A. Gill

发表

Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring.

Richard D. Taylor, Esteban Roman, Steven Whittaker, 2009, Journal of medicinal chemistry.

Heart regeneration: opportunities and challenges for drug discovery with novel chemical and therapeutic methods or agents.

A. Plowright, O. Engkvist, A. Gill, 2014, Angewandte Chemie.

Stapled Vasoactive Intestinal Peptide (VIP) Derivatives Improve VPAC2 Agonism and Glucose-Dependent Insulin Secretion.

A. Gill, Cl Priest, F. Giordanetto, 2013, ACS medicinal chemistry letters.

Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation.

Christopher W Murray, Alessandro Padova, Jayne Curry, 2005, Journal of medicinal chemistry.

What is the most important approach in current drug discovery: doing the right things or doing things right?

A. Plowright, A. Gill, T. Elebring, 2012, Drug discovery today.

Allosteric Inhibition of SHP2 Stimulates Antitumor Immunity by Transforming the Immunosuppressive Environment

M. Goldsmith, Mallika Singh, R. Nichols, 2020, Cancer Research.

A novel series of IKKβ inhibitors part II: description of a potent and pharmacologically active series of analogs.

N. Walker, R. C. Hawley, C. Broka, 2011, Bioorganic & medicinal chemistry letters.

Structure guided lead generation for M. tuberculosis thymidylate kinase (Mtb TMK): discovery of 3-cyanopyridone and 1,6-naphthyridin-2-one as potent inhibitors.

S. Prasad, J. Tucker, A. Gill, 2015, Journal of medicinal chemistry.

Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.

Mladen Vinković, Paul G Wyatt, Jayne Curry, 2009, Journal of medicinal chemistry.

Automated iterative Csp3–C bond formation

A. Gill, M. Burke, Danielle L. Gray, 2022, Nature.

Bi-steric mTORC1-selective Inhibitors activate 4EBP1 reversing MYC-induced tumorigenesis and synergize with immunotherapy

D. Felsher, Mallika Singh, A. Gill, 2022, bioRxiv.

RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers

G. Kiss, M. Goldsmith, Mallika Singh, 2018, Nature Cell Biology.

Efficacy of SHP2 phosphatase inhibition in cancers with nucleotide-cycling oncogenic RAS, RAS-GTP dependent oncogenic BRAF and NF1 loss

G. Kiss, M. Goldsmith, Mallika Singh, 2017, bioRxiv.

Abstract 3597: Direct targeting of KRASG12X mutant cancers with RMC-6236, a first-in-class, RAS-selective, orally bioavailable, tri-complex RASMULTI(ON) inhibitor

Mallika Singh, A. Gill, W. C. Gustafson, 2022, Cancer Research.

Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth

G. Kiss, N. Rosen, Mallika Singh, 2021, Nature Chemical Biology.

Small molecule Son of Sevenless 1 (SOS1) inhibitors: a review of the patent literature

A. Gill, E. Griffen, Severin Thompson, 2021, Expert opinion on therapeutic patents.

New lead generation strategies for protein kinase inhibitors - fragment based screening approaches.

A. Gill, Adrian Gill, 2004, Mini reviews in medicinal chemistry.

The Discovery of Novel Protein Kinase Inhibitors by Using Fragment‐Based High‐Throughput X‐ray Crystallography

H. Jhoti, A. Gill, Harren Jhoti, 2005, Chembiochem : a European journal of chemical biology.

Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).

Richard D. Taylor, H. Dijkstra, S. Whittaker, 2009, Journal of medicinal chemistry.

Abstract 1261: A next generation tri-complex KRASG12C(ON) inhibitor directly targets the active, GTP-bound state of mutant RAS and may overcome resistance to KRASG12C(OFF) inhibition

Mallika Singh, R. Nichols, A. Gill, 2021, Experimental and Molecular Therapeutics.

Abstract 3595: RMC-6291, a next-generation tri-complex KRASG12C(ON) inhibitor, outperforms KRASG12C(OFF) inhibitors in preclinical models of KRASG12C cancers

Mallika Singh, A. Gill, J. Knox, 2022, Cancer Research.

Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors

G. Wang, G. Kiss, Mallika Singh, 2022, Journal of medicinal chemistry.

A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit.

N. Walker, R. C. Hawley, C. Broka, 2011, Bioorganic & medicinal chemistry letters.

Kinetic efficiency: the missing metric for enhancing compound quality?

A. Gill, G. Holdgate, Adrian L Gill, 2011, Drug discovery today.

Abstract 3596: RM-036, a first-in-class, orally-bioavailable, Tri-Complex covalent KRASG12D(ON) inhibitor, drives profound anti-tumor activity in KRASG12D mutant tumor models

Mallika Singh, A. Gill, C. Weller, 2022, Cancer Research.

Abstract 3598: A first-in-class tri-complex KRASG13C(ON) inhibitor validates therapeutic targeting of KRASG13Cand drives tumor regressions in preclinical models

Mallika Singh, A. Gill, J. Knox, 2022, Cancer Research.

Using Matched Molecular Series as a Predictive Tool To Optimize Biological Activity

Jonas Boström, Roger A. Sayle, Noel M. O'Boyle, 2014, Journal of medicinal chemistry.

Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors.

A. Gill, James S. Scott, J. Swales, 2012, Bioorganic & medicinal chemistry letters.

287 POSTER Fragment-based discovery of AT9283; a multi-targeted kinase inhibitor with potent Aurora kinase activity

V. Berdini, P. Wyatt, L. Fazal, 2008 .

Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS

Mallika Singh, R. Nichols, Y. Pourfarjam, 2023, Science.

A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development.

M. Verdonk, A. Gill, Adrian L Gill, 2007, Current topics in medicinal chemistry.

What is the most important approach in current drug discovery: doing the right things or doing things right?

A. Plowright, A. Gill, Adrian L Gill, 2012, Drug discovery today.

Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.

V. Berdini, P. Wyatt, L. Fazal, 2009, Journal of medicinal chemistry.

Heart regeneration: opportunities and challenges for drug discovery with novel chemical and therapeutic methods or agents.

A. Plowright, O. Engkvist, A. Gill, 2014, Angewandte Chemie.