Vanderbilt Institute of Chemical Biology

 

 

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VICB 2016-2017 Fall Winter Seminar Schedule

 

 

Fall 2016
Seminar Schedule


Andrew Mesecar

Purdue University

 

"Selective (Yin) and Broad-Spectrum (Yang) Targeting of Coronavirus Proteases" 

 

Wednesday, September 7, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

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Key Lecture Points:
· The main interest of the Mesecar lab is the structure & function of enzymes of biomedical importance.
· One of our fundamental goals is to gain a deeper understanding into the roles of protein dynamics and conformational changes in the molecular recognition and catalytic processes and to exploit this knowledge for the design of small molecule drugs that target these enzymes.
· We are currently studying the structure and function of enzymes involved in cancer chemoprevention, cancer cell proliferation and bacterial and viral pathogenesis.
· We are actively involved in the discovery of both natural and synthetic compounds that can be used as anti-cancer, anti-viral and anti-bacterial therapeutics, as well as compounds that can prevent cancer and promote cell longevity.

David Sweatt

Vanderbilt University

 

"Targeting the Epigenome for Cognitive Enhancement" 

 

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Key Lecture Points:
· An overview of epigenetic mechanisms and the discovery of their role in behavioral learning.

· Pharmacological and genetic evidence that targeting the epigenome can regulate memory formation in the CNS.

· Speculations that the epigenome might represent a particularly rich set of targets for drug development in the area of cognitive dysfunction.

 

Wednesday, September 14, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

Christian Melander

NC State University

 

"Antibiotic Adjuvants Based Upon Nitrogen Dense Marine Alkaloids"  

 

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Key Lecture Points:
· Antibiotic Resistance
· Marine Alkaloid Derivatives
· Antibiotic Adjuvants

 

Wednesday, September 21, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

Zhiqiang An

UT Health science center, houston

 

Lecture #1 This Week

 

"Chemistry and Biology of the Echinocandin Family of Antifungal Drugs"

 

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Key Lecture Points:
· Genetic manipulation of the pneumocandin biosynthetic pathway for generation of analogues
· Evolution of chemical diversity in echinocandin lipopeptide antifungal metabolites
· Functional operons in secondary metabolic gene clusters in the fungus Glarea lozoyensis

 

Wednesday, September 28, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

David Craik

University of queensland, australia

 

Lecture #2 This Week

 

"Cyclic peptides in plants and animals and their applications in drug design"

 

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Key Lecture Points:
· Peptide-based drug design
· Structural biology
· Production of pharmaceuticals in plants

 

Friday, September 30, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

Jack Taunton

UC - San francisco

 

"Targeting Protein Biogenesis as a Therapeutic Strategy for Cancer"

 

Key Lecture Points:
· Our lab is broadly interested in structure-based design of covalent inhibitors and the study of cyclic peptide natural products with novel mechanisms of action
· Cotransin cyclic peptides inhibit Sec61-mediated translocation of nascent secretory proteins into the endoplasmic reticulum
· Ternatin, an unrelated cyclic peptide natural product, kills cancer cells by interfering with a translation elongation complex.

 

Wednesday, October 5, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

Jeff Conn

Vanderbilt university

 

"Allosteric Modulators of Muscarinic Acetylcholine Receptors as a Novel Approach for Treatment of Schizophrenia"

 

Key Lecture Points:
· Early studies with non-selective muscarinic receptor agonists suggest that these compounds can reduce multiple symptoms in schizophrenia patients
· All traditional muscarinic agonists lack selectivity for individual receptor subtypes and have adverse effects by activation of peripheral muscarinic receptors
· We have developed and optimized highly selective positive allosteric modulators (PAMs) of individual mAChR subtypes and found that selective PAMs for M1 or M4 have robust efficacy in rodent models of different symptom clusters
· Optimized drug candidates for M1 and M4 are now advancing towards future clinical studies

 

Wednesday, October 12, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

John Jay Schneekloth, Jr.

NIH, center for cancer research

 

"Targeting Structurally and Functionally Diverse Nucleic Acids with Druglike Small Molecules" 

 

Research Topics:
· Small Molecule Probes of Protein Sumoylation
· Mechanistic probes, natural products, and synthetic inhibitors
· Identification of RNA- and DNA-binding Small Molecules Using Small Molecule Microarrays

 

Wednesday, October 19, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

Daniel Nomura

uc berkeley

 

"Using Chemoproteomic and Metabolomic Platforms to Map Drivers of Human Disease"

 

Key Lecture Points:
· Chemoproteomic and metabolomic platforms can be used to identify, characterize, and pharmacologically target metabolic drivers of human disease

 

Wednesday, October 26, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

Tarun Kapoor

Rockefeller university

 

"Leveraging Resistance to Uncover Mechanisms of Action of Drugs and New Chemical Probes"

 

Key Lecture Points:
· Identifying new chemical probes for dynamic cellular processes

· Using chemical biology to dissect cell division mechanisms

· Combining genomics and chemical biology to unravel mechanisms of action of chemotherapeutic agents

 

Wednesday, November 2, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

Anthony Kossiakoff

university of chicago

 

"Modifying Biological Function Using Conformational Trapping By Customized Synthetic Antibodies"

 

Seminar Co-Sponsored by the Center for Structural Biology (CSB)

 

Key Lecture Points:
· Antibody Engineering
· Phage display
· Conformation trapping

 

Wednesday, November 9, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

Leonard Rome

UClA

 

"Vault Nanoparticles for Immuno-Oncology and Therapeutic Vaccines"

 

Key Lecture Points:
· Vaults are novel nano-scale particles first described in 1986 and found to exist in thousands of copies in most eukaryotic cells

· They have an intricate shape composed of multiple arches reminiscent of cathedral vaults, hence their name
· Vault size (~74 x 42 x 42 nm), shape, molecular composition and facile assembly suggest that they have the potential to be engineered to deliver of a wide variety of therapeutics
· A number of strategies are under development to encapsulate immune modulators into the vault particle for use in cancer immunotherapy and vaccine production

 

Wednesday, November 30, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

Samie Jaffrey

Cornell University

 

Samie Jaffrey "Imaging RNA and RNA Biology Using RNA Mimics of Green Fluorescent Protein"

 

Key Lecture Points:
· RNA imaging
· RNA trafficking
· Metabolite sensors

 

Wednesday, December 7, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

Douglas Green

St. jude children's research hospital

 

"LC3-Associated Phagocytosis: Two Ancient Pathways Converge on Innate Immunity, Inflammation, and Aging"

SEMINAR CANCELLED

Wednesday, December 14, 2016

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Key Lecture Points:
· The phenomenon of LC-3 associated phagocytosis (LAP) =
· How LAP is distinct from autophagy
· How LAP controls auto-inflammation, innate immunity, and vision
· How LAP influences cancer

  Winter-Spring 2017
Seminar Schedule

Craig Lindsley

Vanderbilt university

 

"Allosteric Modulation: Challenges for Medicinal Chemistry and Opportunities to Improve Human Health"  

 

Key Lecture Points:

· Overview of allosteric modulation of GPCRs, Kinases and other targets

· Strategies to mitigate 'steep' SAR with allosteric modulators

· Signal Bias to avoid adverse effect liabilities

· The importance of phenotypic screens in lead optimization to avoid AE-prone series

 

Wednesday, January 4, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

Natalie Ahn

uc boulder

 

"The Importance of Protein Dynamics for Kinase Activation and Implications for Inhibitor Design: The Case of ERK2"

 

Key Lecture Points:
· Changes in protein motions accompany phosphorylation and activation of ERK2

· These motions are needed for allosteric regulation, in a manner that may link dynamics to the reaction cycle

· This allostery can be exploited by small molecules to confer favorable properties of inhibition

 

Wednesday, January 11, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Jonathan Ellman

Yale university

 

"Development of PTP Inhibitors and Privileged Heterocycle Synthesis by C-H Functionalization"

 

Wednesday, January 18, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Key Lecture Points:

· New strategies for the development and application of protein tyrosine phosphatase (PTP) inhibitors.

· Convergent, regio- and stereoselective C-H functionalization cascades for the rapid synthesis of piperidines, including fused and bridged bi- and tricyclic derivatives as well as natural product and drug synthesis applications.

Abigail Doyle

Princeton University

 

"New Directions in Ni-Catalyzed Cross Coupling"

 

Co-Hosted by the Department of Chemistry (Ingersoll Lecture)

 

Wednesday, January 25, 2017
3:30 - 4:50 P.M. (Refreshments at 3:30, seminar starting promptly at 3:45)

208 Light Hall

 

Research Overview:

· Our laboratory has identified two strategies that achieve mild and efficient nucleophilic fluorination using transition metal catalysis

· These stereoselective methods represent platforms for the invention of a wide spectrum of chemical transformations

· We are interested in assembling a better understanding of the properties and reactivity of transition metal fluorides

Lorraine Gudas

Cornell University

 

"Nuclear Receptor Selective Agonists for the Prevention and Treatment of Cancer and Diabetes"

 

Wednesday, February 1, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Research Overview:

The Gudas laboratory performs pharmacology research in four major areas:

· Retinoids, which include both natural and synthetic derivatives of vitamin A (retinol)

· A murine model of human head and neck and esophageal squamous cell carcinomas (SCCs)

· A murine model of human clear cell renal cell carcinoma

· Development of new drugs for type 2 diabetes and fatty liver disease

John McLean

Vanderbilt university

 

"Molecular phenomics in systems, synthetic, and chemical biology" 

 

Wednesday, February 8, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Key Lecture Points:
· Integrated omics using structural mass spectrometry
· Generation of high fidelity big data
· Informatics strategies to transform big data into information

Matthew Bogyo

stanford University

 

"Chemical Tools for the Study of Protease Function"

 

Co-Hosted by the Chemical Biology Association of Students (CBAS)

 

Wednesday, February 15, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Key Lecture Points:
· Applications of protease probes to imaging cancer
· Development of probes for imaging infectious diseases
· Using chemical probes for drug development efforts

David Aronoff

vanderbilt university

 

"Modeling Innate Immunity in Fetal Membranes"

 

Wednesday, February 22, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Key Lecture Points:
· The fetal membranes are a deceptively simple structure surrounding the developing fetus and amniotic fluid during pregnancy

· Infection of the fetal membranes, a condition known as chorioamnionitis, is an important cause of preterm birth and premature rupture of the membranes

· Despite the central role for fetal membranes in defending the pregnant uterus against infection, we know very little about the nature of innate immunity in the membranes or how microbes evade host defense to cause chorioamnionitis

· Our multidisciplinary research team is using in vitro, ex vivo and in vivo methods to define host-microbial interactions important to the pathogenesis of chorioamnionitis and its consequences.

Scott Snyder

University of chicago

 

"Strategies to Rapidly Create Molecular Complexity"

 

Wednesday, March 1, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Key Lecture Points:
· Natural product synthesis from common intermediates to prepare entire families of structures
• Developing new tools and reaction processes to build complexity
• Identifying ways to differentiate similar functional groups on polyfunctional molecules

Wendy Thomas

University of Washington

 

"Bacteria Use Fluid Flow to Strengthen Adhesion"

 

Wednesday, March 8, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Key Lecture Points:
· Bacteria and blood cells have evolved mechanisms to specifically target immobilized receptors over those circulating in bodily fluids
· Adhesive receptor-ligand interactions called "catch bonds" are activated instead of overpowered by tensile mechanical force
· Cells utilize hydrodynamic processes like lift and margination that move cells away from or towards surfaces in flow

Tomas Cihlar

Gilead sciences

 

"Therapeutic Approaches Towards HIV Remission and Cure"  

 

Wednesday, March 15, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Key Lecture Points:
· HIV infection cannot be cured with direct antivirals and patients require life-long therapy
· Persistence of HIV infection is due to long-lived latent viral reservoir that is not affected by antiviral treatment
· Specific reservoir-targeting therapeutic strategies are needed to achieve long term drug-free remission and potentially cure of HIV
· Research is focused on HIV latency reversal combined with immune-based therapies including effector antibodies and therapeutic vaccines

Thomas Bernhardt

harvard medical school

 

"Getting Bacteria Into Shape: Mechanisms of Cell Wall Assembly and Remodeling" 

 

Key Lecture Points:

· The cell wall is essential for bacterial cell shape and integrity.

· The biogenesis of this structure is an important target for antibiotics.

· We are only just beginning to understand how cell wall synthase and remodeling proteins are regulated to build the wall.

 

Wednesday, March 22, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

Jon Clardy

harvard medical school

 

"Molecular Regulators of Complex Inter Kingdom Symbioses" 

 

Wednesday, March 29, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Research Overview:

With an overall goal of understanding how small molecules control biological processes, the laboratory focuses on biologically active small molecules, especially those known as natural products, and their interactions with larger molecules.

 

Maurine Linder

cornell university

 

"Mechanism and Consequences of Protein S-Palmitoylation" 

 

Wednesday, April 5, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Research Overview:

Our goal is to understand the biology and enzymology of protein palmitoylation, a reversible posttranslational modification of proteins that impacts their localization, trafficking, and stability. A major focus of our work is the characterization of a recently discovered family of enzymes that palmitoylate proteins

 

Martin Burke

university of illinois

 

"Making Molecular Prosthetics With a Small Molecule Synthesizer" 

 

Wednesday, April 12, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Summary Lecture:

This talk will discuss small molecules with protein like functions (molecular prosthetics) and a generalized automated platform for small molecule synthesis.

Peter Kim

stanford university

 

"Preventing Diseases with Vaccines"

 

Wednesday, April 19, 2017

12:15 P.M. — 1:15 P.M.

1220 MRB III

 

Research Overview:

We are studying the mechanism of viral membrane fusion and its inhibition by drugs and antibodies. We use the HIV envelope protein (gp120/gp41) as a model system. Some of our studies are aimed at creating an HIV vaccine that elicits antibodies against a transient, but vulnerable, intermediate in the membrane-fusion process, called the pre-hairpin intermediate. We are also interested in protein surfaces that are referred to as "non-druggable".

 

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