About
Multidisciplinary scientist focused on discovering and advancing precisely targeted…
Activity
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The #NuCrew had three stellar additions this summer: thank you to Project Onramp for connecting us with our interns, Genevieve Hayes, Alexia Walters,…
The #NuCrew had three stellar additions this summer: thank you to Project Onramp for connecting us with our interns, Genevieve Hayes, Alexia Walters,…
Liked by Henry Pelish
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⁉️WHAT WAS I THINKING⁉️… the perfect theme for a stellar line up at The Storyroom. The event sold out in a heartbeat - 260 ears - 6 fabulous…
⁉️WHAT WAS I THINKING⁉️… the perfect theme for a stellar line up at The Storyroom. The event sold out in a heartbeat - 260 ears - 6 fabulous…
Liked by Henry Pelish
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Today we report our Q2 2024 financial results, highlighting pipeline progress and reinforcing anticipated milestones. We look forward to sharing data…
Today we report our Q2 2024 financial results, highlighting pipeline progress and reinforcing anticipated milestones. We look forward to sharing data…
Liked by Henry Pelish
Experience
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Education
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Contributed to the development of a diversity-oriented synthesis (DOS) platform at Harvard. Synthesized 2,500 natural product-like small molecules and collaborated to screen the compounds in a variety of biochemical and cell-based (phenotypic) assays. From the library, we discovered secramine, an inhibitor of Golgi to plasma membrane trafficking (Pelish et. al., JACS 2001, 123(27):6740-1), which I later determined to inhibit the Ras superfamily GTPases CDC42 and Rac1.
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Publications
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Mediator Kinase Phosphorylation of STAT1 S727 Promotes Growth of Neoplasms with JAK-STAT Activation.
EBioMedicine 2017, 26: 112-125
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STAT3 Inhibitory Activity of Structurally Simplified Withaferin A Analogues
Organic Letters 2017, 19(7):1538-1541
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Identification of Mediator Kinase Substrates in Human Cells using Cortistatin A and Quantitative Phosphoproteomics.
Cell Reports 2016, 15(2):436-50
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Mediator kinase inhibition further activates super-enhancer-associated genes in AML.
Nature 2015, 526(7572):273-276
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The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes.
Journal of Natural Products. 2011, 74(4):567-73
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Use of dynasore, the small molecule inhibitor of dynamin, in the regulation of endocytosis.
Methods in Enzymology 2008, 438:77-93
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Biochemical suppression of small-molecule inhibitors: a strategy to identify inhibitor targets and signaling pathway components.
Chemistry and Biology 2006, 13(4):443-52
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Large scale synthesis of the Cdc42 inhibitor secramine A and its inhibition of cell spreading.
Org Biomol Chem. 2006, 4(22):4149-57
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Secramine inhibits Cdc42-dependent functions in cells and Cdc42 activation in vitro.
Nature Chemical Biology 2006, 2(1):39-46
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The Cdc42 inhibitor secramine B prevents cAMP-induced K+ conductance in intestinal epithelial cells.
Biochemical Pharmacology 2006, 71(12):1720-6
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An alkylsilyl-tethered, high-capacity solid support amenable to diversity-oriented synthesis for one-bead, one-stock solution chemical genetics.
Journal of Combinatorial Chemistry 2001, 3(3):312-8
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Use of biomimetic diversity-oriented synthesis to discover galanthamine-like molecules with biological properties beyond those of the natural product.
Journal of the American Chemical Society 2001, 123(27):6740-1
Patents
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Biomimetic combinatorial synthesis of polycyclic natural products.
US WO 9964379 A2 19991216
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Biomimetic preparation of a galanthamine alkaloid library for pharmaceutical use.
US US 6,797,819 B1 20040928
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PRPK-TPRKB modulators and uses thereof.
US WO 2011160042 A2 20111222
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Preparation of cortistatin analogs for the treatment of cancer.
US WO 2017142621 A1 20170824
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Syntheses and uses of cortistatin analogs.
US WO 2015100420 A1 20150702
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Syntheses of cortistatin analogs and medicinal uses thereof.
US WO 2016182932 A1 20161117
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Synthesis of cortistatin analogs and uses in treating angiogenesis associated diseases.
US WO 2017004411 A1 20170105
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Synthesis of cortistatin analogs for treating disorders mediated by CDK8 and/or CDK19.
US WO 2017112815 A1 20170629
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Targeted selection of cancer patients for treatment with specific cortistatin derivatives.
US WO 2017112823 A1 20170629
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Targeted selection of patients for treatment of cancer with cortistatin derivatives by determination of RUNX1 pathway impairment.
US WO 2016182904 A1 20161117
More activity by Henry
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📣 The #NuCrew is hiring! We are on the lookout for a Director / Senior Director, Biostatistics! 👀 Learn more about this role and other new…
📣 The #NuCrew is hiring! We are on the lookout for a Director / Senior Director, Biostatistics! 👀 Learn more about this role and other new…
Liked by Henry Pelish
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https://lnkd.in/eGRsbt6V The Pan-Mass Challenge is this weekend! It's not too late to donate to support life saving cancer research through the…
https://lnkd.in/eGRsbt6V The Pan-Mass Challenge is this weekend! It's not too late to donate to support life saving cancer research through the…
Liked by Henry Pelish
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On this day 17 years ago, Drs Soda, Mano, et al, published an article in Nature that changed the fate of hundreds of thousands of people with a very…
On this day 17 years ago, Drs Soda, Mano, et al, published an article in Nature that changed the fate of hundreds of thousands of people with a very…
Liked by Henry Pelish
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In case you missed it: ALK Positive has joined 23andMe to Launch Lung Cancer Genetics Study to Advance Research. We are excited to be…
In case you missed it: ALK Positive has joined 23andMe to Launch Lung Cancer Genetics Study to Advance Research. We are excited to be…
Liked by Henry Pelish
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Sponsored by Genentech. Today, August 1, is World Lung Cancer Day – an important day to come together to raise awareness for lung cancer patients…
Sponsored by Genentech. Today, August 1, is World Lung Cancer Day – an important day to come together to raise awareness for lung cancer patients…
Liked by Henry Pelish
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