ACS chemical biology. [DOI] 10.1021/acschembio.6b00918. [PMID] 28032978.
2017
Full antagonism of the estrogen receptor without a prototypical ligand side chain.
Nature chemical biology. [DOI] 10.1038/nchembio.2236. [PMID] 27870835.
2017
Structural and Molecular Mechanisms of Cytokine-Mediated Endocrine Resistance in Human Breast Cancer Cells.
Molecular cell. [DOI] 10.1016/j.molcel.2017.02.008. [PMID] 28306507.
2017
Structurally Novel Antiestrogens Elicit Differential Responses from Constitutively Active Mutant Estrogen Receptors in Breast Cancer Cells and Tumors.
Cancer research. [DOI] 10.1158/0008-5472.CAN-17-1265. [PMID] 28904064.
2017
Synthesis of novel steroidal agonists, partial agonists, and antagonists for the glucocorticoid receptor.
Bioorganic & medicinal chemistry letters. [DOI] 10.1016/j.bmcl.2016.11.007. [PMID] 27919657.
2017
Systems Structural Biology Analysis of Ligand Effects on ERα Predicts Cellular Response to Environmental Estrogens and Anti-hormone Therapies.
Cell chemical biology. [DOI] 10.1016/j.chembiol.2016.11.014. [PMID] 28042045.
2017
Tethering not required: the glucocorticoid receptor binds directly to activator protein-1 recognition motifs to repress inflammatory genes.
Nucleic acids research. [DOI] 10.1093/nar/gkx509. [PMID] 28591827.
2016
Crizotinib inhibits NF2-associated schwannoma through inhibition of focal adhesion kinase 1.
Oncotarget. [DOI] 10.18632/oncotarget.10248. [PMID] 27363027.
2016
Predictive features of ligand‐specific signaling through the estrogen receptor
Molecular Systems Biology. [DOI] 10.15252/msb.20156701. [PMID] 27107013.
2015
Dual suppression of estrogenic and inflammatory activities for targeting of endometriosis.
Science translational medicine. [DOI] 10.1126/scitranslmed.3010626. [PMID] 25609169.
2015
Structural mechanism for signal transduction in RXR nuclear receptor heterodimers.
Nature communications. [DOI] 10.1038/ncomms9013. [PMID] 26289479.
2014
Creb coactivators direct anabolic responses and enhance performance of skeletal muscle.
The EMBO journal. [DOI] 10.1002/embj.201386145. [PMID] 24674967.
2014
Resveratrol modulates the inflammatory response via an estrogen receptor-signal integration network.
eLife. [DOI] 10.7554/eLife.02057. [PMID] 24771768.
2014
Triaryl-substituted Schiff bases are high-affinity subtype-selective ligands for the estrogen receptor.
Journal of medicinal chemistry. [DOI] 10.1021/jm500268j. [PMID] 24708493.
2013
Improved crystallographic structures using extensive combinatorial refinement.
Structure (London, England : 1993). [DOI] 10.1016/j.str.2013.07.025. [PMID] 24076406.
2013
Ligand-binding dynamics rewire cellular signaling via estrogen receptor-α.
Nature chemical biology. [DOI] 10.1038/nchembio.1214. [PMID] 23524984.
2013
Thiophene-core estrogen receptor ligands having superagonist activity.
Journal of medicinal chemistry. [DOI] 10.1021/jm400157e. [PMID] 23586645.
2012
Bicyclic core estrogens as full antagonists: synthesis, biological evaluation and structure-activity relationships of estrogen receptor ligands based on bridged oxabicyclic core arylsulfonamides.
Organic & biomolecular chemistry. [DOI] 10.1039/c2ob26531a. [PMID] 23033157.
2012
Development of selective estrogen receptor modulator (SERM)-like activity through an indirect mechanism of estrogen receptor antagonism: defining the binding mode of 7-oxabicyclo[2.2.1]hept-5-ene scaffold core ligands.
ChemMedChem. [DOI] 10.1002/cmdc.201200048. [PMID] 22517684.
2012
Identification and structure-activity relationships of a novel series of estrogen receptor ligands based on 7-thiabicyclo[2.2.1]hept-2-ene-7-oxide.
Journal of medicinal chemistry. [DOI] 10.1021/jm201556r. [PMID] 22283328.
2012
Structural mechanisms of allostery and autoinhibition in JNK family kinases.
Structure (London, England : 1993). [DOI] 10.1016/j.str.2012.09.021. [PMID] 23142346.
2012
The nuclear receptor signalling scaffold: insights from full-length structures.
The EMBO journal. [DOI] 10.1038/emboj.2011.475. [PMID] 22252143.
2011
A crystal structure of a model of the repeating r(CGG) transcript found in fragile X syndrome.
Chembiochem : a European journal of chemical biology. [DOI] 10.1002/cbic.201100337. [PMID] 21766409.
2011
Myotonic dystrophy type 1 RNA crystal structures reveal heterogeneous 1 × 1 nucleotide UU internal loop conformations.
Biochemistry. [DOI] 10.1021/bi2013068. [PMID] 21988728.
2010
Coupling of receptor conformation and ligand orientation determine graded activity.
Nature chemical biology. [DOI] 10.1038/nchembio.451. [PMID] 20924370.
2008
CBP Is a dosage-dependent regulator of nuclear factor-kappaB suppression by the estrogen receptor.
Molecular endocrinology (Baltimore, Md.). [PMID] 17932106.
2008
Insights into PPARgamma from structures with endogenous and covalently bound ligands.
Nature structural & molecular biology. [DOI] 10.1038/nsmb0908-893. [PMID] 18769464.
2008
NFkappaB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses.
Nature chemical biology. [DOI] 10.1038/nchembio.76. [PMID] 18344977.
2007
Elemental isomerism: a boron-nitrogen surrogate for a carbon-carbon double bond increases the chemical diversity of estrogen receptor ligands.
Chemistry & biology. [PMID] 17584613.
2007
Partial agonists activate PPARgamma using a helix 12 independent mechanism.
Structure (London, England : 1993). [PMID] 17937915.
2007
Structural plasticity in the oestrogen receptor ligand-binding domain.
EMBO reports. [PMID] 17468738.
2007
Structure-guided optimization of estrogen receptor binding affinity and antagonist potency of pyrazolopyrimidines with basic side chains.
Journal of medicinal chemistry. [PMID] 17228884.
2005
Ligand control of coregulator recruitment to nuclear receptors.
Annual review of physiology. [PMID] 15709961.
2004
A structural explanation for ERalpha/ERbeta SERM discrimination.
Ernst Schering Research Foundation workshop. [PMID] 15248503.
2004
Allosteric control of ligand selectivity between estrogen receptors alpha and beta: implications for other nuclear receptors.
Molecular cell. [PMID] 14967140.
2003
Nuclear receptor ligands and cofactor recruitment: is there a coactivator “on deck”?
Molecular cell. [PMID] 12718871.
2002
Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism.
Nature structural biology. [PMID] 11953755.
2000
Influence of the ventral hippocampal formation on plasma vasopressin, hypothalamic-pituitary-adrenal axis, and behavioral responses to novel acoustic stress.
Brain research. [PMID] 10700613.
1997
Anterior medial temporal lobe volumes in polydipsic schizophrenic patients with and without hypo-osmolemia: a pilot study.
Biological psychiatry. [PMID] 9347125.
1996
Influence of the hippocampus/subiculum on antidiuretic hormone levels during stress.
Psychoneuroendocrinology. [PMID] 9044442.

Grants

Apr 2022 ACTIVE
Chemical, structural and molecular rules for fully antagonizing the estrogen receptor
Role: Principal Investigator
Funding: NATL INST OF HLTH NCI

Contact Details

Phones:
Business:
(561) 228-3209
Emails:
Business:
k.nettles@ufl.edu
Addresses:
Business Mailing:
Location C238
130 SCRIPPS WAY BLDG 2C2
JUPITER FL 33458