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List of works by R. Kiplin Guy

(+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium.

scientific article

8-Triazolylpurines: Towards Fluorescent Inhibitors of the MDM2/p53 Interaction

scientific article

A Convenient Procedure for Parallel Ester Hydrolysis

scientific article

A Facile One-Pot Synthesis of Symmetrical and Unsymmetrical Acetaldehyde Acetals from Primary Alcohols

scientific article

A Water-Soluble Prodrug of Taxol with Self-Assembling Properties

scientific article

A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors.

scientific article published on January 2009

A high-throughput screen indicates gemcitabine and JAK inhibitors may be useful for treating pediatric AML

scientific article published on 16 May 2019

A high-throughput screening method to identify small molecule inhibitors of thyroid hormone receptor coactivator binding

scientific article published on 27 June 2006

A metallopeptide assembly of the HIV-1 gp41 coiled coil is an ideal receptor in fluorescence detection of ligand binding

scientific article published in November 2003

A novel 2'-(N-methylpyridinium acetate) prodrug of paclitaxel induces superior antitumor responses in preclinical cancer models

scientific article published in September 2002

A novel protein crosslinking reagent for the determination of moderate resolution protein structures by mass spectrometry (MS3-D).

scientific article

A quantitative high-throughput screen identifies novel inhibitors of the interaction of thyroid receptor beta with a peptide of steroid receptor coactivator 2

scientific article

A road less traveled by: exploring a decade of Ellman chemistry.

scientific article

A screening-based approach to circumvent tumor microenvironment-driven intrinsic resistance to BCR-ABL+ inhibitors in Ph+ acute lymphoblastic leukemia

scientific article

A selective irreversible inhibitor targeting a PDZ protein interaction domain.

scientific article published in October 2003

A small diversity library of α-methyl amide analogs of sulindac for probing anticancer structure-activity relationships

scientific article published on 10 May 2018

A solid-phase approach to the phallotoxins: total synthesis of [Ala7]-phalloidin.

scientific article published in June 2005

A surface on the androgen receptor that allosterically regulates coactivator binding

scientific article

Activity of piperaquine and other 4-aminoquinoline antiplasmodial drugs against chloroquine-sensitive and resistant blood-stages of Plasmodium falciparum. Role of beta-haematin inhibition and drug concentration in vacuolar water- and lipid-phases.

scientific article published on 19 March 2007

Amine Containing Analogs of Sulindac for Cancer Prevention

scientific article published on 31 January 2018

An all-purpose antimalarial drug target

scientific article published on June 2012

An alpha-helical peptidomimetic inhibitor of the HIV-1 Rev-RRE interaction

scientific article published in March 2006

An antagonist of dishevelled protein-protein interaction suppresses beta-catenin-dependent tumor cell growth.

scientific article published on January 2007

An automated approach to efficiently reformat a large collection of compounds.

scientific article

An inhibitor of the interaction of thyroid hormone receptor beta and glucocorticoid interacting protein 1.

scientific article

An integrated in vitro and in vivo high-throughput screen identifies treatment leads for ependymoma.

scientific article

Anticancer properties of distinct antimalarial drug classes

scientific article (publication date: 2013)

Antimalarial Activity of Tetrahydro-β-carbolines Targeting the ATP Binding Pocket of the Plasmodium falciparum Heat Shock 90 Protein

scientific article published on 18 August 2020

Antimalarial activity of 10-alkyl/aryl esters and -aminoethylethers of artemisinin.

scientific article published on 3 November 2012

Antimalarial activity of thiosemicarbazones and purine derived nitriles.

scientific article published on 5 May 2009

Antimalarials in development in 2014.

scientific article

Antischistosomal versus antiandrogenic properties of aryl hydantoin Ro 13-3978.

scientific article

Assay Optimization and Screening of RNA-Protein Interactions by AlphaScreen.

scientific article published in October 2007

Benzoflavone activators of the cystic fibrosis transmembrane conductance regulator: towards a pharmacophore model for the nucleotide-binding domain

scientific article published in September 2003

Blocking an N-terminal acetylation-dependent protein interaction inhibits an E3 ligase.

scientific article

Bromodomain-selective BET inhibitors are potent antitumor agents against MYC-driven pediatric cancer

scientific article published on 10 July 2020

CDK2 inhibitors as candidate therapeutics for cisplatin- and noise-induced hearing loss.

scientific article published on 7 March 2018

Chemical approaches to nuclear receptors in metabolism

scientific article

Chemical genetics of Plasmodium falciparum

scientific article (publication date: 20 May 2010)

Chemistry and Biology of Taxol

scientific article

Conformation of a water-soluble derivative of taxol in water by 2D-NMR spectroscopy ⬇️

scientific article published on October 1, 1994

Coregulator interactions with the thyroid hormone receptor.

scientific article

Correction to Targeting the Binding Function 3 (BF3) Site of the Human Androgen Receptor through Virtual Screening

scholarly article published in Journal of Medicinal Chemistry

Correction: Cysteine modification reveals an allosteric inhibitory site on the CAL PDZ domain

scientific article published on 06 July 2018

Cysteine modifiers suggest an allosteric inhibitory site on the CAL PDZ domain

scientific article published on 22 February 2018

Design of a selective chemical probe for class I PDZ domains

scientific article published on 17 October 2006

Design, Synthesis and Evaluation of 2,5-Diketopiperazines as Inhibitors of the MDM2-p53 Interaction

scientific article

Development of a cell-based, high-throughput screening assay for ATM kinase inhibitors.

scientific article published on 24 January 2014

Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models.

scientific article

Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB.

scientific article published on 4 January 2008

Dihydroquinazolinone inhibitors of proliferation of blood and liver stage malaria parasites

scientific article

Discovery of Novel Pyrazolo-pyridone DCN1 Inhibitors Controlling Cullin Neddylation

scientific article published on 13 September 2019

Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia.

scientific article

Discovery of an Orally Bioavailable Inhibitor of Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation

scientific article published on 26 March 2018

Discovery of novel antimalarial compounds enabled by QSAR-based virtual screening

scientific article published on 23 January 2013

Discovery of novel, orally bioavailable, antileishmanial compounds using phenotypic screening.

scientific article published on 29 December 2017

Discovery of potent and selective inhibitors of Trypanosoma brucei ornithine decarboxylase

scientific article

Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain

scientific article published in January 2005

Discovery of small molecule inhibitors of the interaction of the thyroid hormone receptor with transcriptional coregulators

scientific article published on 31 October 2005

Discovery of the first irreversible small molecule inhibitors of the interaction between the vitamin D receptor and coactivators

scientific article published on 16 May 2012

Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB

scientific article published on 8 April 2008

Diverse amide analogs of sulindac for cancer treatment and prevention

scientific article published on 13 September 2017

Diversity-oriented natural product platform identifies plant constituents targeting Plasmodium falciparum

scientific article (publication date: 10 May 2016)

Efficacy of Retinoids in IKZF1-Mutated BCR-ABL1 Acute Lymphoblastic Leukemia

scientific article

Evaluation of 1,1-cyclopropylidene as a thioether isostere in the 4-thio-thienopyrimidine (TTP) series of antimalarials

scientific article published on 11 September 2020

Evaluation of Diarylureas for Activity Against Plasmodium falciparum.

scientific article

Evaluation of artemisinins for the treatment of acute myeloid leukemia.

scientific article published on 28 April 2016

Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).

scientific article published on 2 January 2015

Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.

scientific article published on 4 November 2017

Flexibility is important for inhibition of the MDM2/p53 protein-protein interaction by cyclic β-hairpins

scientific article published on 12 October 2016

Fluorescent taxoids.

scientific article

Gene expression as a drug discovery tool

scientific article published on 01 March 2004

Global phenotypic screening for antimalarials

scientific article

High-throughput assays for promiscuous inhibitors.

scientific article published on 3 July 2005

Hit-to-Lead Studies for the Antimalarial Tetrahydroisoquinolone Carboxanilides

scientific article published on 9 August 2016

Identification and characterization of the first small molecule inhibitor of MDMX

scientific article

Identification of Plasmodium falciparum heat shock 90 inhibitors via molecular docking

scientific article

Identification of Selective Inhibitors of the Plasmodium falciparum Hexose Transporter PfHT by Screening Focused Libraries of Anti-Malarial Compounds

scientific article

Identification of Toll-like receptor signaling inhibitors based on selective activation of hierarchically acting signaling proteins

scientific article published on 14 August 2018

Improvement of Oral Bioavailability of Pyrazolo-Pyridone Inhibitors of the Interaction of DCN1/2 and UBE2M

scientific article

Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors.

scientific article published on July 2009

Inactivation of the p53 pathway in retinoblastoma.

scientific article

Incorporation of an Intramolecular Hydrogen-Bonding Motif in the Side Chain of 4-Aminoquinolines Enhances Activity against Drug-Resistant P. falciparum

scientific article

Incorporation of an intramolecular hydrogen-bonding motif in the side chain of 4-aminoquinolines enhances activity against drug-resistant P. falciparum.

scientific article published on July 2006

Inhibition of a viral enzyme by a small-molecule dimer disruptor

scientific article published on 26 July 2009

Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships.

scientific article

Interaction between the androgen receptor and a segment of its corepressor SHP

scientific article

Investigation of the PDZ domain ligand binding site using chemically modified peptides.

scientific article published in September 2002

Isotopically labeled crosslinking reagents: resolution of mass degeneracy in the identification of crosslinked peptides.

scientific article

LC-MS- and (1)H NMR Spectroscopy-Guided Identification of Antifungal Diterpenoids from Sagittaria latifolia

scientific article published on 15 September 2015

Lead optimization of 3-carboxyl-4(1H)-quinolones to deliver orally bioavailable antimalarials

scientific article

Lead optimization of antimalarial propafenone analogues.

scientific article published on 29 June 2012

Ligand competition binding assay for the androgen receptor.

scientific article

Ligand-selective inhibition of the interaction of steroid receptor coactivators and estrogen receptor isoforms.

scientific article

MAGI-1, a Membrane-associated Guanylate Kinase with a Unique Arrangement of Protein-Protein Interaction Domains ⬇️

scientific article published on December 12, 1997

MDM2 antagonist nutlin-3a reverses mitoxantrone resistance by inhibiting breast cancer resistance protein mediated drug transport ⬇️

scientific article published on July 1, 2011

Methylsulfonylnitrobenzoates, a new class of irreversible inhibitors of the interaction of the thyroid hormone receptor and its obligate coactivators that functionally antagonizes thyroid hormone.

scientific article

Monitoring Ligand-Induced Protein Ordering in Drug Discovery

scientific article published on 23 January 2016

NALP3 inflammasome upregulation and CASP1 cleavage of the glucocorticoid receptor cause glucocorticoid resistance in leukemia cells

scientific article published on 4 May 2015

Nanomolar affinity small molecule correctors of defective Delta F508-CFTR chloride channel gating.

scientific article published on 27 June 2003

Non-competitive androgen receptor inhibition in vitro and in vivo.

scholarly article

Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription

scientific article

Novel selective inhibitors of the interaction of individual nuclear hormone receptors with a mutually shared steroid receptor coactivator 2.

scientific article

On the mechanism of action of SJ-172550 in inhibiting the interaction of MDM4 and p53

scientific article

Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond

scientific article (publication date: July 2016)

Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles

scientific article published on 14 September 2016

Optimization of a Novel Series of Ataxia-Telangiectasia Mutated Kinase Inhibitors as Potential Radiosensitizing Agents

scientific article

Optimization of a non-radioactive high-throughput assay for decarboxylase enzymes.

scientific article

Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT).

scientific article published on 26 March 2013

Optimization of propafenone analogues as antimalarial leads

scientific article published on 10 October 2011

Optimization of purine-nitrile TbcatB inhibitors for use in vivo and evaluation of efficacy in murine models.

scientific article published on 8 October 2010

Optimization of the electrophile of chloronitrobenzamide leads active against Trypanosoma brucei

scientific article published on 23 May 2013

Organocatalytic, diastereo- and enantioselective synthesis of nonsymmetric cis-stilbene diamines: a platform for the preparation of single-enantiomer cis-imidazolines for protein-protein inhibition

scientific article

Oxazole and thiazole analogs of sulindac for cancer prevention

scientific article published on 19 April 2018

Parallel synthesis and antimalarial screening of a 4-aminoquinoline library

scientific article published in May 2004

Parallel synthesis of 9-aminoacridines and their evaluation against chloroquine-resistant Plasmodium falciparum

scientific article published on 10 October 2005

Parallel synthesis of diarylureas and their evaluation as inhibitors of insulin-like growth factor receptor.

scientific article published in September 2006

Partial acetylation of lysine residues improves intraprotein cross-linking.

scientific article

Pemetrexed and gemcitabine as combination therapy for the treatment of Group3 medulloblastoma

scientific article

Pentacyclic nitrofurans that rapidly kill nifurtimox-resistant trypanosomes

scientific article published on 18 December 2015

Performance of a docking/molecular dynamics protocol for virtual screening of nutlin-class inhibitors of Mdmx

scientific article published on 24 February 2017

Pharmacokinetics and efficacy of the spleen tyrosine kinase inhibitor r406 after ocular delivery for retinoblastoma

scientific article

Phenotypic screens reveal posaconazole as rapidly cidal combination partner for treatment of Primary Amoebic Meningoencephalitis

scholarly article by Beatrice L Colon et al published 24 October 2018 in Journal of Infectious Diseases

Piperidinyl Ureas Chemically Control Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation

scientific article published on 26 March 2018

Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1.

scientific article published on 17 October 2007

Podophyllotoxin analogues active versus Trypanosoma brucei

scientific article

Potent Plasmodium falciparum gametocytocidal activity of diaminonaphthoquinones, lead antimalarial chemotypes identified in an antimalarial compound screen.

scientific article

Progress in Small Molecule Therapeutics for the Treatment of Retinoblastoma

scientific article published on 21 July 2015

Proteomimetic libraries: design, synthesis, and evaluation of p53-MDM2 interaction inhibitors.

scientific article published in May 2006

Quantification of the vitamin D receptor-coregulator interaction

scientific article

Quantitative proteomics of the thyroid hormone receptor-coregulator interactions

scientific article

Quinolone-3-diarylethers: a new class of antimalarial drug.

scientific article published in March 2013

Rapid repurposing of drugs for COVID-19

scientific article published on 08 May 2020

Rational design of a nonpeptide general chemical scaffold for reversible inhibition of PDZ domain interactions.

scientific article published on 6 October 2006

Report of the 2018-2019 Research and Graduate Affairs Committee

scientific article published on 01 December 2019

Reporting data from high-throughput screening of small-molecule libraries

scientific article

Repositioning: the fast track to new anti-malarial medicines?

scientific article

Role of electrostatic interactions in PDZ domain ligand recognition

scientific article published in March 2003

Safety, tolerability, pharmacokinetics, and antimalarial efficacy of a novel Plasmodium falciparum ATP4 inhibitor SJ733: a first-in-human and induced blood-stage malaria phase 1a/b trial

scientific article published on 07 April 2020

Scaffold composition and biological relevance of screening libraries.

scientific article

Screening and Development of New Inhibitors of FtsZ from M. Tuberculosis

scientific article

Searching for new antimalarial therapeutics amongst known drugs

scientific article

Seeking the Elusive Long-Acting Ozonide: Discovery of Artefenomel (OZ439).

scientific article published on 15 March 2017

Shared Consensus Machine Learning Models for Predicting Blood Stage Malaria Inhibition

scientific article

Similarities and differences between two modes of antagonism of the thyroid hormone receptor.

scientific article published on 15 August 2011

Steroid receptor coactivator peptidomimetics

scientific article published in January 2003

Structural analyses reveal phosphatidyl inositols as ligands for the NR5 orphan receptors SF-1 and LRH-1.

scientific article published on February 2005

Structural insight into the mode of action of a direct inhibitor of coregulator binding to the thyroid hormone receptor

scientific article

Structure-activity relationship study of 9-aminoacridine compounds in scrapie-infected neuroblastoma cells

scientific article published on 24 July 2006

Structure-guided development of selective TbcatB inhibitors

scientific article published on October 2009

Synthesis and characterization of BODIPY-labeled colchicine.

scientific article published on 20 July 2008

Synthesis and evaluation of 7-substituted 4-aminoquinoline analogues for antimalarial activity

scientific article published on 26 September 2011

Synthesis and evaluation of methylsulfonylnitrobenzamides (MSNBAs) as inhibitors of the thyroid hormone receptor-coactivator interaction.

scientific article published on 8 January 2013

Synthesis and evaluation of sulfonylnitrophenylthiazoles (SNPTs) as thyroid hormone receptor-coactivator interaction inhibitors.

scientific article published on 23 February 2012

Synthesis and structure-activity relationship of dual-stage antimalarial pyrazolo[3,4-b]pyridines

scientific article published on 18 September 2020

Synthesis and structure-activity relationships of antimalarial 4-oxo-3-carboxyl quinolones.

scientific article published on 11 February 2010

Synthesis and testing of a focused phenothiazine library for binding to HIV-1 TAR RNA.

scientific article published in September 2006

Synthesis of C-2 Taxol Analogues

scientific article

Synthesis of a fully functionalized CD ring system of taxol

article

Synthesis of artemiside and its effects in combination with conventional drugs against severe murine malaria

scientific article published on 17 October 2011

Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors

scientific article published on 4 August 2006

Synthesis of medium ring heterocycles using an intramolecular Heck reaction

scientific article published on 01 August 2004

Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities.

scientific article published on February 2005

Targeting Histone Demethylases in MYC-Driven Neuroblastomas with Ciclopirox

scientific article published on 6 July 2017

Targeting the binding function 3 (BF3) site of the human androgen receptor through virtual screening.

scientific article

Targeting the regulation of androgen receptor signaling by the heat shock protein 90 cochaperone FKBP52 in prostate cancer cells

scientific article

The interdependence between screening methods and screening libraries.

scientific article

The molecular mechanisms of coactivator utilization in ligand-dependent transactivation by the androgen receptor

scientific article

Total Synthesis of Taxol. 1. Retrosynthesis, Degradation, and Reconstitution

scientific article (publication date: 1995)

Total Synthesis of Taxol. 3. Formation of Taxol's ABC Ring Skeleton

scientific article published in 1995

Total Synthesis of taxol. 2. Construction of A and C ring intermediates and initial attempts to construct the ABC ring system

scientific article (publication date: 1995)

Total synthesis of taxol

scientific article (publication date: 17 February 1994)

Treatment of murine cerebral malaria by artemisone in combination with conventional antimalarial drugs: antiplasmodial effects and immune responses.

scientific article

UPLC-MS-ELSD-PDA as a powerful dereplication tool to facilitate compound identification from small-molecule natural product libraries

scientific article

University-pharmacy partnerships for COVID-19

scientific article

Ventromorphins: A New Class of Small Molecule Activators of the Canonical BMP Signaling Pathway

scientific article

Ventromorphins: A New Class of Small Molecule Activators of the Canonical BMP Signaling Pathway

scientific article published on 28 June 2019

Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.

scientific article

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