From the Knight Lab at UCSF

Chung S, Weber F, Zhong P, Tan CL, Nguyen TN, Beier KT, Hörmann N, Chang WC, Zhang Z, Do JP, Yao S, Krashes MJ, Tasic B, Cetin A, Zeng H, Knight ZA, Luo L, Dan Y (2017). Identification of preoptic sleep neurons using retrograde labelling and gene profiling. Nature. Published online 17 May 2017.

Leib DE, Zimmerman CA, Knight ZA (2016). Thirst. Current Biology 26 (24): R1260–R1265. Published online 19 December 2016. [pdf]

Tan CL, Cooke EK, Leib DE, Lin Y-C, Daly GE, Zimmerman CA, Knight ZA (2016). Warm-sensitive neurons that control body temperature. Cell 167 (1): 47–59. Published online 08 September 2016. [pdf]

Chen Y, Lin Y-C, Zimmerman CA, Essner RA, Knight ZA (2016). Hunger neurons drive feeding through a sustained, positive reinforcement signal. eLife 5: e18640. Published online 24 August 2016. [pdf]

Leib DE, Knight ZA (2016). Rapid sensing of dietary amino acid deficiency does not require GCN2. Cell Reports 16 (8): 2051–2052. Published online 23 August 2016. [pdf]

Zimmerman CA, Lin Y-C, Leib DE, Guo L, Huey EL, Daly GE, Chen Y, Knight ZA (2016). Thirst neurons anticipate the homeostatic consequences of eating and drinking. Nature 537 (7622): 680–684. Published online 03 August 2016. [pdf]

Chen Y, Knight ZA (2016). Making sense of the sensory regulation of hunger neurons. BioEssays 38 (4): 316–324. Published online 22 February 2016. [pdf]

Leib DE, Knight ZA (2015). Re-examination of dietary amino acid sensing reveals a GCN2-independent mechanism. Cell Reports 13 (6): 1081–1089. Published online 29 October 2015. [pdf]

Chen Y, Lin Y-C, Kuo T-W, Knight ZA (2015). Sensory detection of food rapidly modulates arcuate feeding circuits. Cell 160 (5): 829–841. Published online 19 February 2015. [pdf]


Earlier Work

Knight ZA*, Schmidt SF*, Birsoy K, Tan K, Friedman JM (2014). A critical role for mTORC1 in erythropoiesis and anemia. eLife 3: e01913. Published online 08 September 2014. [pdf]

Tan K, Knight ZA, Friedman JM (2014). Ablation of AgRP neurons impairs adaption to restricted feeding. Molecular Metabolism 3 (7): 694–704. Published online 10 July 2014. [pdf]

Ekstrand MI*, Nectow AR*, Knight ZA, Latcha KN, Pomeranz LE, Friedman JM (2014). Molecular profiling of neurons based on connectivity. Cell 157 (5): 1230–1242. Published online 22 May 2014. [pdf]

Knight ZA, Tan K, Birsoy K, Schmidt S, Garrison JL, Wysocki RW, Emiliano A, Ekstrand MI, Friedman JM (2012). Molecular profiling of activated neurons by phosphorylated ribosome capture. Cell 151 (5): 1126–1137. Published online 20 November 2012. [pdf]

Knight ZA (2011). For a PDK1 inhibitor, the substrate matters. Biochemical Journal 433 (2): e1–e2. Published online 15 January 2011. [pdf]

Knight ZA, Hannan KS, Greenberg ML, Friedman JM (2010). Hyperleptinemia is required for the development of leptin resistance. PLoS One 5 (6): e11376. Published online 29 June 2010. [pdf]

Knight ZA (2010). Small molecule inhibitors of the PI3-kinase family. Current Topics in Microbiology & Immunology 347: 263–278. Published online 07 May 2010. [pdf]

Williams O, Houseman BT, Kunkel EJ, Aizenstein B, Hoffman R, Knight ZA, Shokat KM (2010). Discovery of dual inhibitors of the immune cell PI3Ks p110δ and p110γ: a prototype for new anti-inflammatory drugs. Chemistry & Biology 17 (2): 123–134. Published online 25 February 2010. [pdf]

Knight ZA, Lin H, Shokat KM (2010). Targeting the cancer kinome through polypharmacology. Nature Reviews Cancer 10 (2): 130–137. Published online 01 February 2010. [pdf]

Niedermeier M, Hennessy BT, Knight ZA, Henneberg M, Hu J, Kurtova AV, Wierda WG, Keating MJ, Shokat KM, Burger JA (2009). Isoform-selective phosphoinositide 3′-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: a novel therapeutic approach. Blood 113 (22): 5549–5557. Published online 24 March 2009. [pdf]

Feldman ME, Apsel B, Uotila A, Loewith R, Knight ZA, Ruggero D, Shokat KM (2009). Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biology 7 (2): e1000038. Published online 10 February 2009. [pdf]

Fan Q-W, Cheng C, Knight ZA, Haas-Kogan D, Stokoe D, James CD, McCormick F, Shokat KM, Weiss WA (2009). EGFR signals to mTOR through PKC and independently of Akt in glioma. Science Signaling 2 (55): ra4. Published online 27 January 2009. [pdf]

Mirzoeva OK, Das D, Heiser LM, Bhattacharya S, Siwak D, Gendelman R, Bayani N, Wang NJ, Neve RM, Guan Y, Hu Z, Knight ZA, Feiler HS, Gascard P, Parvin B, Spellman PT, Shokat KM, Wyrobek AJ, Bissell MJ, McCormick F, Kuo W-L, Mills GB, Gray JW, Korn WM (2009). Basal subtype and MAPK/ERK kinase (MEK)-phosphoinositide 3-kinase feedback signaling determine susceptibility of breast cancer cells to MEK inhibition. Cancer Research 69 (2): 565–572. Published online 15 January 2009. [pdf]

Chaisuparat R, Hu J, Jham BC, Knight ZA, Shokat KM, Montaner S (2008). Dual inhibition of PI3Kα and mTOR as an alternative treatment for Kaposi's sarcoma. Cancer Research 68 (20): 8361–8368. Published online 15 October 2008. [pdf]

Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA (2008). Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nature Chemical Biology 4 (11): 691–699. Published online 12 October 2008. [pdf]

Zhang T-T, Okkenhaug K, Nashed BF, Puri KD, Knight ZA, Shokat KM, Vanhaesebroeck B, Marshall AJ (2008). Genetic or pharmaceutical blockade of p110δ phosphoinositide 3-kinase enhances IgE production. Journal of Allergy & Clinical Immunology 122 (4): 811–819. Published online 04 October 2008. [pdf]

Oda K, Okada J, Timmerman L, Rodriguez-Viciana P, Stokoe D, Shoji K, Taketani Y, Kuramoto H, Knight ZA, Shokat KM, McCormick F (2008). PIK3CA cooperates with other phosphatidylinositol 3′-kinase pathway mutations to effect oncogenic transformation. Cancer Research 68 (19): 8127–8136. Published online 30 September 2008. [pdf]

Kharas MG*, Janes MR*, Scarfone VM, Lilly MB, Knight ZA, Shokat KM, Fruman DA (2008). Ablation of PI3K blocks BCR-ABL leukemogenesis in mice, and a dual PI3K/mTOR inhibitor prevents expansion of human BCR-ABL+ leukemia cells. Journal of Clinical Investigation 118 (9): 3038–3050. Published online 14 August 2008. [pdf]

Zunder ER, Knight ZA, Houseman BT, Apsel B, Shokat KM (2008). Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110α. Cancer Cell 14 (2): 180–192. Published online 11 August 2008. [pdf]

Wang J, Knight ZA, Fiedler D, Williams O, Shokat KM, Pearce D (2008). Activity of the p110-α subunit of phosphatidylinositol-3-kinase is required for activation of epithelial sodium transport. American Journal of Physiology: Renal Physiology 295 (3): F843–F850. Published online 23 July 2008. [pdf]

Park S, Chapuis N, Bardet V, Tamburini J, Gallay N, Willems L, Knight ZA, Shokat KM, Azar N, Viguié F, Ifrah N, Dreyfus F, Mayeux P, Lacombe C, Bouscary D (2008). PI-103, a dual inhibitor of class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML. Leukemia 22 (9): 1698–1706. Published online 12 June 2008. [pdf]

Sauer S, Bruno L, Hertweck A, Finlay D, Leleu M, Spivakov M, Knight ZA, Cobb BS, Cantrell D, O'Connor E, Shokat KM, Fisher AG, Merkenschlager M (2008). T cell receptor signaling controls Foxp3 expression via PI3K, Akt, and mTOR. Proceedings of the National Academy of Sciences 105 (22): 7797–7802. Published online 28 May 2008. [pdf]

Torbett NE, Luna-Moran A, Knight ZA, Houk A, Moasser M, Weiss W, Shokat KM, Stokoe D (2008). A chemical screen in diverse breast cancer cell lines reveals genetic enhancers and suppressors of sensitivity to PI3K isoform-selective inhibition. Biochemical Journal 415 (1): 97–110. Published online 22 May 2008. [pdf]

Chen JS*, Zhou LJ*, Entin-Meer M, Yang X, Donker M, Knight ZA, Weiss W, Shokat KM, Haas-Kogan D, Stokoe D (2008). Characterization of structurally distinct, isoform-selective phosphoinositide 3′-kinase inhibitors in combination with radiation in the treatment of glioblastoma. Molecular Cancer Therapeutics 7 (4): 841–850. Published online 15 April 2008. [pdf]

Balla A, Tuymetova G, Toth B, Szentpetery Z, Zhao X, Knight ZA, Shokat K, Steinbach PJ, Balla T (2008). Design of drug-resistant alleles of type-III phosphatidylinositol 4-kinases using mutagenesis and molecular modeling. Biochemistry 47 (6): 1599–1607. Published online 19 January 2008. [pdf]

Balla A, Kim YJ, Varnai P, Szentpetery Z, Knight ZA, Shokat KM, Balla T (2008). Maintenance of hormone-sensitive phosphoinositide pools in the plasma membrane requires phosphatidylinositol 4-kinase IIIα. Molecular Biology of the Cell 19 (2): 711–721. Published online 12 December 2007. [pdf]

Knight ZA, Feldman ME, Balla A, Balla T, Shokat KM (2007). A membrane capture assay for lipid kinase activity. Nature Protocols 2 (10): 2459–2466. Published online 04 October 2007. [pdf]

Knight ZA, Garrison JL, Chan K, King DS, Shokat KM (2007). A remodelled protease that cleaves phosphotyrosine substrates. Journal of the American Chemical Society 129 (38): 11672–11673. Published online 06 September 2007. [pdf]

Fan Q-W, Cheng CK, Nicolaides TP, Hackett CS, Knight ZA, Shokat KM, Weiss WA (2007). A dual phosphoinositide-3-kinase α/mTOR inhibitor cooperates with blockade of epidermal growth factor receptor in PTEN-mutant glioma. Cancer Research 67 (17): 7960–7965. Published online 01 September 2007. [pdf]

Hung C-H*, Thomas L*, Ruby CE, Atkins KM, Morris NP, Knight ZA, Scholz I, Barklis E, Weinberg AD, Shokat KM, Thomas G (2007). HIV-1 Nef assembles a Src family kinase-ZAP-70/Syk-PI3K cascade to downregulate cell surface MHC-I. Cell Host & Microbe 1 (2): 121–133. Published online 18 April 2007. [pdf]

Knight ZA, Shokat KM (2007). Chemically targeting the PI3K family. Biochemical Society Transactions 35 (2): 245–249. Published online 01 April 2007. [pdf]

Knight ZA, Shokat KM (2007). Chemical genetics: where genetics and pharmacology meet. Cell 128 (3): 425–430. Published online 08 February 2007. [pdf]

Tóth B, Balla A, Ma H, Knight ZA, Shokat KM, Balla T (2006). Phosphatidylinositol 4-kinase IIIβ regulates the transport of ceramide between the endoplasmic reticulum and golgi. Journal of Biological Chemistry 281 (47): 36369–36377. Published online 26 September 2006. [pdf]

Van Keymeulen A*, Wong K*, Knight ZA, Govaerts C, Hahn KM, Shokat KM, Bourne HR (2006). To stabilize neutrophil polarity, PIP3 and Cdc42 augment RhoA activity at the back as well as signals at the front. Journal of Cell Biology 174 (3): 437–445. Published online 24 July 2006. [pdf]

Fan Q-W, Knight ZA, Goldenberg DD, Yu W, Mostov KE, Stokoe D, Shokat KM, Weiss WA (2006). A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell 9 (5): 341–349. Published online 15 May 2006. [pdf]

Sturgeon CM, Knight ZA, Shokat KM, Roberge M (2006). Effect of combined DNA repair inhibition and G2 checkpoint inhibition on cell cycle progression after DNA damage. Molecular Cancer Therapeutics 5 (4): 885–892. Published online 28 April 2006. [pdf]

Knight ZA, Gonzalez B, Feldman ME, Zunder ER, Goldenberg DD, Williams O, Loewith R, Stokoe D, Balla A, Toth B, Balla T, Weiss WA, Williams RL, Shokat KM (2006). A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Cell 125 (4): 733–747. Published online 27 April 2006. [pdf]

Knight ZA, Shokat KM (2006). Knock-outs and inhibitors: one in the same?. Blood 107 (2): 420–421. Published online 09 January 2006. [pdf]

Knight ZA, Shokat KM (2005). Features of selective kinase inhibitors. Cell Chemical Biology 12 (6): 621–637. Published online 24 June 2005. [pdf]

Alaimo PJ*, Knight ZA*, Shokat KM (2005). Targeting the gatekeeper residue in phosphoinositide 3-kinases. Bioorganic & Medicinal Chemistry 13 (8): 2825–2836. Published online 10 March 2005. [pdf]

Knight ZA, Chiang GG, Alaimo PJ, Kenski DM, Ho CB, Coan K, Abraham RT, Shokat KM (2004). Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold. Bioorganic & Medicinal Chemistry 12 (17): 4749–4759. Published online 20 July 2004. [pdf]

Knight ZA, Schilling B, Row RH, Kenski DM, Gibson BW, Shokat KM (2003). Phosphospecific proteolysis for mapping sites of protein phosphorylation. Nature Biotechnology 21 (9): 1047–1054. Published online 17 August 2003. [pdf]

Tzfati Y, Knight ZA, Roy J, Blackburn EH (2003). A novel pseudoknot element is essential for the action of a yeast telomerase. Genes & Development 17 (14): 1779–1788. Published online 27 June 2003. [pdf]

Knight ZA (2000). Another possible mechanism of resistance to STI571. Blood 96 (12): 4003–4005. Published online 01 December 2000. [pdf]

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