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Afjal Hussain Miah
Researcher at GlaxoSmithKline
Publications - 22
Citations - 1619
Afjal Hussain Miah is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Ubiquitin ligase & Proteolysis targeting chimera. The author has an hindex of 11, co-authored 22 publications receiving 1196 citations. Previous affiliations of Afjal Hussain Miah include University of Cambridge.
Papers
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Journal ArticleDOI
Catalytic in vivo protein knockdown by small-molecule PROTACs
Daniel P. Bondeson,Alina Mares,Ian Edward David Smith,Ko Eunhwa,Sebastien Andre Campos,Afjal Hussain Miah,Katie E Mulholland,Natasha Routly,Dennis L. Buckley,Jeffrey L. Gustafson,Nico Zinn,Paola Grandi,Satoko Shimamura,Giovanna Bergamini,Maria Faelth-Savitski,Marcus Bantscheff,Carly S. Cox,Deborah A. Gordon,Ryan R. Willard,John J. Flanagan,Linda N. Casillas,Bartholomew J. Votta,Willem den Besten,Kristoffer Famm,Laurens Kruidenier,Paul S. Carter,John D. Harling,Ian Churcher,Craig M. Crews +28 more
TL;DR: Major improvements to the proteolysis targeting chimeras (PROTACs) method are described, a chemical knockdown strategy in which a heterobifunctional molecule recruits a specific protein target to an E3 ubiquitin ligase, resulting in the target's ubiquitination and degradation.
Journal ArticleDOI
HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins
Dennis L. Buckley,Kanak Raina,Nicole Darricarrère,John Hines,Jeffrey L. Gustafson,Ian Edward David Smith,Afjal Hussain Miah,John D. Harling,Craig M. Crews +8 more
TL;DR: The design of a novel class of PROTACs are reported that incorporate small molecule VHL ligands to successfully degrade HaloTag7 fusion proteins and are useful chemical genetic tools, due to their ability to chemically knock down widely used HaloTag 7 fusion proteins in a general fashion.
Journal ArticleDOI
Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2.
Alina Mares,Afjal Hussain Miah,Ian Edward David Smith,Mark David Rackham,Aditya R. Thawani,Jenni Cryan,Pamela A. Haile,Bartholomew J. Votta,Allison M. Beal,Carol A. Capriotti,Michael Reilly,Don T. Fisher,Nico Zinn,Marcus Bantscheff,Thomas T. MacDonald,Anna Vossenkämper,Phoebe Dace,Ian Churcher,Andrew B. Benowitz,Gillian F. Watt,Jane Denyer,Paul Scott-Stevens,John D. Harling +22 more
TL;DR: This study suggests that PROTAC has a therapeutic potential that is superior to traditional RIPK2 small-molecule inhibitors, and when coupled with low nanomolar potency, offers the potential for low human doses and infrequent dosing regimens with PROTAC medicines.
Patent
Compounds&methods for the enhanced degradation of targeted proteins&other polypeptides by an e3 ubiquitin ligase
Craig M. Crews,Dennis Buckley,Alessio Ciulli,William L. Jorgensen,Peter C. Gareiss,Inge Van Molle,Jeffrey L. Gustafson,Hyun-Seop Tae,Julien Michel,Dentin Wade Hoyer,Anke G. Roth,John D. Harling,Ian Edward David Smith,Afjal Hussain Miah,Sebastien Andre Campos,Joelle Le +15 more
TL;DR: In this paper, a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides, are described.
Journal ArticleDOI
Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach
Zuni I. Bassi,Martin Christian Fillmore,Afjal Hussain Miah,Trevor D. Chapman,Claire Maller,Emma J. Roberts,Lauren C. Davis,Darcy E. Lewis,Nicholas Galwey,Kirsty E Waddington,Valentino Parravicini,Abigail L. Macmillan-Jones,Céline Gongora,Philip G. Humphreys,Ian Churcher,Rab K. Prinjha,David F. Tough +16 more
TL;DR: By generating the first PCAF/GCN5 proteolysis targeting chimera (PROTAC), small molecules able to degrade and to potently modulate the expression of multiple inflammatory mediators in LPS-stimulated macrophages and dendritic cells are identified.